You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameOmapatrilat
Accession NumberDB00886  (APRD00443)
TypeSmall Molecule
GroupsInvestigational
DescriptionOmapatrilat is an investigational drug that inhibits both neutral endopeptidase (NEP) and angiotensin converting enzyme (ACE). NEP inhibition results in elevated natriuretic peptide levels, promoting natriuresis, diuresis, vasodilation, and reductions in preload and ventricular remodeling. This drug from BMS was not approved by the FDA due to angioedema safety concerns.
Structure
Thumb
Synonyms
Omapatrilate
External Identifiers
  • BMS 186716
  • BMS-186716
Approved Prescription ProductsNot Available
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
VanlevNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNII36NLI90E7T
CAS number167305-00-2
WeightAverage: 408.53
Monoisotopic: 408.117749609
Chemical FormulaC19H24N2O4S2
InChI KeyLVRLSYPNFFBYCZ-VGWMRTNUSA-N
InChI
InChI=1S/C19H24N2O4S2/c22-17(15(26)11-12-5-2-1-3-6-12)20-13-9-10-27-16-8-4-7-14(19(24)25)21(16)18(13)23/h1-3,5-6,13-16,26H,4,7-11H2,(H,20,22)(H,24,25)/t13-,14-,15-,16-/m0/s1
IUPAC Name
(4S,7S,10aS)-5-oxo-4-[(2S)-3-phenyl-2-sulfanylpropanamido]-octahydro-2H-pyrido[2,1-b][1,3]thiazepine-7-carboxylic acid
SMILES
[H][C@]12CCC[[email protected]](N1C(=O)[[email protected]](CCS2)NC(=O)[C@@H](S)CC1=CC=CC=C1)C(O)=O
Pharmacology
IndicationFor the treatment of hypertension.
Structured Indications Not Available
PharmacodynamicsOmapatrilat is used to treat hypertension. Vasopeptidase inhibitor that simultaneously inhibits angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP). Omapatrilat lowers blood pressure by inhibiting the action of the angiotensin converting enzyme (ACE), which causes blood vessels to constrict. But unlike other drugs, omapatrilat also inhibits another enzyme known as neutral endopeptidase (NEP), which helps blood vessels relax. Omapatrilat demonstrated greater reduction in blood pressure than the ACE inhibitor lisinopril in individuals with salt-sensitive hypertension who typically do not respond well to ACE inhibitors.
Mechanism of actionOmapatrilat binds to both angiotensin converting enzyme and neutral endopeptidase. This results in a decrease renin-angiotensin-aldosterone production and increase natriuretic peptidase circulation.
TargetKindPharmacological actionActionsOrganismUniProt ID
Angiotensin-converting enzymeProteinunknownNot AvailableHumanP12821 details
NeprilysinProteinyesNot AvailableHumanP08473 details
Related Articles
AbsorptionThe absolute oral bioavailability of omapatrilat is 20% to 30% and the absorption is not affected by food intake.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Hepatic

Route of eliminationNot Available
Half lifeNot Available
ClearanceNot Available
ToxicitySide effects include hyperkalemia, cough, hypotension, increased SrCr, and dizziness. Dizziness, diarrhea, vision disturbance, hypotension and angioedema
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE may increase the hypotensive activities of Omapatrilat.Experimental
AbacavirThe serum concentration of Abacavir can be decreased when it is combined with Omapatrilat.Approved, Investigational
AcebutololOmapatrilat may increase the hypotensive activities of Acebutolol.Approved
AceclofenacThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Aceclofenac.Approved
AcetovanilloneThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Acetovanillone.Investigational
Acetylsalicylic acidAcetylsalicylic acid may decrease the antihypertensive activities of Omapatrilat.Approved, Vet Approved
AdapaleneThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Adapalene.Approved
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Omapatrilat.Approved, Investigational
AliskirenAliskiren may increase the hyperkalemic activities of Omapatrilat.Approved, Investigational
AllopurinolThe risk of a hypersensitivity reaction to Allopurinol is increased when it is combined with Omapatrilat.Approved
AlogliptinThe risk or severity of adverse effects can be increased when Alogliptin is combined with Omapatrilat.Approved
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Omapatrilat.Approved, Illicit, Investigational
AlprenololAlprenolol may increase the hypotensive activities of Omapatrilat.Approved, Withdrawn
AmbrisentanOmapatrilat may increase the hypotensive activities of Ambrisentan.Approved, Investigational
Ambroxol acefyllinateThe serum concentration of Ambroxol acefyllinate can be decreased when it is combined with Omapatrilat.Experimental
AmifostineOmapatrilat may increase the hypotensive activities of Amifostine.Approved, Investigational
AmilorideAmiloride may increase the hyperkalemic activities of Omapatrilat.Approved
AmineptineThe serum concentration of Amineptine can be increased when it is combined with Omapatrilat.Illicit, Withdrawn
AminophyllineThe serum concentration of Aminophylline can be decreased when it is combined with Omapatrilat.Approved
Aminosalicylic AcidAminosalicylic Acid may decrease the antihypertensive activities of Omapatrilat.Approved
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Omapatrilat.Approved
AmlodipineAmlodipine may increase the hypotensive activities of Omapatrilat.Approved
AnisodamineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Anisodamine.Investigational
AntipyrineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Antipyrine.Approved
ApremilastThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Apremilast.Approved, Investigational
AprotininAprotinin may decrease the antihypertensive activities of Omapatrilat.Approved, Withdrawn
ArdeparinArdeparin may increase the hyperkalemic activities of Omapatrilat.Approved, Withdrawn
AtenololAtenolol may increase the hypotensive activities of Omapatrilat.Approved
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Omapatrilat.Approved
AzapropazoneThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Azapropazone.Withdrawn
AzathioprineOmapatrilat may increase the myelosuppressive activities of Azathioprine.Approved
AzelastineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Azelastine.Approved
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Omapatrilat.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Balsalazide.Approved, Investigational
BemiparinBemiparin may increase the hyperkalemic activities of Omapatrilat.Approved
BenazeprilBenazepril may increase the hypotensive activities of Omapatrilat.Approved, Investigational
BendroflumethiazideBendroflumethiazide may increase the hypotensive activities of Omapatrilat.Approved
BenmoxinBenmoxin may increase the hypotensive activities of Omapatrilat.Withdrawn
BenoxaprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Benoxaprofen.Withdrawn
BepridilOmapatrilat may increase the hypotensive activities of Bepridil.Approved, Withdrawn
BetaxololBetaxolol may increase the hypotensive activities of Omapatrilat.Approved
BethanidineBethanidine may increase the hypotensive activities of Omapatrilat.Approved
Betulinic AcidThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Betulinic Acid.Investigational
BimatoprostOmapatrilat may increase the hypotensive activities of Bimatoprost.Approved, Investigational
BisoprololBisoprolol may increase the hypotensive activities of Omapatrilat.Approved
BoceprevirThe serum concentration of Omapatrilat can be decreased when it is combined with Boceprevir.Approved
BosentanBosentan may increase the hypotensive activities of Omapatrilat.Approved, Investigational
BretyliumOmapatrilat may increase the hypotensive activities of Bretylium.Approved
BrimonidineBrimonidine may increase the hypotensive activities of Omapatrilat.Approved
BrimonidineBrimonidine may increase the antihypertensive activities of Omapatrilat.Approved
BromfenacThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Bromfenac.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Omapatrilat.Approved, Investigational
BucillamineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Bucillamine.Investigational
BumetanideBumetanide may increase the hypotensive activities of Omapatrilat.Approved
BupranololOmapatrilat may increase the hypotensive activities of Bupranolol.Approved
CabergolineThe serum concentration of Cabergoline can be increased when it is combined with Omapatrilat.Approved
CanagliflozinCanagliflozin may increase the hyperkalemic activities of Omapatrilat.Approved
CandesartanThe risk or severity of adverse effects can be increased when Candesartan is combined with Omapatrilat.Approved
CandoxatrilCandoxatril may increase the hypotensive activities of Omapatrilat.Experimental
CaptoprilOmapatrilat may increase the hypotensive activities of Captopril.Approved
CarbamazepineThe metabolism of Omapatrilat can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneCaroxazone may increase the hypotensive activities of Omapatrilat.Withdrawn
CarprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Carprofen.Approved, Vet Approved, Withdrawn
CarteololCarteolol may increase the hypotensive activities of Omapatrilat.Approved
CarvedilolOmapatrilat may increase the hypotensive activities of Carvedilol.Approved, Investigational
CastanospermineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Castanospermine.Experimental
CelecoxibThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Celecoxib.Approved, Investigational
CeliprololOmapatrilat may increase the hypotensive activities of Celiprolol.Approved, Investigational
CertoparinCertoparin may increase the hyperkalemic activities of Omapatrilat.Approved
ChloroquineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Chloroquine.Approved, Vet Approved
ChlorothiazideChlorothiazide may increase the hypotensive activities of Omapatrilat.Approved, Vet Approved
ChlorotrianiseneThe serum concentration of Chlorotrianisene can be decreased when it is combined with Omapatrilat.Withdrawn
ChlorthalidoneChlorthalidone may increase the hypotensive activities of Omapatrilat.Approved
CilazaprilOmapatrilat may increase the hypotensive activities of Cilazapril.Approved
CiprofloxacinOmapatrilat may increase the arrhythmogenic activities of Ciprofloxacin.Approved, Investigational
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Omapatrilat.Approved, Investigational, Withdrawn
ClarithromycinThe therapeutic efficacy of Clarithromycin can be decreased when used in combination with Omapatrilat.Approved
ClomipramineThe serum concentration of Clomipramine can be increased when it is combined with Omapatrilat.Approved, Vet Approved
ClonidineClonidine may increase the hypotensive activities of Omapatrilat.Approved
ClonixinThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Clonixin.Approved
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be decreased when it is combined with Omapatrilat.Approved
CryptenamineCryptenamine may increase the hypotensive activities of Omapatrilat.Approved
CurcuminThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Curcumin.Investigational
CyclobenzaprineThe serum concentration of Cyclobenzaprine can be increased when it is combined with Omapatrilat.Approved
CyclophosphamideThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Omapatrilat.Approved, Investigational, Vet Approved
CyclothiazideCyclothiazide may increase the hypotensive activities of Omapatrilat.Approved
D-LimoneneThe risk or severity of adverse effects can be increased when Omapatrilat is combined with D-Limonene.Investigational
DalteparinDalteparin may increase the hyperkalemic activities of Omapatrilat.Approved
DapoxetineDapoxetine may increase the orthostatic hypotensive activities of Omapatrilat.Investigational
DebrisoquinOmapatrilat may increase the hypotensive activities of Debrisoquin.Approved
DelavirdineThe serum concentration of Delavirdine can be decreased when it is combined with Omapatrilat.Approved
dersalazinedersalazine may decrease the antihypertensive activities of Omapatrilat.Investigational
DeserpidineOmapatrilat may increase the hypotensive activities of Deserpidine.Approved
DesipramineThe serum concentration of Desipramine can be increased when it is combined with Omapatrilat.Approved
DiazoxideDiazoxide may increase the hypotensive activities of Omapatrilat.Approved
DiclofenacThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Diclofenac.Approved, Vet Approved
DienestrolThe serum concentration of Dienestrol can be decreased when it is combined with Omapatrilat.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be decreased when it is combined with Omapatrilat.Approved
DiflunisalDiflunisal may decrease the antihypertensive activities of Omapatrilat.Approved
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Omapatrilat.Approved
DihydralazineOmapatrilat may increase the hypotensive activities of Dihydralazine.Investigational
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Omapatrilat.Approved
DiltiazemThe metabolism of Diltiazem can be decreased when combined with Omapatrilat.Approved
DorzolamideDorzolamide may increase the hypotensive activities of Omapatrilat.Approved
DosulepinThe serum concentration of Dosulepin can be increased when it is combined with Omapatrilat.Approved
DoxazosinDoxazosin may increase the hypotensive activities of Omapatrilat.Approved
DoxepinThe serum concentration of Doxepin can be increased when it is combined with Omapatrilat.Approved
DrospirenoneOmapatrilat may increase the hyperkalemic activities of Drospirenone.Approved
DroxicamThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Droxicam.Approved
DuvelisibThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Duvelisib.Investigational
DyphyllineThe serum concentration of Dyphylline can be decreased when it is combined with Omapatrilat.Approved
E6201The risk or severity of adverse effects can be increased when Omapatrilat is combined with E6201.Investigational
EbselenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Ebselen.Investigational
EfonidipineOmapatrilat may increase the hypotensive activities of Efonidipine.Approved
EnalaprilEnalapril may increase the hypotensive activities of Omapatrilat.Approved, Vet Approved
EnalaprilatOmapatrilat may increase the hypotensive activities of Enalaprilat.Approved
EnfuvirtideThe serum concentration of Enfuvirtide can be increased when it is combined with Omapatrilat.Approved, Investigational
EnoxaparinEnoxaparin may increase the hyperkalemic activities of Omapatrilat.Approved
EpirizoleThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Epirizole.Approved
EplerenoneEplerenone may increase the hyperkalemic activities of Omapatrilat.Approved
EpoprostenolOmapatrilat may increase the hypotensive activities of Epoprostenol.Approved
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Omapatrilat.Approved
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Omapatrilat.Approved
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Omapatrilat.Approved
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Omapatrilat.Approved
EsmirtazapineThe serum concentration of Esmirtazapine can be increased when it is combined with Omapatrilat.Investigational
EstradiolThe serum concentration of Estradiol can be decreased when it is combined with Omapatrilat.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Estramustine can be decreased when it is combined with Omapatrilat.Approved
Estrogens, esterifiedThe serum concentration of Estrogens, esterified can be decreased when it is combined with Omapatrilat.Approved
Estrone sulfateThe serum concentration of Estrone sulfate can be decreased when it is combined with Omapatrilat.Approved
Etacrynic acidEtacrynic acid may increase the hypotensive activities of Omapatrilat.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Etanercept.Approved, Investigational
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be decreased when it is combined with Omapatrilat.Approved
EtodolacThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Etodolac.Approved, Investigational, Vet Approved
EtofenamateThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Etofenamate.Approved
EtoricoxibThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Etoricoxib.Approved, Investigational
EtravirineThe serum concentration of Etravirine can be decreased when it is combined with Omapatrilat.Approved
Evening primrose oilThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Evening primrose oil.Approved
EverolimusThe risk or severity of adverse effects can be increased when Everolimus is combined with Omapatrilat.Approved
exisulindThe risk or severity of adverse effects can be increased when Omapatrilat is combined with exisulind.Investigational
FelodipineOmapatrilat may increase the hypotensive activities of Felodipine.Approved, Investigational
FenbufenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Fenbufen.Approved
FenoldopamFenoldopam may increase the hypotensive activities of Omapatrilat.Approved
FenoprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Fenoprofen.Approved
FloctafenineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Floctafenine.Approved, Withdrawn
FlunixinThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Flunixin.Vet Approved
FlurbiprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Flurbiprofen.Approved, Investigational
ForasartanThe risk or severity of adverse effects can be increased when Forasartan is combined with Omapatrilat.Experimental
FosinoprilFosinopril may increase the hypotensive activities of Omapatrilat.Approved
FurazolidoneFurazolidone may increase the hypotensive activities of Omapatrilat.Approved, Vet Approved
FurosemideFurosemide may increase the hypotensive activities of Omapatrilat.Approved, Vet Approved
GarlicThe serum concentration of Omapatrilat can be decreased when it is combined with Garlic.Approved
GuanabenzGuanabenz may increase the hypotensive activities of Omapatrilat.Approved
GuanadrelGuanadrel may increase the hypotensive activities of Omapatrilat.Approved
GuanethidineOmapatrilat may increase the hypotensive activities of Guanethidine.Approved
GuanfacineOmapatrilat may increase the hypotensive activities of Guanfacine.Approved, Investigational
HeparinHeparin may increase the hyperkalemic activities of Omapatrilat.Approved, Investigational
HexamethoniumOmapatrilat may increase the hypotensive activities of Hexamethonium.Experimental
HexestrolThe serum concentration of Hexestrol can be decreased when it is combined with Omapatrilat.Withdrawn
HigenamineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Higenamine.Investigational
HMPL-004The risk or severity of adverse effects can be increased when Omapatrilat is combined with HMPL-004.Investigational
HydracarbazineHydracarbazine may increase the hypotensive activities of Omapatrilat.Approved
HydralazineOmapatrilat may increase the hypotensive activities of Hydralazine.Approved
HydrochlorothiazideOmapatrilat may increase the hypotensive activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the hypotensive activities of Omapatrilat.Approved
IbuprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Ibuprofen.Approved
IbuproxamThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Ibuproxam.Withdrawn
IcatibantIcatibant may decrease the antihypertensive activities of Omapatrilat.Approved
IloprostIloprost may increase the hypotensive activities of Omapatrilat.Approved, Investigational
ImidaprilOmapatrilat may increase the hypotensive activities of Imidapril.Investigational
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Omapatrilat.Approved
IndapamideIndapamide may increase the hypotensive activities of Omapatrilat.Approved
IndenololOmapatrilat may increase the hypotensive activities of Indenolol.Withdrawn
IndomethacinThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Indomethacin.Approved, Investigational
IndoprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Indoprofen.Withdrawn
IndoraminOmapatrilat may increase the hypotensive activities of Indoramin.Withdrawn
IproclozideIproclozide may increase the hypotensive activities of Omapatrilat.Withdrawn
IproniazidIproniazid may increase the hypotensive activities of Omapatrilat.Withdrawn
IrbesartanThe risk or severity of adverse effects can be increased when Irbesartan is combined with Omapatrilat.Approved, Investigational
IronThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Iron.Approved
Iron DextranThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Iron Dextran.Approved, Vet Approved
IsocarboxazidIsocarboxazid may increase the hypotensive activities of Omapatrilat.Approved
IsoxicamThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Isoxicam.Withdrawn
IsradipineIsradipine may increase the hypotensive activities of Omapatrilat.Approved
KebuzoneThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Kebuzone.Experimental
KetanserinOmapatrilat may increase the hypotensive activities of Ketanserin.Investigational
KetoprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Ketoprofen.Approved, Vet Approved
KetorolacThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Ketorolac.Approved
LabetalolLabetalol may increase the hypotensive activities of Omapatrilat.Approved
LacidipineOmapatrilat may increase the hypotensive activities of Lacidipine.Approved
Lanthanum carbonateThe serum concentration of Omapatrilat can be decreased when it is combined with Lanthanum carbonate.Approved
LatanoprostLatanoprost may increase the hypotensive activities of Omapatrilat.Approved, Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Leflunomide.Approved, Investigational
LercanidipineLercanidipine may increase the hypotensive activities of Omapatrilat.Approved, Investigational
LinagliptinThe risk or severity of adverse effects can be increased when Linagliptin is combined with Omapatrilat.Approved
LisinoprilLisinopril may increase the hypotensive activities of Omapatrilat.Approved, Investigational
LisofyllineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Lisofylline.Investigational
LithiumThe serum concentration of Lithium can be increased when it is combined with Omapatrilat.Approved
LofexidineOmapatrilat may increase the hypotensive activities of Lofexidine.Approved, Investigational
LornoxicamThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Lornoxicam.Approved
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Omapatrilat.Approved
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Omapatrilat.Approved, Investigational
LoxoprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Loxoprofen.Approved
LumiracoxibThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Lumiracoxib.Approved, Investigational
MacitentanOmapatrilat may increase the hypotensive activities of Macitentan.Approved
Magnesium salicylateThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Magnesium salicylate.Approved
ManidipineOmapatrilat may increase the hypotensive activities of Manidipine.Approved
MasoprocolThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Masoprocol.Approved
MebanazineMebanazine may increase the hypotensive activities of Omapatrilat.Withdrawn
MecamylamineMecamylamine may increase the hypotensive activities of Omapatrilat.Approved
Meclofenamic acidThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Meclofenamic acid.Approved, Vet Approved
Mefenamic acidThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Mefenamic acid.Approved
MeloxicamThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Meloxicam.Approved, Vet Approved
MesalazineMesalazine may decrease the antihypertensive activities of Omapatrilat.Approved
MestranolThe serum concentration of Mestranol can be decreased when it is combined with Omapatrilat.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Metamizole.Withdrawn
MethallenestrilThe serum concentration of Methallenestril can be decreased when it is combined with Omapatrilat.Experimental
MethyclothiazideMethyclothiazide may increase the hypotensive activities of Omapatrilat.Approved
MethyldopaOmapatrilat may increase the hypotensive activities of Methyldopa.Approved
Methylene blueMethylene blue may increase the hypotensive activities of Omapatrilat.Investigational
MethylphenidateMethylphenidate may decrease the antihypertensive activities of Omapatrilat.Approved, Investigational
MetipranololOmapatrilat may increase the hypotensive activities of Metipranolol.Approved
MetolazoneMetolazone may increase the hypotensive activities of Omapatrilat.Approved
MetoprololMetoprolol may increase the hypotensive activities of Omapatrilat.Approved, Investigational
MetyrosineOmapatrilat may increase the hypotensive activities of Metyrosine.Approved
MibefradilOmapatrilat may increase the hypotensive activities of Mibefradil.Withdrawn
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Omapatrilat.Approved, Illicit
MinaprineMinaprine may increase the hypotensive activities of Omapatrilat.Approved
MinoxidilMinoxidil may increase the hypotensive activities of Omapatrilat.Approved
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Omapatrilat.Approved
MizoribineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Mizoribine.Investigational
MoclobemideMoclobemide may increase the hypotensive activities of Omapatrilat.Approved
MoexiprilMoexipril may increase the hypotensive activities of Omapatrilat.Approved
MolsidomineMolsidomine may increase the hypotensive activities of Omapatrilat.Approved
MoxonidineOmapatrilat may increase the hypotensive activities of Moxonidine.Approved
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Mycophenolate mofetil.Approved, Investigational
Mycophenolic acidThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Mycophenolic acid.Approved
NabumetoneThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Nabumetone.Approved
NadololOmapatrilat may increase the hypotensive activities of Nadolol.Approved
NadroparinNadroparin may increase the hyperkalemic activities of Omapatrilat.Approved
NafamostatThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Nafamostat.Investigational
NaftifineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Naftifine.Approved
NaftopidilOmapatrilat may increase the hypotensive activities of Naftopidil.Investigational
NaproxenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Naproxen.Approved, Vet Approved
NCX 4016The risk or severity of adverse effects can be increased when Omapatrilat is combined with NCX 4016.Investigational
NebivololOmapatrilat may increase the hypotensive activities of Nebivolol.Approved, Investigational
NefazodoneThe serum concentration of Nefazodone can be increased when it is combined with Omapatrilat.Approved, Withdrawn
NepafenacThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Nepafenac.Approved
NialamideNialamide may increase the hypotensive activities of Omapatrilat.Withdrawn
NicardipineNicardipine may increase the hypotensive activities of Omapatrilat.Approved
NicorandilNicorandil may increase the hyperkalemic activities of Omapatrilat.Approved
Niflumic AcidThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Niflumic Acid.Approved
NiguldipineOmapatrilat may increase the hypotensive activities of Niguldipine.Experimental
NilvadipineOmapatrilat may increase the hypotensive activities of Nilvadipine.Approved
NimesulideThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Nimesulide.Approved, Withdrawn
NimodipineNimodipine may increase the hypotensive activities of Omapatrilat.Approved
NisoldipineNisoldipine may increase the hypotensive activities of Omapatrilat.Approved
NitrendipineOmapatrilat may increase the hypotensive activities of Nitrendipine.Approved
NitroaspirinNitroaspirin may decrease the antihypertensive activities of Omapatrilat.Investigational
NitroprussideNitroprusside may increase the hypotensive activities of Omapatrilat.Approved
NortriptylineThe serum concentration of Nortriptyline can be increased when it is combined with Omapatrilat.Approved
ObinutuzumabOmapatrilat may increase the hypotensive activities of Obinutuzumab.Approved
OctamoxinOctamoxin may increase the hypotensive activities of Omapatrilat.Withdrawn
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Omapatrilat.Approved, Investigational
OlopatadineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Olopatadine.Approved
OlsalazineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Olsalazine.Approved
OpipramolThe serum concentration of Opipramol can be increased when it is combined with Omapatrilat.Investigational
OrgoteinThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Orgotein.Vet Approved
OxaprozinThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Oxaprozin.Approved
OxprenololOmapatrilat may increase the hypotensive activities of Oxprenolol.Approved
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Oxyphenbutazone.Withdrawn
ParecoxibThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Parecoxib.Approved
PargylinePargyline may increase the hypotensive activities of Omapatrilat.Approved
ParnaparinParnaparin may increase the hyperkalemic activities of Omapatrilat.Approved
PenbutololOmapatrilat may increase the hypotensive activities of Penbutolol.Approved, Investigational
PentoliniumOmapatrilat may increase the hypotensive activities of Pentolinium.Approved
PentoxifyllinePentoxifylline may increase the hypotensive activities of Omapatrilat.Approved, Investigational
PerindoprilPerindopril may increase the hypotensive activities of Omapatrilat.Approved
PethidineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Pethidine.Approved
PhenelzinePhenelzine may increase the hypotensive activities of Omapatrilat.Approved
PheniprazinePheniprazine may increase the hypotensive activities of Omapatrilat.Withdrawn
PhenoxybenzamineOmapatrilat may increase the hypotensive activities of Phenoxybenzamine.Approved
PhenoxypropazinePhenoxypropazine may increase the hypotensive activities of Omapatrilat.Withdrawn
PhentolaminePhentolamine may increase the hypotensive activities of Omapatrilat.Approved
PhenylbutazoneThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Phenylbutazone.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Pimecrolimus.Approved, Investigational
PimozideThe serum concentration of Pimozide can be increased when it is combined with Omapatrilat.Approved
PinacidilOmapatrilat may increase the hypotensive activities of Pinacidil.Withdrawn
PindololOmapatrilat may increase the hypotensive activities of Pindolol.Approved
PiretanidePiretanide may increase the hypotensive activities of Omapatrilat.Experimental
PirfenidoneThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Pirfenidone.Investigational
PirlindolePirlindole may increase the hypotensive activities of Omapatrilat.Approved
PiroxicamThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Piroxicam.Approved, Investigational
PivhydrazinePivhydrazine may increase the hypotensive activities of Omapatrilat.Withdrawn
PolythiazideOmapatrilat may increase the hypotensive activities of Polythiazide.Approved
PrazosinPrazosin may increase the hypotensive activities of Omapatrilat.Approved
PregabalinThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Pregabalin.Approved, Illicit, Investigational
PropacetamolThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Propacetamol.Approved
PropranololPropranolol may increase the hypotensive activities of Omapatrilat.Approved, Investigational
ProtriptylineThe serum concentration of Protriptyline can be increased when it is combined with Omapatrilat.Approved
PTC299The risk or severity of adverse effects can be increased when Omapatrilat is combined with PTC299.Investigational
QuinaprilQuinapril may increase the hypotensive activities of Omapatrilat.Approved, Investigational
QuinethazoneQuinethazone may increase the hypotensive activities of Omapatrilat.Approved
QuinineQuinine may increase the hypotensive activities of Omapatrilat.Approved
RamiprilRamipril may increase the hypotensive activities of Omapatrilat.Approved
RasagilineRasagiline may increase the hypotensive activities of Omapatrilat.Approved
RemikirenRemikiren may increase the hypotensive activities of Omapatrilat.Approved
RescinnamineOmapatrilat may increase the hypotensive activities of Rescinnamine.Approved
ReserpineReserpine may increase the hypotensive activities of Omapatrilat.Approved
ResveratrolThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Resveratrol.Experimental, Investigational
ReviparinReviparin may increase the hyperkalemic activities of Omapatrilat.Approved
RilmenidineOmapatrilat may increase the hypotensive activities of Rilmenidine.Investigational
RiociguatThe serum concentration of Riociguat can be increased when it is combined with Omapatrilat.Approved
RituximabOmapatrilat may increase the hypotensive activities of Rituximab.Approved
RofecoxibThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Rofecoxib.Investigational, Withdrawn
RosuvastatinThe serum concentration of Rosuvastatin can be increased when it is combined with Omapatrilat.Approved
SacubitrilThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Sacubitril.Approved
SafrazineSafrazine may increase the hypotensive activities of Omapatrilat.Withdrawn
SalicylamideThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Salicylamide.Approved
Salicylic acidSalicylic acid may decrease the antihypertensive activities of Omapatrilat.Approved, Vet Approved
SalsalateThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Salsalate.Approved
SaprisartanThe risk or severity of adverse effects can be increased when Saprisartan is combined with Omapatrilat.Experimental
SaralasinThe risk or severity of adverse effects can be increased when Saralasin is combined with Omapatrilat.Investigational
SaxagliptinThe risk or severity of adverse effects can be increased when Saxagliptin is combined with Omapatrilat.Approved
SelegilineSelegiline may increase the hypotensive activities of Omapatrilat.Approved, Investigational, Vet Approved
SelexipagOmapatrilat may increase the hypotensive activities of Selexipag.Approved
SeratrodastThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Seratrodast.Approved, Investigational
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Omapatrilat.Approved, Investigational
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Omapatrilat.Approved
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Omapatrilat.Approved
SirolimusThe risk or severity of adverse effects can be increased when Sirolimus is combined with Omapatrilat.Approved, Investigational
SitagliptinThe risk or severity of adverse effects can be increased when Sitagliptin is combined with Omapatrilat.Approved, Investigational
SitaxentanOmapatrilat may increase the hypotensive activities of Sitaxentan.Approved, Investigational, Withdrawn
Sodium aurothiomalateThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Sodium aurothiomalate.Approved
SpiraprilOmapatrilat may increase the hypotensive activities of Spirapril.Approved
SpironolactoneSpironolactone may increase the hyperkalemic activities of Omapatrilat.Approved
SRT501The risk or severity of adverse effects can be increased when Omapatrilat is combined with SRT501.Investigational
St. John's WortThe metabolism of Omapatrilat can be increased when combined with St. John's Wort.Nutraceutical
SulfasalazineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Sulfasalazine.Approved
SulindacThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Sulindac.Approved
SuprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Suprofen.Approved, Withdrawn
Synthetic Conjugated Estrogens, AThe serum concentration of Synthetic Conjugated Estrogens, A can be decreased when it is combined with Omapatrilat.Approved
TacrolimusThe metabolism of Tacrolimus can be decreased when combined with Omapatrilat.Approved, Investigational
TadalafilTadalafil may increase the antihypertensive activities of Omapatrilat.Approved, Investigational
TasosartanThe risk or severity of adverse effects can be increased when Tasosartan is combined with Omapatrilat.Approved
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Omapatrilat.Approved, Investigational
TemocaprilOmapatrilat may increase the hypotensive activities of Temocapril.Experimental, Investigational
TemsirolimusThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Temsirolimus.Approved
TenoxicamThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Tenoxicam.Approved
TepoxalinThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Tepoxalin.Vet Approved
TeriflunomideThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Teriflunomide.Approved
TerlipressinOmapatrilat may increase the hypotensive activities of Terlipressin.Approved, Investigational
TheophyllineThe serum concentration of Theophylline can be decreased when it is combined with Omapatrilat.Approved
TianeptineThe serum concentration of Tianeptine can be increased when it is combined with Omapatrilat.Approved
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Tiaprofenic acid.Approved
TiboloneOmapatrilat may increase the hypotensive activities of Tibolone.Approved
TicrynafenOmapatrilat may increase the hypotensive activities of Ticrynafen.Withdrawn
TimololTimolol may increase the hypotensive activities of Omapatrilat.Approved
TinoridineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Tinoridine.Investigational
TinzaparinTinzaparin may increase the hyperkalemic activities of Omapatrilat.Approved
TipranavirThe serum concentration of Omapatrilat can be decreased when it is combined with Tipranavir.Approved, Investigational
TizanidineTizanidine may increase the hypotensive activities of Omapatrilat.Approved
TolazolineTolazoline may increase the hypotensive activities of Omapatrilat.Approved, Vet Approved
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Tolfenamic Acid.Approved
TolmetinThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Tolmetin.Approved
ToloxatoneToloxatone may increase the hypotensive activities of Omapatrilat.Approved
TolvaptanTolvaptan may increase the hyperkalemic activities of Omapatrilat.Approved
TorasemideTorasemide may increase the hypotensive activities of Omapatrilat.Approved
TrandolaprilTrandolapril may increase the hypotensive activities of Omapatrilat.Approved
TranilastThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Tranilast.Approved, Investigational
Trans-2-PhenylcyclopropylamineTrans-2-Phenylcyclopropylamine may increase the hypotensive activities of Omapatrilat.Experimental
TranylcypromineTranylcypromine may increase the hypotensive activities of Omapatrilat.Approved
TravoprostTravoprost may increase the hypotensive activities of Omapatrilat.Approved
TreprostinilTreprostinil may increase the hypotensive activities of Omapatrilat.Approved, Investigational
TriamtereneTriamterene may increase the hyperkalemic activities of Omapatrilat.Approved
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Omapatrilat.Approved
TrichlormethiazideOmapatrilat may increase the hypotensive activities of Trichlormethiazide.Approved, Vet Approved
TrimazosinOmapatrilat may increase the hypotensive activities of Trimazosin.Experimental
TrimethaphanOmapatrilat may increase the hypotensive activities of Trimethaphan.Approved
TrimethoprimTrimethoprim may increase the hyperkalemic activities of Omapatrilat.Approved, Vet Approved
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Omapatrilat.Approved
Trisalicylate-cholineThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Trisalicylate-choline.Approved
UdenafilUdenafil may increase the antihypertensive activities of Omapatrilat.Approved, Investigational
UnoprostoneOmapatrilat may increase the hypotensive activities of Unoprostone.Approved
ValdecoxibThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Valdecoxib.Investigational, Withdrawn
Valproic AcidThe serum concentration of Valproic Acid can be decreased when it is combined with Omapatrilat.Approved, Investigational
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Omapatrilat.Approved, Investigational
VardenafilVardenafil may increase the antihypertensive activities of Omapatrilat.Approved
VerapamilThe metabolism of Verapamil can be decreased when combined with Omapatrilat.Approved
VildagliptinThe risk or severity of adverse effects can be increased when Vildagliptin is combined with Omapatrilat.Approved, Investigational
VinpocetineOmapatrilat may increase the hypotensive activities of Vinpocetine.Investigational
XylometazolineOmapatrilat may increase the hypotensive activities of Xylometazoline.Approved
YohimbineYohimbine may decrease the antihypertensive activities of Omapatrilat.Approved, Vet Approved
ZaltoprofenThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Zaltoprofen.Approved
ZidovudineThe serum concentration of Zidovudine can be decreased when it is combined with Omapatrilat.Approved
ZileutonThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Zileuton.Approved, Investigational, Withdrawn
ZomepiracThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Zomepirac.Withdrawn
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
General References
  1. Rabkin SW, Klassen SS: Omapatrilat enhances adrenomedullin's reduction of cardiomyocyte cell death. Eur J Pharmacol. 2007 May 21;562(3):174-82. Epub 2007 Feb 8. [PubMed:17343842 ]
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB Entries
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.9567
Blood Brain Barrier-0.9219
Caco-2 permeable-0.7793
P-glycoprotein substrateSubstrate0.7377
P-glycoprotein inhibitor INon-inhibitor0.7782
P-glycoprotein inhibitor IINon-inhibitor0.9778
Renal organic cation transporterNon-inhibitor0.8896
CYP450 2C9 substrateNon-substrate0.7898
CYP450 2D6 substrateNon-substrate0.9117
CYP450 3A4 substrateNon-substrate0.5745
CYP450 1A2 substrateNon-inhibitor0.8791
CYP450 2C9 inhibitorNon-inhibitor0.8218
CYP450 2D6 inhibitorNon-inhibitor0.8781
CYP450 2C19 inhibitorNon-inhibitor0.7666
CYP450 3A4 inhibitorInhibitor0.5854
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.93
Ames testNon AMES toxic0.8423
CarcinogenicityNon-carcinogens0.9497
BiodegradationNot ready biodegradable0.9922
Rat acute toxicity2.0641 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9918
hERG inhibition (predictor II)Non-inhibitor0.624
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage formsNot Available
PricesNot Available
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP2.6Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0769 mg/mLALOGPS
logP2.15ALOGPS
logP2.06ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)3.77ChemAxon
pKa (Strongest Basic)-3.6ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count3ChemAxon
Polar Surface Area86.71 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity106.68 m3·mol-1ChemAxon
Polarizability41.8 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as dipeptides. These are organic compounds containing a sequence of exactly two alpha-amino acids joined by a peptide bond.
KingdomOrganic compounds
Super ClassOrganic acids and derivatives
ClassCarboxylic acids and derivatives
Sub ClassAmino acids, peptides, and analogues
Direct ParentDipeptides
Alternative Parents
Substituents
  • Alpha-dipeptide
  • N-acyl-alpha amino acid or derivatives
  • Alpha-amino acid or derivatives
  • Piperidinecarboxylic acid
  • Monocyclic benzene moiety
  • Fatty amide
  • Piperidine
  • Benzenoid
  • Fatty acyl
  • Tertiary carboxylic acid amide
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Lactam
  • Alkylthiol
  • Hemithioaminal
  • Thioether
  • Azacycle
  • Organoheterocyclic compound
  • Dialkylthioether
  • Carboxylic acid
  • Monocarboxylic acid or derivatives
  • Hydrocarbon derivative
  • Organic oxygen compound
  • Organic nitrogen compound
  • Organonitrogen compound
  • Organooxygen compound
  • Organosulfur compound
  • Organic oxide
  • Carbonyl group
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Zinc ion binding
Specific Function:
Converts angiotensin I to angiotensin II by release of the terminal His-Leu, this results in an increase of the vasoconstrictor activity of angiotensin. Also able to inactivate bradykinin, a potent vasodilator. Has also a glycosidase activity which releases GPI-anchored proteins from the membrane by cleaving the mannose linkage in the GPI moiety.
Gene Name:
ACE
Uniprot ID:
P12821
Molecular Weight:
149713.675 Da
References
  1. Azizi M, Massien C, Michaud A, Corvol P: In vitro and in vivo inhibition of the 2 active sites of ACE by omapatrilat, a vasopeptidase inhibitor. Hypertension. 2000 Jun;35(6):1226-31. [PubMed:10856268 ]
  2. Ferdinand KC: Advances in antihypertensive combination therapy: benefits of low-dose thiazide diuretics in conjunction with omapatrilat, a vasopeptidase inhibitor. J Clin Hypertens (Greenwich). 2001 Sep-Oct;3(5):307-12. [PubMed:11588409 ]
  3. Heudi O, Ramirez-Molina C, Marshall P, Amour A, Peace S, McKeown S, Abou-Shakra F: Investigation of bradykinin metabolism in human and rat plasma in the presence of the dual ACE/NEP inhibitors GW660511X and omapatrilat. J Pept Sci. 2002 Nov;8(11):591-600. [PubMed:12487427 ]
  4. Neal B, MacMahon S, Ohkubo T, Brnabic A, Tonkin A: Effects of the vasopeptidase inhibitor, omapatrilat, in 723 patients with coronary heart disease. J Renin Angiotensin Aldosterone Syst. 2002 Dec;3(4):270-6. [PubMed:12584671 ]
  5. Trippodo NC, Fox M, Monticello TM, Panchal BC, Asaad MM: Vasopeptidase inhibition with omapatrilat improves cardiac geometry and survival in cardiomyopathic hamsters more than does ACE inhibition with captopril. J Cardiovasc Pharmacol. 1999 Dec;34(6):782-90. [PubMed:10598120 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
General Function:
Zinc ion binding
Specific Function:
Thermolysin-like specificity, but is almost confined on acting on polypeptides of up to 30 amino acids (PubMed:15283675, PubMed:8168535). Biologically important in the destruction of opioid peptides such as Met- and Leu-enkephalins by cleavage of a Gly-Phe bond (PubMed:17101991). Able to cleave angiotensin-1, angiotensin-2 and angiotensin 1-9 (PubMed:15283675). Involved in the degradation of at...
Gene Name:
MME
Uniprot ID:
P08473
Molecular Weight:
85513.225 Da
References
  1. Intengan HD, Schiffrin EL: Vasopeptidase inhibition has potent effects on blood pressure and resistance arteries in stroke-prone spontaneously hypertensive rats. Hypertension. 2000 Jun;35(6):1221-5. [PubMed:10856267 ]
  2. Azizi M, Massien C, Michaud A, Corvol P: In vitro and in vivo inhibition of the 2 active sites of ACE by omapatrilat, a vasopeptidase inhibitor. Hypertension. 2000 Jun;35(6):1226-31. [PubMed:10856268 ]
  3. McClean DR, Ikram H, Garlick AH, Richards AM, Nicholls MG, Crozier IG: The clinical, cardiac, renal, arterial and neurohormonal effects of omapatrilat, a vasopeptidase inhibitor, in patients with chronic heart failure. J Am Coll Cardiol. 2000 Aug;36(2):479-86. [PubMed:10933361 ]
  4. Troughton RW, Rademaker MT, Powell JD, Yandle TG, Espiner EA, Frampton CM, Nicholls MG, Richards AM: Beneficial renal and hemodynamic effects of omapatrilat in mild and severe heart failure. Hypertension. 2000 Oct;36(4):523-30. [PubMed:11040230 ]
  5. Burrell LM, Droogh J, Man in't Veld O, Rockell MD, Farina NK, Johnston CI: Antihypertensive and antihypertrophic effects of omapatrilat in SHR. Am J Hypertens. 2000 Oct;13(10):1110-6. [PubMed:11041166 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23