This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Name
Relcovaptan
Accession Number
DB13929
Type
Small Molecule
Groups
Investigational
Description
Not Available
Structure
Thumb
Synonyms
Not Available
External IDs
SR 49059 / SR-49059 / SR49059 / TDI-0134
Categories
UNII
C1GL8G6G0O
CAS number
150375-75-0
Weight
Average: 620.5
Monoisotopic: 619.0946768
Chemical Formula
C28H27Cl2N3O7S
InChI Key
CEBYCSRFKCEUSW-NAYZPBBASA-N
InChI
InChI=1S/C28H27Cl2N3O7S/c1-39-23-12-10-17(15-24(23)40-2)41(37,38)33-21-11-9-16(29)14-19(21)28(36,18-6-3-4-7-20(18)30)25(33)27(35)32-13-5-8-22(32)26(31)34/h3-4,6-7,9-12,14-15,22,25,36H,5,8,13H2,1-2H3,(H2,31,34)/t22-,25-,28+/m0/s1
IUPAC Name
(2S)-1-[(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxybenzenesulfonyl)-3-hydroxy-2,3-dihydro-1H-indole-2-carbonyl]pyrrolidine-2-carboxamide
SMILES
COC1=CC=C(C=C1OC)S(=O)(=O)N1[[email protected]@H](C(=O)N2CCC[[email protected]]2C(N)=O)[[email protected]](O)(C2=CC(Cl)=CC=C12)C1=CC=CC=C1Cl

Pharmacology

Indication
Not Available
Structured Indications
Not Available
Pharmacodynamics
Not Available
Mechanism of action
TargetActionsOrganism
UOxytocin receptor
antagonist
Human
UVasopressin V1a receptor
antagonist
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabRelcovaptan may increase the anticoagulant activities of Abciximab.Approved
AcenocoumarolRelcovaptan may increase the anticoagulant activities of Acenocoumarol.Approved, Investigational
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Acetylsalicylic acid.Approved, Vet Approved
AloxiprinThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Aloxiprin.Experimental
AlprostadilAlprostadil may increase the antiplatelet activities of Relcovaptan.Approved, Investigational
AlteplaseRelcovaptan may increase the anticoagulant activities of Alteplase.Approved
Aminosalicylic AcidThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Aminosalicylic Acid.Approved
AnagrelideRelcovaptan may increase the anticoagulant activities of Anagrelide.Approved
AncrodRelcovaptan may increase the anticoagulant activities of Ancrod.Approved, Investigational
AndrographolideAndrographolide may increase the antiplatelet activities of Relcovaptan.Investigational
AnistreplaseRelcovaptan may increase the anticoagulant activities of Anistreplase.Approved
Antithrombin III humanRelcovaptan may increase the anticoagulant activities of Antithrombin III human.Approved
ApixabanThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Apixaban.Approved
ArdeparinRelcovaptan may increase the anticoagulant activities of Ardeparin.Approved, Investigational, Withdrawn
ArgatrobanRelcovaptan may increase the anticoagulant activities of Argatroban.Approved, Investigational
AstaxanthinRelcovaptan may increase the anticoagulant activities of Astaxanthin.Investigational
AzelastineAzelastine may increase the antiplatelet activities of Relcovaptan.Approved
BalsalazideThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Balsalazide.Approved, Investigational
BatroxobinRelcovaptan may increase the anticoagulant activities of Batroxobin.Experimental
BecaplerminRelcovaptan may increase the anticoagulant activities of Becaplermin.Approved, Investigational
BemiparinRelcovaptan may increase the anticoagulant activities of Bemiparin.Approved, Investigational
BeraprostRelcovaptan may increase the anticoagulant activities of Beraprost.Investigational
BivalirudinRelcovaptan may increase the anticoagulant activities of Bivalirudin.Approved, Investigational
BrinaseRelcovaptan may increase the anticoagulant activities of Brinase.Experimental
BuflomedilBuflomedil may increase the antiplatelet activities of Relcovaptan.Experimental
ButylphthalideButylphthalide may increase the antiplatelet activities of Relcovaptan.Investigational
CangrelorRelcovaptan may increase the anticoagulant activities of Cangrelor.Approved
CaplacizumabRelcovaptan may increase the anticoagulant activities of Caplacizumab.Investigational
Carbaspirin calciumThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Carbaspirin calcium.Experimental, Investigational
CertoparinRelcovaptan may increase the anticoagulant activities of Certoparin.Approved, Investigational
CilostazolRelcovaptan may increase the anticoagulant activities of Cilostazol.Approved, Investigational
Citric AcidRelcovaptan may increase the anticoagulant activities of Citric Acid.Approved, Nutraceutical, Vet Approved
ClopidogrelRelcovaptan may increase the anticoagulant activities of Clopidogrel.Approved
CloricromenRelcovaptan may increase the anticoagulant activities of Cloricromen.Experimental
ClorindioneRelcovaptan may increase the anticoagulant activities of Clorindione.Experimental
Collagenase clostridium histolyticumThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Collagenase clostridium histolyticum.Approved, Investigational
Dabigatran etexilateRelcovaptan may increase the anticoagulant activities of Dabigatran etexilate.Approved
DalteparinRelcovaptan may increase the anticoagulant activities of Dalteparin.Approved
DanaparoidRelcovaptan may increase the anticoagulant activities of Danaparoid.Approved, Withdrawn
DarexabanRelcovaptan may increase the anticoagulant activities of Darexaban.Investigational
DasatinibDasatinib may increase the anticoagulant activities of Relcovaptan.Approved, Investigational
DefibrotideRelcovaptan may increase the anticoagulant activities of Defibrotide.Approved, Investigational
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Deoxycholic Acid.Approved
DersalazineThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Dersalazine.Investigational
DesirudinRelcovaptan may increase the anticoagulant activities of Desirudin.Approved
DesmoteplaseRelcovaptan may increase the anticoagulant activities of Desmoteplase.Investigational
DextranRelcovaptan may increase the anticoagulant activities of Dextran.Approved, Investigational, Vet Approved
DicoumarolRelcovaptan may increase the anticoagulant activities of Dicoumarol.Approved
DiflunisalThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Diflunisal.Approved, Investigational
DiphenadioneRelcovaptan may increase the anticoagulant activities of Diphenadione.Experimental
DipyridamoleRelcovaptan may increase the anticoagulant activities of Dipyridamole.Approved
DitazoleRelcovaptan may increase the anticoagulant activities of Ditazole.Approved, Withdrawn
Drotrecogin alfaRelcovaptan may increase the anticoagulant activities of Drotrecogin alfa.Approved, Investigational, Withdrawn
Edetic AcidRelcovaptan may increase the anticoagulant activities of Edetic Acid.Approved, Vet Approved
EdoxabanRelcovaptan may increase the anticoagulant activities of Edoxaban.Approved
EnoxaparinRelcovaptan may increase the anticoagulant activities of Enoxaparin.Approved
EpinastineEpinastine may increase the antiplatelet activities of Relcovaptan.Approved, Investigational
EplivanserinRelcovaptan may increase the anticoagulant activities of Eplivanserin.Investigational
eplivanserineRelcovaptan may increase the anticoagulant activities of eplivanserine.Investigational
EpoprostenolRelcovaptan may increase the anticoagulant activities of Epoprostenol.Approved
EptifibatideRelcovaptan may increase the anticoagulant activities of Eptifibatide.Approved, Investigational
Ethyl biscoumacetateRelcovaptan may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
Ferulic acidRelcovaptan may increase the anticoagulant activities of Ferulic acid.Experimental
FibrinolysinRelcovaptan may increase the anticoagulant activities of Fibrinolysin.Investigational
FluindioneRelcovaptan may increase the anticoagulant activities of Fluindione.Approved, Investigational
FondaparinuxRelcovaptan may increase the anticoagulant activities of Fondaparinux.Approved, Investigational
Fondaparinux sodiumRelcovaptan may increase the anticoagulant activities of Fondaparinux sodium.Approved, Investigational
GabexateRelcovaptan may increase the anticoagulant activities of Gabexate.Investigational
GlucosamineGlucosamine may increase the antiplatelet activities of Relcovaptan.Approved, Investigational
GuacetisalThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Guacetisal.Experimental
Hemoglobin crosfumarilThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Hemoglobin crosfumaril.Experimental
HeparinRelcovaptan may increase the anticoagulant activities of Heparin.Approved, Investigational
HigenamineRelcovaptan may increase the anticoagulant activities of Higenamine.Investigational
HydroxytyrosolHydroxytyrosol may increase the antiplatelet activities of Relcovaptan.Investigational
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Ibritumomab tiuxetan.Approved, Investigational
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Relcovaptan.Approved
IbudilastIbudilast may increase the antiplatelet activities of Relcovaptan.Approved, Investigational
Icosapent ethylIcosapent ethyl may increase the antiplatelet activities of Relcovaptan.Approved, Investigational, Nutraceutical
IdraparinuxRelcovaptan may increase the anticoagulant activities of Idraparinux.Investigational
IfenprodilIfenprodil may increase the antiplatelet activities of Relcovaptan.Approved, Investigational, Withdrawn
IfetrobanIfetroban may increase the antiplatelet activities of Relcovaptan.Investigational
IloprostRelcovaptan may increase the anticoagulant activities of Iloprost.Approved, Investigational
IndobufenRelcovaptan may increase the anticoagulant activities of Indobufen.Investigational
KetanserinKetanserin may increase the antiplatelet activities of Relcovaptan.Investigational
LepirudinRelcovaptan may increase the anticoagulant activities of Lepirudin.Approved
LetaxabanRelcovaptan may increase the anticoagulant activities of Letaxaban.Investigational
LimaprostLimaprost may increase the antiplatelet activities of Relcovaptan.Approved, Investigational
LinsidomineLinsidomine may increase the antiplatelet activities of Relcovaptan.Experimental
MelagatranRelcovaptan may increase the anticoagulant activities of Melagatran.Experimental
MesalazineThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Mesalazine.Approved
Methyl salicylateThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Methyl salicylate.Approved, Vet Approved
MilrinoneMilrinone may increase the antiplatelet activities of Relcovaptan.Approved
NadroparinRelcovaptan may increase the anticoagulant activities of Nadroparin.Approved, Investigational
NafamostatRelcovaptan may increase the anticoagulant activities of Nafamostat.Approved, Investigational
NaftopidilNaftopidil may increase the antiplatelet activities of Relcovaptan.Investigational
NimesulideNimesulide may increase the antiplatelet activities of Relcovaptan.Approved, Investigational, Withdrawn
NitroaspirinThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Nitroaspirin.Investigational
ObinutuzumabThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Obinutuzumab.Approved, Investigational
OlsalazineThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Olsalazine.Approved
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Relcovaptan.Approved, Nutraceutical
OtamixabanRelcovaptan may increase the anticoagulant activities of Otamixaban.Investigational
OzagrelRelcovaptan may increase the anticoagulant activities of Ozagrel.Investigational
ParnaparinRelcovaptan may increase the anticoagulant activities of Parnaparin.Approved, Investigational
Pentaerythritol TetranitrateRelcovaptan may increase the anticoagulant activities of Pentaerythritol Tetranitrate.Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Relcovaptan.Approved
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Relcovaptan.Approved, Investigational
PhenindioneRelcovaptan may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonRelcovaptan may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
Phenyl aminosalicylateThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Phenyl aminosalicylate.Approved
PicotamideRelcovaptan may increase the anticoagulant activities of Picotamide.Experimental
PrasugrelRelcovaptan may increase the anticoagulant activities of Prasugrel.Approved
Protein CRelcovaptan may increase the anticoagulant activities of Protein C.Approved
Protein S humanRelcovaptan may increase the anticoagulant activities of Protein S human.Approved
ProtocatechualdehydeRelcovaptan may increase the anticoagulant activities of Protocatechualdehyde.Approved
RamatrobanRamatroban may increase the antiplatelet activities of Relcovaptan.Investigational
ResveratrolResveratrol may increase the antiplatelet activities of Relcovaptan.Approved, Experimental, Investigational
ReteplaseRelcovaptan may increase the anticoagulant activities of Reteplase.Approved, Investigational
ReviparinRelcovaptan may increase the anticoagulant activities of Reviparin.Approved, Investigational
RidogrelRidogrel may increase the antiplatelet activities of Relcovaptan.Approved
RivaroxabanRelcovaptan may increase the anticoagulant activities of Rivaroxaban.Approved
RosiglitazoneRelcovaptan may increase the anticoagulant activities of Rosiglitazone.Approved, Investigational
Salicylic acidThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Salicylic acid.Approved, Investigational, Vet Approved
SarpogrelateRelcovaptan may increase the anticoagulant activities of Sarpogrelate.Investigational
SaruplaseRelcovaptan may increase the anticoagulant activities of Saruplase.Experimental
SelexipagRelcovaptan may increase the anticoagulant activities of Selexipag.Approved
SevofluraneSevoflurane may increase the antiplatelet activities of Relcovaptan.Approved, Vet Approved
SRT501SRT501 may increase the antiplatelet activities of Relcovaptan.Investigational
StreptokinaseRelcovaptan may increase the anticoagulant activities of Streptokinase.Approved, Investigational
SulodexideRelcovaptan may increase the anticoagulant activities of Sulodexide.Approved, Investigational
TenecteplaseRelcovaptan may increase the anticoagulant activities of Tenecteplase.Approved
TesmilifeneTesmilifene may increase the antiplatelet activities of Relcovaptan.Investigational
TicagrelorRelcovaptan may increase the anticoagulant activities of Ticagrelor.Approved
TiclopidineRelcovaptan may increase the anticoagulant activities of Ticlopidine.Approved
TinzaparinRelcovaptan may increase the anticoagulant activities of Tinzaparin.Approved
TioclomarolRelcovaptan may increase the anticoagulant activities of Tioclomarol.Experimental
TipranavirTipranavir may increase the antiplatelet activities of Relcovaptan.Approved, Investigational
TirofibanRelcovaptan may increase the anticoagulant activities of Tirofiban.Approved
TositumomabThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Tositumomab.Approved, Investigational
TranilastTranilast may increase the antiplatelet activities of Relcovaptan.Approved, Investigational
TrapidilTrapidil may increase the antiplatelet activities of Relcovaptan.Approved
TreprostinilRelcovaptan may increase the anticoagulant activities of Treprostinil.Approved, Investigational
TriflusalRelcovaptan may increase the anticoagulant activities of Triflusal.Approved, Investigational
Trolamine salicylateThe risk or severity of adverse effects can be increased when Relcovaptan is combined with Trolamine salicylate.Approved
TroxerutinRelcovaptan may increase the anticoagulant activities of Troxerutin.Investigational
UrokinaseRelcovaptan may increase the anticoagulant activities of Urokinase.Approved, Investigational, Withdrawn
Vitamin EVitamin E may increase the antiplatelet activities of Relcovaptan.Approved, Nutraceutical, Vet Approved
VorapaxarRelcovaptan may increase the anticoagulant activities of Vorapaxar.Approved
WarfarinRelcovaptan may increase the anticoagulant activities of Warfarin.Approved
XimelagatranRelcovaptan may increase the anticoagulant activities of Ximelagatran.Approved, Investigational, Withdrawn
Food Interactions
Not Available

References

General References
  1. Ponzoni L, Braida D, Bondiolotti G, Sala M: The Non-Peptide Arginine-Vasopressin v1a Selective Receptor Antagonist, SR49059, Blocks the Rewarding, Prosocial, and Anxiolytic Effects of 3,4-Methylenedioxymethamphetamine and Its Derivatives in Zebra Fish. Front Psychiatry. 2017 Aug 14;8:146. doi: 10.3389/fpsyt.2017.00146. eCollection 2017. [PubMed:28855876]
External Links
ChemSpider
54910
BindingDB
50114031
ChEBI
93701
ChEMBL
CHEMBL419667
Wikipedia
Relcovaptan

Clinical Trials

Clinical Trials
Not Available

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00767 mg/mLALOGPS
logP3.74ALOGPS
logP2.83ChemAxon
logS-4.9ALOGPS
pKa (Strongest Acidic)7.72ChemAxon
pKa (Strongest Basic)-3.8ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area139.47 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity152.18 m3·mol-1ChemAxon
Polarizability59.59 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Taxonomy

Classification
Not classified

Targets

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Vasopressin receptor activity
Specific Function
Receptor for oxytocin. The activity of this receptor is mediated by G proteins which activate a phosphatidylinositol-calcium second messenger system.
Gene Name
OXTR
Uniprot ID
P30559
Uniprot Name
Oxytocin receptor
Molecular Weight
42770.99 Da
References
  1. Akerlund M, Bossmar T, Brouard R, Kostrzewska A, Laudanski T, Lemancewicz A, Serradeil-Le Gal C, Steinwall M: Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women. Br J Obstet Gynaecol. 1999 Oct;106(10):1047-53. [PubMed:10519430]
  2. Pierzynski P: Oxytocin and vasopressin V(1A) receptors as new therapeutic targets in assisted reproduction. Reprod Biomed Online. 2011 Jan;22(1):9-16. doi: 10.1016/j.rbmo.2010.09.015. Epub 2010 Oct 14. [PubMed:21130036]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Antagonist
General Function
Vasopressin receptor activity
Specific Function
Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl-inositol-calcium second messenger system. Has been involved in social behavi...
Gene Name
AVPR1A
Uniprot ID
P37288
Uniprot Name
Vasopressin V1a receptor
Molecular Weight
46799.105 Da
References
  1. Akerlund M, Bossmar T, Brouard R, Kostrzewska A, Laudanski T, Lemancewicz A, Serradeil-Le Gal C, Steinwall M: Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women. Br J Obstet Gynaecol. 1999 Oct;106(10):1047-53. [PubMed:10519430]
  2. Pierzynski P: Oxytocin and vasopressin V(1A) receptors as new therapeutic targets in assisted reproduction. Reprod Biomed Online. 2011 Jan;22(1):9-16. doi: 10.1016/j.rbmo.2010.09.015. Epub 2010 Oct 14. [PubMed:21130036]

Drug created on December 06, 2017 18:19 / Updated on May 02, 2018 00:41