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Identification
NameMilnacipran
Accession NumberDB04896
TypeSmall Molecule
GroupsApproved
Description

Milnacipran is an antidepressant of the serotonin-norepinephrine reuptake inhibitor class. It more potently inhibits norepinephrine uptake than serotonin. It is provided as a racemic mixture. FDA approved in January 2009.

Structure
Thumb
Synonyms
(-)-milnacipran
Midalcipran
Milnacipran
Milnacipranum
External Identifiers
  • F2207
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Savellatablet, film coated25 mg/1oralRebel Distributors Corp2009-04-17Not applicableUs
SavellakitoralForest Laboratories, Inc.2009-04-17Not applicableUs
Savellatablet, film coated50 mg/1oralCardinal Health2009-04-17Not applicableUs
Savellatablet, film coated100 mg/1oralSTAT Rx USA LLC2009-04-17Not applicableUs
Savellatablet, film coated50 mg/1oralPhysicians Total Care, Inc.2009-06-22Not applicableUs
Savellatablet, film coated50 mg/1oralSTAT Rx USA LLC2009-04-17Not applicableUs
Savellatablet, film coated100 mg/1oralPhysicians Total Care, Inc.2010-01-19Not applicableUs
Savellatablet, film coated25 mg/1oralSTAT Rx USA LLC2009-04-17Not applicableUs
Savellatablet, film coated25 mg/1oralUnit Dose Services2009-04-17Not applicableUs
Savellatablet, film coated50 mg/1oralForest Laboratories, Inc.2009-04-17Not applicableUs
Savellatablet, film coated25 mg/1oralLake Erie Medical DBA Quality Care Products LLC2009-04-17Not applicableUs
Savellatablet, film coated25 mg/1oralForest Laboratories, Inc.2009-04-17Not applicableUs
Savellatablet, film coated50 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2011-11-17Not applicableUs
Savellatablet, film coated12.5 mg/1oralForest Laboratories, Inc.2009-04-17Not applicableUs
Savellatablet, film coated50 mg/1oralRebel Distributors Corp2009-04-17Not applicableUs
Savellatablet, film coated100 mg/1oralForest Laboratories, Inc.2009-04-17Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Milnacipran Hydrochloridetablet, film coated12.5 mg/1oralRanbaxy Pharmaceuticals Inc.2014-11-27Not applicableUs
Milnacipran Hydrochloridetablet, film coated100 mg/1oralRanbaxy Pharmaceuticals Inc.2014-11-27Not applicableUs
Milnacipran Hydrochloridetablet, film coated50 mg/1oralRanbaxy Pharmaceuticals Inc.2014-11-27Not applicableUs
Milnacipran Hydrochloridetablet, film coated25 mg/1oralRanbaxy Pharmaceuticals Inc.2014-11-27Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
Dalcipran Not Available
IxelNot Available
ToledominNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Milnacipran Hydrochloride
Thumb
  • InChI Key: XNCDYJFPRPDERF-PBCQUBLHSA-N
  • Monoisotopic Mass: 282.149891075
  • Average Mass: 282.809
DBSALT000119
Categories
UNIIG56VK1HF36
CAS number92623-85-3
WeightAverage: 246.348
Monoisotopic: 246.173213336
Chemical FormulaC15H22N2O
InChI KeyInChIKey=GJJFMKBJSRMPLA-HIFRSBDPSA-N
InChI
InChI=1S/C15H22N2O/c1-3-17(4-2)14(18)15(10-13(15)11-16)12-8-6-5-7-9-12/h5-9,13H,3-4,10-11,16H2,1-2H3/t13-,15+/m1/s1
IUPAC Name
(1R,2S)-2-(aminomethyl)-N,N-diethyl-1-phenylcyclopropane-1-carboxamide
SMILES
CCN(CC)C(=O)[C@@]1(C[C@@H]1CN)C1=CC=CC=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as phenylacetamides. These are amide derivatives of phenylacetic acids.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenylacetamides
Direct ParentPhenylacetamides
Alternative Parents
Substituents
  • Phenylacetamide
  • Aralkylamine
  • Cyclopropanecarboxylic acid or derivatives
  • Tertiary carboxylic acid amide
  • Tertiary amine
  • Carboxamide group
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationMilnacipran is used to treat moderate to severe clinical depression but this indication is not yet FDA-approved in the USA. Milnacipran is labelled for the treatment of fibromyalgia pain.
PharmacodynamicsAlthough milnacipran prolongs the QTc interval, the increase is not considered clinically significant.
Mechanism of actionMilnacipran inhibits norepinephrine and serotonin reuptake in a 3:1 ratio, in practical use this means a balanced (equal) action upon both transmitters. The serotonin reuptake inhibition is likely to improve depression, while the norepinephrine reuptake inihibition probably improves chronic pain. Milnacipran exerts no significant actions on postynaptic H1, alpha-1, D1, D2, and muscarinic receptors, as well as on benzodiazepine/opiate binding sites. [Wikipedia]
Related Articles
AbsorptionMilnacipran is well absorbed following oral administration with an absolute bioavailability of 85-90%. Meals have no effect on absorption. Peak concentrations occur 2 -4 hours post-administration and is delayed in elderly patients. Time to steady state = 36 - 48 hours;
Volume of distribution

400 L, following a single IV dose to a healthy subject.

Protein bindingPlasma protein binding is 13%.
Metabolism

Hepatic metabolism of milnacipran occurs via glucuronidation. No involvement of CYP450 isozymes or active metabolites found.

Route of eliminationIt is excreted predominantly unchanged in urine (50%- 60%, 24% as l-milnacipran and 31% as d-milnacipran). The l-milnacipran carbamoyl-O-glucuronide was the major metabolite excreted in urine and accounted for approximately 17% of the dose; approximately 2% of the dose was excreted in urine as d-milnacipran carbamoyl-O-glucuronide. Approximately 8% of the dose was excreted in urine as the N-desethyl milnacipran metabolite.
Half lifeThe terminal elimination half-life, when given to healthy subjects is 6-8 hours. When given to severe renal impairment patients is 7 - 10 hours. The active enantiomer, d-milnacipran, has a longer elimination half-life (8-10 hours) than the l-enantiomer (4-6 hours).
ClearanceNot Available
ToxicityLD50, oral, rat: 213 mg/kg. The most frequently occurring adverse reactions (≥ 5% and greater than placebo) were nausea, headache, constipation, dizziness, insomnia, hot flush, hyperhidrosis, vomiting, palpitations, heart rate increased, dry mouth, and hypertension.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9889
Caco-2 permeable+0.5914
P-glycoprotein substrateSubstrate0.5928
P-glycoprotein inhibitor INon-inhibitor0.902
P-glycoprotein inhibitor IINon-inhibitor0.8787
Renal organic cation transporterNon-inhibitor0.8119
CYP450 2C9 substrateNon-substrate0.8494
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6514
CYP450 1A2 substrateNon-inhibitor0.6383
CYP450 2C9 inhibitorNon-inhibitor0.7697
CYP450 2D6 inhibitorNon-inhibitor0.7718
CYP450 2C19 inhibitorNon-inhibitor0.8587
CYP450 3A4 inhibitorNon-inhibitor0.6327
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7004
Ames testNon AMES toxic0.8013
CarcinogenicityNon-carcinogens0.5456
BiodegradationNot ready biodegradable0.9972
Rat acute toxicity2.6162 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.993
hERG inhibition (predictor II)Non-inhibitor0.6823
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Kitoral
Tablet, film coatedoral100 mg/1
Tablet, film coatedoral12.5 mg/1
Tablet, film coatedoral25 mg/1
Tablet, film coatedoral50 mg/1
Prices
Unit descriptionCostUnit
Savella 100 mg tablet2.13USD tablet
Savella 12.5 mg tablet2.13USD tablet
Savella 25 mg tablet2.13USD tablet
Savella 50 mg tablet2.13USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6602911 No2003-01-142023-01-14Us
US6992110 No2001-11-052021-11-05Us
US7888342 No2001-11-052021-11-05Us
US7994220 No2009-09-192029-09-19Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point179°C Bernstein CD, Albrecht KL, Marcus DA: Milnacipran for fibromyalgia: a useful addition to the treatment armamentarium. Expert Opin Pharmacother. 2013 Mar 19. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/23506481
water solubility19 mg/mLMSDS
Predicted Properties
PropertyValueSource
Water Solubility1.23 mg/mLALOGPS
logP1.72ALOGPS
logP1.42ChemAxon
logS-2.3ALOGPS
pKa (Strongest Basic)9.83ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area46.33 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity73.81 m3·mol-1ChemAxon
Polarizability28.03 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Jean Deregnaucourt, “Use of the (1S,2R) enantiomer of milnacipran for the preparation of a drug.” U.S. Patent US20040259953, issued December 23, 2004.

US20040259953
General References
  1. Leo RJ, Brooks VL: Clinical potential of milnacipran, a serotonin and norepinephrine reuptake inhibitor, in pain. Curr Opin Investig Drugs. 2006 Jul;7(7):637-42. [PubMed:16869117 ]
  2. Sato S, Yamakawa Y, Terashima Y, Ohta H, Asada T: Efficacy of milnacipran on cognitive dysfunction with post-stroke depression: preliminary open-label study. Psychiatry Clin Neurosci. 2006 Oct;60(5):584-9. [PubMed:16958942 ]
  3. Simon LS: Is milnacipran effective in treating pain in patients with fibromyalgia? Nat Clin Pract Rheumatol. 2006 Mar;2(3):126-7. [PubMed:16932669 ]
  4. Soya A, Terao T, Nakajima M, Kojima H, Okamoto T, Inoue Y, Iwakawa M, Shinkai K, Yoshimura R, Ueta Y, Nakamura J: Effects of repeated milnacipran administration on brain serotonergic and noradrenergic functions in healthy volunteers. Psychopharmacology (Berl). 2006 Sep;187(4):526-7. Epub 2006 Jul 8. [PubMed:16830129 ]
  5. King T, Rao S, Vanderah T, Chen Q, Vardanyan A, Porreca F: Differential blockade of nerve injury-induced shift in weight bearing and thermal and tactile hypersensitivity by milnacipran. J Pain. 2006 Jul;7(7):513-20. [PubMed:16814690 ]
  6. Moojen VK, Martins MR, Reinke A, Feier G, Agostinho FR, Cechin EM, Quevedo J: Effects of milnacipran in animal models of anxiety and memory. Neurochem Res. 2006 Apr;31(4):571-7. Epub 2006 May 9. [PubMed:16758367 ]
  7. Moret C, Charveron M, Finberg JP, Couzinier JP, Briley M: Biochemical profile of midalcipran (F 2207), 1-phenyl-1-diethyl-aminocarbonyl-2-aminomethyl-cyclopropane (Z) hydrochloride, a potential fourth generation antidepressant drug. Neuropharmacology. 1985 Dec;24(12):1211-9. [PubMed:3005901 ]
  8. Briley M, Prost JF, Moret C: Preclinical pharmacology of milnacipran. Int Clin Psychopharmacol. 1996 Sep;11 Suppl 4:9-14. [PubMed:8923122 ]
  9. Puozzo C, Panconi E, Deprez D: Pharmacology and pharmacokinetics of milnacipran. Int Clin Psychopharmacol. 2002 Jun;17 Suppl 1:S25-35. [PubMed:12369608 ]
  10. Leinonen E, Lepola U, Koponen H, Mehtonen OP, Rimon R: Long-term efficacy and safety of milnacipran compared to clomipramine in patients with major depression. Acta Psychiatr Scand. 1997 Dec;96(6):497-504. [PubMed:9421348 ]
  11. Papakostas GI, Fava M: A meta-analysis of clinical trials comparing milnacipran, a serotonin--norepinephrine reuptake inhibitor, with a selective serotonin reuptake inhibitor for the treatment of major depressive disorder. Eur Neuropsychopharmacol. 2007 Jan;17(1):32-6. Epub 2006 Jun 8. [PubMed:16762534 ]
  12. Kako Y, Niwa Y, Toyomaki A, Yamanaka H, Kitagawa N, Denda K, Koyama T: A case of adult attention-deficit/hyperactivity disorder alleviated by milnacipran. Prog Neuropsychopharmacol Biol Psychiatry. 2007 Apr 13;31(3):772-5. Epub 2007 Jan 12. [PubMed:17300859 ]
  13. Bernstein CD, Albrecht KL, Marcus DA: Milnacipran for fibromyalgia: a useful addition to the treatment armamentarium. Expert Opin Pharmacother. 2013 May;14(7):905-16. doi: 10.1517/14656566.2013.779670. Epub 2013 Mar 19. [PubMed:23506481 ]
External Links
ATC CodesN06AX17
AHFS Codes
  • 28:16.04.16
  • 28:40
PDB EntriesNot Available
FDA labelDownload (332 KB)
MSDSDownload (83.2 KB)
Interactions
Drug Interactions
Drug
AbciximabMilnacipran may increase the anticoagulant activities of Abciximab.
AcenocoumarolThe risk or severity of adverse effects can be increased when Milnacipran is combined with Acenocoumarol.
AcepromazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Acepromazine.
AcetophenazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Acetophenazine.
Acetylsalicylic acidMilnacipran may increase the antiplatelet activities of Acetylsalicylic acid.
AlteplaseMilnacipran may increase the anticoagulant activities of Alteplase.
AmisulprideThe risk or severity of adverse effects can be increased when Milnacipran is combined with Amisulpride.
AnistreplaseMilnacipran may increase the anticoagulant activities of Anistreplase.
ApixabanThe risk or severity of adverse effects can be increased when Milnacipran is combined with Apixaban.
AripiprazoleThe risk or severity of adverse effects can be increased when Milnacipran is combined with Aripiprazole.
BenzquinamideThe risk or severity of adverse effects can be increased when Milnacipran is combined with Benzquinamide.
CarphenazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Carphenazine.
ChlormezanoneThe risk or severity of adverse effects can be increased when Milnacipran is combined with Chlormezanone.
ChlorpromazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Chlorpromazine.
ChlorprothixeneThe risk or severity of adverse effects can be increased when Milnacipran is combined with Chlorprothixene.
Citric AcidMilnacipran may increase the anticoagulant activities of Citric Acid.
ClomipramineThe risk or severity of adverse effects can be increased when Clomipramine is combined with Milnacipran.
ClozapineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Clozapine.
CollagenaseThe risk or severity of adverse effects can be increased when Milnacipran is combined with Collagenase.
Dabigatran etexilateMilnacipran may increase the anticoagulant activities of Dabigatran etexilate.
DalteparinMilnacipran may increase the anticoagulant activities of Dalteparin.
DapoxetineThe risk or severity of adverse effects can be increased when Dapoxetine is combined with Milnacipran.
DasatinibDasatinib may increase the anticoagulant activities of Milnacipran.
Deoxycholic AcidThe risk or severity of adverse effects can be increased when Milnacipran is combined with Deoxycholic Acid.
DesmopressinMilnacipran may increase the antiplatelet activities of Desmopressin.
DicoumarolThe risk or severity of adverse effects can be increased when Milnacipran is combined with Dicoumarol.
DigoxinThe risk or severity of adverse effects can be increased when Milnacipran is combined with Digoxin.
DipivefrinMilnacipran may decrease the antihypertensive activities of Dipivefrin.
DroperidolThe risk or severity of adverse effects can be increased when Milnacipran is combined with Droperidol.
Edetic AcidMilnacipran may increase the anticoagulant activities of Edetic Acid.
EnoxaparinMilnacipran may increase the anticoagulant activities of Enoxaparin.
EthanolThe risk or severity of adverse effects can be increased when Ethanol is combined with Milnacipran.
Ethyl biscoumacetateMilnacipran may increase the anticoagulant activities of Ethyl biscoumacetate.
FencamfamineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Fencamfamine.
FlupentixolThe risk or severity of adverse effects can be increased when Milnacipran is combined with Flupentixol.
FluphenazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Fluphenazine.
FluspirileneThe risk or severity of adverse effects can be increased when Milnacipran is combined with Fluspirilene.
FluvoxamineThe risk or severity of adverse effects can be increased when Fluvoxamine is combined with Milnacipran.
Fondaparinux sodiumMilnacipran may increase the anticoagulant activities of Fondaparinux sodium.
GlucosamineGlucosamine may increase the antiplatelet activities of Milnacipran.
GranisetronGranisetron may increase the serotonergic activities of Milnacipran.
HaloperidolThe risk or severity of adverse effects can be increased when Milnacipran is combined with Haloperidol.
HeparinMilnacipran may increase the anticoagulant activities of Heparin.
Ibritumomab tiuxetanThe risk or severity of adverse effects can be increased when Milnacipran is combined with Ibritumomab.
IbrutinibThe risk or severity of adverse effects can be increased when Ibrutinib is combined with Milnacipran.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Milnacipran.
Ioflupane I 123Milnacipran may decrease effectiveness of Ioflupane I 123 as a diagnostic agent.
LimaprostLimaprost may increase the antiplatelet activities of Milnacipran.
LinezolidLinezolid may increase the serotonergic activities of Milnacipran.
LoxapineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Loxapine.
MesoridazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Mesoridazine.
MethotrimeprazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Methotrimeprazine.
Methylene blueMilnacipran may increase the serotonergic activities of Methylene blue.
MetoclopramideThe risk or severity of adverse effects can be increased when Metoclopramide is combined with Milnacipran.
MolindoneThe risk or severity of adverse effects can be increased when Milnacipran is combined with Molindone.
ObinutuzumabThe risk or severity of adverse effects can be increased when Milnacipran is combined with Obinutuzumab.
OlanzapineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Olanzapine.
Omega-3 fatty acidsOmega-3 fatty acids may increase the antiplatelet activities of Milnacipran.
OndansetronThe risk or severity of adverse effects can be increased when Milnacipran is combined with Ondansetron.
PaliperidoneThe risk or severity of adverse effects can be increased when Milnacipran is combined with Paliperidone.
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Milnacipran.
PentoxifyllinePentoxifylline may increase the antiplatelet activities of Milnacipran.
PerphenazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Perphenazine.
PhenelzinePhenelzine may increase the serotonergic activities of Milnacipran.
PhenindioneMilnacipran may increase the anticoagulant activities of Phenindione.
PhenprocoumonMilnacipran may increase the anticoagulant activities of Phenprocoumon.
PimozideThe risk or severity of adverse effects can be increased when Milnacipran is combined with Pimozide.
PiperacetazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Piperacetazine.
ProchlorperazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Prochlorperazine.
PromazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Promazine.
QuetiapineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Quetiapine.
RemoxiprideThe risk or severity of adverse effects can be increased when Milnacipran is combined with Remoxipride.
ReserpineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Reserpine.
ReteplaseMilnacipran may increase the anticoagulant activities of Reteplase.
RidogrelMilnacipran may increase the anticoagulant activities of Ridogrel.
RisperidoneThe risk or severity of adverse effects can be increased when Milnacipran is combined with Risperidone.
RivaroxabanMilnacipran may increase the anticoagulant activities of Rivaroxaban.
SertindoleThe risk or severity of adverse effects can be increased when Milnacipran is combined with Sertindole.
StreptokinaseMilnacipran may increase the anticoagulant activities of Streptokinase.
SulodexideMilnacipran may increase the anticoagulant activities of Sulodexide.
SulpirideThe risk or severity of adverse effects can be increased when Milnacipran is combined with Sulpiride.
Tedizolid PhosphateTedizolid Phosphate may increase the serotonergic activities of Milnacipran.
TenecteplaseMilnacipran may increase the anticoagulant activities of Tenecteplase.
ThioridazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Thioridazine.
ThiothixeneThe risk or severity of adverse effects can be increased when Milnacipran is combined with Thiothixene.
TipranavirTipranavir may increase the antiplatelet activities of Milnacipran.
TositumomabThe risk or severity of adverse effects can be increased when Milnacipran is combined with Tositumomab.
TramadolThe risk or severity of adverse effects can be increased when Tramadol is combined with Milnacipran.
TranylcypromineTranylcypromine may increase the serotonergic activities of Milnacipran.
TreprostinilMilnacipran may increase the anticoagulant activities of Treprostinil.
TrifluoperazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Trifluoperazine.
TriflupromazineThe risk or severity of adverse effects can be increased when Milnacipran is combined with Triflupromazine.
UrokinaseMilnacipran may increase the anticoagulant activities of Urokinase.
Vitamin EVitamin E may increase the antiplatelet activities of Milnacipran.
WarfarinThe risk or severity of adverse effects can be increased when Milnacipran is combined with Warfarin.
ZiprasidoneThe risk or severity of adverse effects can be increased when Milnacipran is combined with Ziprasidone.
ZuclopenthixolThe risk or severity of adverse effects can be increased when Milnacipran is combined with Zuclopenthixol.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Serotonin:sodium symporter activity
Specific Function:
Serotonin transporter whose primary function in the central nervous system involves the regulation of serotonergic signaling via transport of serotonin molecules from the synaptic cleft back into the pre-synaptic terminal for re-utilization. Plays a key role in mediating regulation of the availability of serotonin to other receptors of serotonergic systems. Terminates the action of serotonin an...
Gene Name:
SLC6A4
Uniprot ID:
P31645
Molecular Weight:
70324.165 Da
References
  1. Leo RJ, Brooks VL: Clinical potential of milnacipran, a serotonin and norepinephrine reuptake inhibitor, in pain. Curr Opin Investig Drugs. 2006 Jul;7(7):637-42. [PubMed:16869117 ]
  2. Moret C, Charveron M, Finberg JP, Couzinier JP, Briley M: Biochemical profile of midalcipran (F 2207), 1-phenyl-1-diethyl-aminocarbonyl-2-aminomethyl-cyclopropane (Z) hydrochloride, a potential fourth generation antidepressant drug. Neuropharmacology. 1985 Dec;24(12):1211-9. [PubMed:3005901 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Norepinephrine:sodium symporter activity
Specific Function:
Amine transporter. Terminates the action of noradrenaline by its high affinity sodium-dependent reuptake into presynaptic terminals.
Gene Name:
SLC6A2
Uniprot ID:
P23975
Molecular Weight:
69331.42 Da
References
  1. Leo RJ, Brooks VL: Clinical potential of milnacipran, a serotonin and norepinephrine reuptake inhibitor, in pain. Curr Opin Investig Drugs. 2006 Jul;7(7):637-42. [PubMed:16869117 ]
  2. Moret C, Charveron M, Finberg JP, Couzinier JP, Briley M: Biochemical profile of midalcipran (F 2207), 1-phenyl-1-diethyl-aminocarbonyl-2-aminomethyl-cyclopropane (Z) hydrochloride, a potential fourth generation antidepressant drug. Neuropharmacology. 1985 Dec;24(12):1211-9. [PubMed:3005901 ]
Kind
Protein group
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Voltage-gated cation channel activity
Specific Function:
NMDA receptor subtype of glutamate-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Mediated by glycine. This protein plays a key role in synaptic plasticity, synaptogenesis, excitotoxicity, memory acquisition and learning. It mediates neuronal functions in glutamate neurotransmission. Is involved in the cell surface targeting of NMDA receptors (By similarity).
Components:
NameUniProt IDDetails
Glutamate receptor ionotropic, NMDA 1Q05586 Details
Glutamate receptor ionotropic, NMDA 2AQ12879 Details
Glutamate receptor ionotropic, NMDA 2BQ13224 Details
Glutamate receptor ionotropic, NMDA 2CQ14957 Details
Glutamate receptor ionotropic, NMDA 2DO15399 Details
Glutamate receptor ionotropic, NMDA 3AQ8TCU5 Details
Glutamate receptor ionotropic, NMDA 3BO60391 Details
References
  1. Kohno T, Kimura M, Sasaki M, Obata H, Amaya F, Saito S: Milnacipran inhibits glutamatergic N-methyl-D-aspartate receptor activity in spinal dorsal horn neurons. Mol Pain. 2012 Jun 19;8:45. doi: 10.1186/1744-8069-8-45. [PubMed:22716121 ]
  2. Shuto S, Takada H, Mochizuki D, Tsujita R, Hase Y, Ono S, Shibuya N, Matsuda A: (+/-)-(Z)-2-(aminomethyl)-1-phenylcyclopropanecarboxamide derivatives as a new prototype of NMDA receptor antagonists. J Med Chem. 1995 Jul 21;38(15):2964-8. [PubMed:7636857 ]
Comments
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Drug created on October 21, 2007 16:23 / Updated on June 25, 2016 01:51