DGIdb - COCAINE Drug Record

COCAINE chembl:CHEMBL370805 Approved

Alternate Names:

RX-0041
RX0041
COCAINE
IDS-NC-004
BETA-COCAIN
KOKAIN
(-)-COCAINE
METHYL [1R-(EXO,EXO)]-3-(BENZOYLOXY)-8-METHYL-8-AZABICYCLO[3.2.1]OCTANE-2-CARBOXYLATE
COCAINUM
L-COCAIN
METHYL BENZOYLECGONINE
BENZOYLMETHYLECGONINE
2-METHYL-3BETA-HYDROXY-1ALPHAH,5ALPHAH-TROPANE-2BETA-CARBOXYLATE BENZOATE (ESTER)
[1R-(EXO,EXO)]-3-(BENZOYLOXY)-8-METHYL-8-AZABICYCLO[3.2.1]OCTANE-2-CARBOXYLIC ACID, METHYL ESTER
NEUROCAINE
L-COCAINE
COCAINA
(−)-COCAINE
COCAIN
chembl:CHEMBL370805
drugbank:00907
rxcui:2653
pubchem.compound:446220
chemidplus:50-36-2

Drug Info:

FDA Approval	Approved before 1982
Drug Class	small molecule
Drug Indications	local anesthetic
Year of Approval	approved before 1982
Drug Class	anesthetics, local

(1 More Sources)

Publications:

Patkar et al., 2002, Serotonin transporter polymorphisms and measures of impulsivity, aggression, and sensation seeking among African-American cocaine-dependent individuals., Psychiatry Res
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
Barker et al., 1999, Transmembrane domain I contributes to the permeation pathway for serotonin and ions in the serotonin transporter., J. Neurosci.
Carrera et al., 2004, Cocaine pharmacology and current pharmacotherapies for its abuse., Bioorg. Med. Chem.
Corey et al., 1994, A cocaine-sensitive Drosophila serotonin transporter: cloning, expression, and electrophysiological characterization., Proc. Natl. Acad. Sci. U.S.A.
Zhao et al., Perinatal cocaine exposure reduces myocardial norepinephrine transporter function in the neonatal rat., Neurotoxicol Teratol
Burchett et al., 1997, Serotonin, dopamine and norepinephrine transporter mRNAs: heterogeneity of distribution and response to 'binge' cocaine administration., Brain Res. Mol. Brain Res.
Galli et al., 1995, Sodium-dependent norepinephrine-induced currents in norepinephrine-transporter-transfected HEK-293 cells blocked by cocaine and antidepressants., J. Exp. Biol.
Antzelevitch, 2006, Brugada syndrome., Pacing Clin Electrophysiol
Satish et al., 2005, Brugada syndrome--an update., Chang Gung Med J
Wright et al., 1999, State-dependent cocaine block of sodium channel isoforms, chimeras, and channels coexpressed with the beta1 subunit., Biophys. J.
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Negrão AB et al., 2013, Butyrylcholinesterase genetic variants: association with cocaine dependence and related phenotypes., PLoS One
Wilson et al., 1996, Striatal dopamine, dopamine transporter, and vesicular monoamine transporter in chronic cocaine users., Ann. Neurol.
Rothman et al., 1999, Discovery of novel peptidic dopamine transporter ligands by screening a positional scanning combinatorial hexapeptide library., Synapse
Kim et al., 2003, Synthesis and pharmacology of site specific cocaine abuse treatment agents: 8-substituted isotropane (3-azabicyclo[3.2.1]octane) dopamine uptake inhibitors., J. Med. Chem.
Verma V, 2015, Classic Studies on the Interaction of Cocaine and the Dopamine Transporter., Clin Psychopharmacol Neurosci
Türkan H et al., 2019, The association between the OPRM1 A118G polymorphism and addiction in a Turkish population., Arh Hig Rada Toksikol
Arias A et al., 2006, Association of an Asn40Asp (A118G) polymorphism in the mu-opioid receptor gene with substance dependence: a meta-analysis., Drug Alcohol Depend
Schinka JA et al., 2002, A functional polymorphism within the mu-opioid receptor gene and risk for abuse of alcohol and other substances., Mol Psychiatry
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
Aroche AP et al., 2020, Association of CHRNA5 Gene Variants with Crack Cocaine Addiction., Neuromolecular Med
da Silva BS et al., 2019, The association between SYT1-rs2251214 and cocaine use disorder further supports its role in psychiatry., Prog Neuropsychopharmacol Biol Psychiatry

COCAINE SYT1

Interaction Score: 6.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31059723

Sources:
PharmGKB
COCAINE CHRNA5

Interaction Score: 1.52

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
32152934

Sources:
PharmGKB
COCAINE SLC6A1

Interaction Score: 0.61

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
COCAINE SLC6A3

Interaction Score: 0.51

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8797532 10420171 15351386 12672245 9537821 26598579

Sources:
TdgClinicalTrial TEND PharmGKB TTD
COCAINE SLC6A2

Interaction Score: 0.37

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
15113605 15351386 9387868 7500004

Sources:
TdgClinicalTrial TEND
COCAINE SLC6A4

Interaction Score: 0.36

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12057823 9537821 10366604 15351386 8302852

Sources:
TdgClinicalTrial TEND
COCAINE CHRNA3

Interaction Score: 0.3

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
32152934

Sources:
PharmGKB
COCAINE BCHE

Interaction Score: 0.29

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24312228

Sources:
PharmGKB
COCAINE KAT2B

Interaction Score: 0.23

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
COCAINE SCN5A

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17038146 15880981 9876137

Sources:
TdgClinicalTrial TEND PharmGKB
COCAINE SCN11A

Interaction Score: 0.2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
COCAINE SCN10A

Interaction Score: 0.16

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND
COCAINE OPRM1

Interaction Score: 0.1

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
31246565 16387451 11840318

Sources:
PharmGKB
COCAINE CNR1

Interaction Score: 0.08

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
COCAINE DRD3

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
COCAINE OPRK1

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND
COCAINE OPRD1

Interaction Score: 0.05

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
COCAINE GABRA2

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
COCAINE DRD1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TEND
COCAINE DRD2

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
COCAINE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9187528

Sources:
PharmGKB

TdgClinicalTrial: COCAINE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications local anesthetic

Drug Class small molecule

FDA Approval Approved before 1982

Publications:
TEND: COCAINE
- Version: 01-August-2011
Alternate Names:

Drug Info:

Drug Class anesthetics, local

Year of Approval approved before 1982

Publications:

PharmGKB: cocaine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Aroche AP et al., 2020, Association of CHRNA5 Gene Variants with Crack Cocaine Addiction., Neuromolecular Med

Negrão AB et al., 2013, Butyrylcholinesterase genetic variants: association with cocaine dependence and related phenotypes., PLoS One

Schinka JA et al., 2002, A functional polymorphism within the mu-opioid receptor gene and risk for abuse of alcohol and other substances., Mol Psychiatry

TTD: Cocaine
- Version: 2020.06.01
Alternate Names:

D04XPW TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL370805
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Trial Name	-
Novel drug target	Established target

Trial Name	-
Novel drug target	Established target

Trial Name	-
Novel drug target	Established target

Trial Name	-
Novel drug target	Established target

COCAINE Drug Record

COCAINE chembl:CHEMBL370805 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31059723

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 32152934

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 8797532 10420171 15351386 12672245 9537821 26598579

Sources: TdgClinicalTrial TEND PharmGKB TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 15113605 15351386 9387868 7500004

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 12057823 9537821 10366604 15351386 8302852

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 32152934

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24312228

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17038146 15880981 9876137

Sources: TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 17016423 17139284

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 31246565 16387451 11840318

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: None found

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info: Trial Name - Novel drug target Established target

PMIDs: None found

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Interaction Types & Directionality:

n/a

PMIDs:
31059723

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
32152934

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
8797532 10420171 15351386 12672245 9537821 26598579

Sources:
TdgClinicalTrial TEND PharmGKB TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
15113605 15351386 9387868 7500004

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
12057823 9537821 10366604 15351386 8302852

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
32152934

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
24312228

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17038146 15880981 9876137

Sources:
TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
17016423 17139284

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
31246565 16387451 11840318

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
None found

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name -

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TEND

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9187528

Sources:
PharmGKB

Drug Info:

Drug Indications local anesthetic

Drug Class small molecule

FDA Approval Approved before 1982

Drug Info:

Drug Class anesthetics, local

Year of Approval approved before 1982

Alternate Names:

D04XPW TTD Drug ID