Target Information

Target General Information

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Target ID

T23547 (Former ID: TTDS00125)

Target Name

Opioid receptor (OPR)

Synonyms

Opioid receptor

Click to Show/Hide

Gene Name

NO-GeName

Target Type

Successful target

[1]

Disease

[+] 5 Target-related Diseases

Cough [ICD-11: MD12]

Opioid use disorder [ICD-11: 6C43]

Pain [ICD-11: MG30-MG3Z]

Sensation disturbance [ICD-11: MB40]

Substance abuse [ICD-11: 6C40]

UniProt ID

NOUNIPROTAC

Drugs and Modes of Action

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Approved Drug(s)

[+] 11 Approved Drugs

Dextropropoxyphene

Drug Info

Approved

Pain

[2], [3]

Ketobemidone

Drug Info

Approved

Pain

[4]

Levorphanol

Drug Info

Approved

Pain

[4]

Methadone

Drug Info

Approved

Dry cough

[4]

Nalmefene

Drug Info

Approved

Opioid dependence

[4]

Naltrexone

Drug Info

Approved

Alcohol dependence

[4]

Oxymorphone

Drug Info

Approved

Pain

[4]

Pentazocine

Drug Info

Approved

Pain

[4]

Sufentanil

Drug Info

Approved

Analgesia

[4]

Tilidine

Drug Info

Approved

Pain

[4]

Dihydrocodeine

Drug Info

Phase 4

Cancer related pain

[5], [6]

Clinical Trial Drug(s)

[+] 14 Clinical Trial Drugs

ALO-02

Drug Info

Phase 3

Pain

[7]

AMG 386

Drug Info

Phase 3

Neuropathic pain

[8]

Bupropion+naltrexone

Drug Info

Phase 3

Obesity

[9]

AeroLEF

Drug Info

Phase 2

Pain

[10]

AZD-7268

Drug Info

Phase 2

Anxiety disorder

[11], [12]

CNSB-001

Drug Info

Phase 2

Neuropathic pain

[13]

JKB-122

Drug Info

Phase 2

Hepatitis virus infection

[14]

NP-2

Drug Info

Phase 2

Influenza A virus infection

[15]

OCFENTANIL

Drug Info

Phase 2

Pain

[16]

Odelepran

Drug Info

Phase 2

Alcohol dependence

[17]

Oxytrex

Drug Info

Phase 2

Pain

[18]

S-297995

Drug Info

Phase 2

Opioid dependence

[19]

PTI-202

Drug Info

Phase 1

Pain

[20]

SYN-1001

Drug Info

Phase 1

Pain

[21]

Discontinued Drug(s)

[+] 10 Discontinued Drugs

Propiram fumarate

Drug Info

Discontinued in Phase 3

Cancer related pain

[22]

CereCRIB

Drug Info

Discontinued in Phase 2

Pain

[23]

OxycoDex

Drug Info

Discontinued in Phase 2

Pain

[24]

PTI-701

Drug Info

Discontinued in Phase 2

Pain

[25]

Ultramorph

Drug Info

Discontinued in Phase 2

Pain

[26]

BL-1827

Drug Info

Discontinued in Phase 1

Cancer related pain

[27]

APF-580

Drug Info

Terminated

Pain

[29]

EK-399

Drug Info

Terminated

Inflammation

[30]

Org-30035

Drug Info

Terminated

Psychotic disorder

[31]

OX-23

Drug Info

Terminated

Pain

[32]

Preclinical Drug(s)

[+] 1 Preclinical Drugs

CB-01-16

Drug Info

Preclinical

Constipation

[28]

Mode of Action

[+] 3 Modes of Action

Agonist

[+] 9 Agonist drugs

Dextropropoxyphene

Drug Info

[3]

Levorphanol

Drug Info

[34]

Methadone

Drug Info

[1], [35]

AMG 386

Drug Info

[8]

AeroLEF

Drug Info

[46]

CNSB-001

Drug Info

[48]

SYN-1001

Drug Info

[55]

Ultramorph

Drug Info

[60]

BL-1827

Drug Info

[61]

Modulator

[+] 18 Modulator drugs

Ketobemidone

Drug Info

[4], [33]

Oxymorphone

Drug Info

[39]

Tilidine

Drug Info

[4], [42]

Dihydrocodeine

Drug Info

[43]

ALO-02

Drug Info

[44]

AZD-7268

Drug Info

[47]

JKB-122

Drug Info

[4], [49]

OCFENTANIL

Drug Info

[4], [51]

Oxytrex

Drug Info

[53]

PTI-202

Drug Info

[54]

Propiram fumarate

Drug Info

[56]

CereCRIB

Drug Info

[57]

OxycoDex

Drug Info

[58]

PTI-701

Drug Info

[59]

APF-580

Drug Info

[63]

EK-399

Drug Info

[64]

Org-30035

Drug Info

[65]

BRIFENTANIL

Drug Info

[4], [67]

Antagonist

[+] 10 Antagonist drugs

Nalmefene

Drug Info

[36], [37]

Naltrexone

Drug Info

[4], [38]

Pentazocine

Drug Info

[40], [41]

Sufentanil

Drug Info

[35]

Bupropion+naltrexone

Drug Info

[45]

NP-2

Drug Info

[50]

Odelepran

Drug Info

[52]

S-297995

Drug Info

[19]

CB-01-16

Drug Info

[62]

Cyprodine

Drug Info

[68]

Drug Property Profile of Target

Top

(1) Molecular Weight (mw) based Drug Clustering

(2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering

(3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering

(4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering

(5) Rotatable Bond Count (rotbonds) based Drug Clustering

(6) Topological Polar Surface Area (polararea) based Drug Clustering

"RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five

Co-Targets

Top

Co-Targets

Co-Targets Info

Target-Related Models and Studies

Top

Target Validation

Target Validation Info

References

Top

REF 1

Methadone treatment and its dangers. Medicina (Kaunas). 2009;45(5):419-25.

REF 2

URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7593).

REF 3

Retrospective diagnosis of an adverse drug reaction in a breastfed neonate: liquid chromatography-tandem mass spectrometry quantification of dextropropoxyphene and norpropoxyphene in newborn and maternal hair. J Anal Toxicol. 2008 Nov-Dec;39(9):787-9.

REF 4

Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015

REF 5

REF 6

ClinicalTrials.gov (NCT00547885) Randomized Controlled Double Blind Trial of Short vs Long Acting Dihydrocodeine in Chronic Non-malignant Pain. U.S. National Institutes of Health.

REF 7

Clinical pipeline report, company report or official report of Pfizer.

REF 8

Emerging drugs in neuropathic pain. Expert Opin Emerg Drugs. 2007 Mar;12(1):113-26.

REF 9

A randomized, phase 3 trial of naltrexone SR/bupropion SR on weight and obesity-related risk factors (COR-II). Obesity (Silver Spring). 2013 May;21(5):935-43.

REF 10

ClinicalTrials.gov (NCT00791804) Phase II Study of Inhaled AeroLEF for Analgesia After ACL Knee Surgery. U.S. National Institutes of Health.

REF 11

REF 12

ClinicalTrials.gov (NCT01020799) AZD7268 Safety and Tolerability Study. U.S. National Institutes of Health.

REF 13

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800029018)

REF 14

ClinicalTrials.gov (NCT02556372) Liver Test Study of Using JKB-122 in AIH Patients.

REF 15

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800028817)

REF 16

A phase II clinical study of once-a-day fentanyl citrate patch in patients with cancer pain--switching from once-every-three-days fentanyl patch to once-a-day fentanyl citrate patch. Gan To Kagaku Ryoho. 2010 Sep;37(9):1747-52.

REF 17

ClinicalTrials.gov (NCT00804570) A Study for the Treatment of Alcohol Dependence.. U.S. National Institutes of Health.

REF 18

ClinicalTrials.gov (NCT00734461) Study to Evaluate the Subjective Effects of PTI-801 in Non-Physically Dependent Subjects With a History of Drug Abuse. U.S. National Institutes of Health.

REF 19

Clinical pipeline report, company report or official report of Shionogi (2011).

REF 20

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800024906)

REF 21

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019167)

REF 22

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003460)

REF 23

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007886)

REF 24

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017613)

REF 25

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014737)

REF 26

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013632)

REF 27

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013581)

REF 28

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800030751)

REF 29

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026787)

REF 30

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004080)

REF 31

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002901)

REF 32

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027164)

REF 33

The mu1 and mu2 opioid receptor binding of ketobemidone, norketobemidone and 3-dimethylamino-1,1-diphenylbutene. Pharmacol Toxicol. 1996 Aug;79(2):103-4.

REF 34

Comparison of the effects of dextromethorphan, dextrorphan, and levorphanol on the hypothalamo-pituitary-adrenal axis. J Pharmacol Exp Ther. 2004 May;309(2):515-22.

REF 35

mu-opioid receptor-stimulated synthesis of reactive oxygen species is mediated via phospholipase D2. J Neurochem. 2009 Aug;110(4):1288-96.

REF 36

Unconditioned behavioral effects of the powerful kappa-opioid hallucinogen salvinorin A in nonhuman primates: fast onset and entry into cerebrospin... J Pharmacol Exp Ther. 2009 Feb;328(2):588-97.

REF 37

Effects of opioid receptor gene variation on targeted nalmefene treatment in heavy drinkers. Alcohol Clin Exp Res. 2008 Jul;32(7):1159-66.

REF 38

An evaluation of mu-opioid receptor (OPRM1) as a predictor of naltrexone response in the treatment of alcohol dependence: results from the Combined Pharmacotherapies and Behavioral Interventions for Alcohol Dependence (COMBINE) study. Arch Gen Psychiatry. 2008 Feb;65(2):135-44.

REF 39

REF 40

Functional characterization of a sigma receptor and its gene expression by haloperidol. Nippon Yakurigaku Zasshi. 1999 Jul;114(1):61-8.

REF 41

Propiram. A review of its pharmacodynamic and pharmacokinetic properties, and clinical use as an analgesic. Drugs. 1993 Sep;46(3):428-45.

REF 42

Actions of tilidine and nortilidine on cloned opioid receptors. Eur J Pharmacol. 2005 Jan 4;506(3):205-8.

REF 43

Affinities of dihydrocodeine and its metabolites to opioid receptors. Pharmacol Toxicol. 2002 Aug;91(2):57-63.

REF 44

Adding ultralow-dose naltrexone to oxycodone enhances and prolongs analgesia: a randomized, controlled trial of Oxytrex. J Pain. 2005 Jun;6(6):392-9.

REF 45

Anti-obesity drugs. Expert Opin Pharmacother. 2008 Jun;9(8):1339-50.

REF 46

Current Research on Opioid Receptor Function. Curr Drug Targets. 2012 February; 13(2): 230-246.

REF 47

EP patent application no. 2774991, Drug delivery system for use in the treatment or diagnosis of neurological disorders.

REF 48

Molecular Mechanisms of Opioid Receptor-Dependent Signaling and Behavior. Anesthesiology. 2011 December; 115(6): 1363-1381.

REF 49

WO patent application no. 2011,1401,90, Tetrazolones as inhibitors of fatty acid synthase.

REF 50

Vascular endothelial growth factor receptor-1 and neuropilin-2 form complexes. J Biol Chem. 2001 Jun 1;276(22):18688-94.

REF 51

Comparison of ocfentanil and fentanyl as supplements to general anesthesia. Anesth Analg. 1991 Nov;73(5):622-6.

REF 52

A phase 2, placebo-controlled study of the opioid receptor antagonist LY2196044 for the treatment of alcohol dependence. Alcohol Clin Exp Res. 2014 Feb;38(2):511-20.

REF 53

Oxytrex: an oxycodone and ultra-low-dose naltrexone formulation. Expert Opin Investig Drugs. 2007 Aug;16(8):1277-83.

REF 54

Clinical pipeline report, company report or official report of Pain Therapeutics, Inc.

REF 55

Improved brain uptake and pharmacological activity profile of morphine-6-glucuronide using a peptide vector-mediated strategy. J Pharmacol Exp Ther. 2005 May;313(2):712-9.

REF 56

The relative analgesic efficacy of propiram fumarate, codeine, aspirin, and placebo in post-impaction dental pain. J Clin Pharmacol. 1984 Jan;24(1):35-42.

REF 57

US patent application no. 5,874,099, Methods for making immunoisolatary implantable vehicles with a biocompatible jacket and a biocompatible matrix core.

REF 58

Differential activation of the -opioid receptor by oxycodone and morphine in pain-related brain regions in a bone cancer pain model. Br J Pharmacol. 2013 Jan;168(2):375-88.

REF 59

Clinical pipeline report, company report or official report of Pain Therapeutics.

REF 60

Antagonists of excitatory opioid receptor functions enhance morphine's analgesic potency and attenuate opioid tolerance/dependence liability. Pain. 2000 Feb;84(2-3):121-31.

REF 61

Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013581)

REF 62

Clinical pipeline report, company report or official report of Cosmo.

REF 63

WO patent application no. 2010,0094,51, Long-acting injectable analgesic formulations for animals.

REF 64

Evaluation of the discriminative stimulus effect of an enkephalin analog, EK-399, in the rat. Nihon Yakurigaku Zasshi. 1991 Jun;97(6):361-9.

REF 65

WO patent application no. 2010,0332,07, Polymer conjugates of therapeutic peptides.

REF 66

CA patent application no. 212323, Method for improving gastrointestinal motility.

REF 67

Synthesis and pharmacological evaluation of a series of new 3-methyl-1,4-disubstituted-piperidine analgesics. J Med Chem. 1990 Oct;33(10):2876-82.

REF 68

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