Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DM4O7KA)

Drug Name

R-84760 Drug Info

Synonyms

R-84760; R-84761; R-86436; R 86428; R 84761; R-86428; R 86436; R 84760; 3-(1-Pyrrolidinylmethyl)-4-(5,6-dichloro-1-indancarbonyl)-tetrahydro-1,4-thiazine hydrochloride; Thiomorpholine, 4-((5,6-dichloro-2,3-dihydro-1H-inden-1-yl)carbonyl)-3-(1-pyrrolidinylmethyl)-, monohydrochloride, (R-(R*,S*))-; C19H24Cl2N2OS.HCl; 157824-23-2; AC1L3220; LS-173526; [(1S)-5,6-dichloro-2,3-dihydro-1H-inden-1-yl]-[(3R)-3-(pyrrolidin-1-ylmethyl)thiomorpholin-4-yl]methanone hydrochloride

Indication

Disease Entry	ICD 11	Status	REF
Pain	MG30-MG3Z	Discontinued in Phase 2	[1]

Cross-matching ID

PubChem CID: 133035
CAS Number: CAS 157824-23-2
TTD Drug ID: DM4O7KA

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

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Drug(s) Targeting Opioid receptor kappa (OPRK1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Nalbuphine	DMOSQGU	Pain	MG30-MG3Z	Approved	[3]
Nalfurafine hcl	DMA9DHW	Uremic pruritus	EC90.10	Approved	[4]
CHLOROXINE	DMFZBMQ	Erythema	ME64.0	Approved	[5]
Difelikefalin	DMHZBEO	Pruritus	EC90	Approved	[6]
Dezocine	DMJDB0Y	Pain	MG30-MG3Z	Approved	[7]
Asimadoline	DMND3AB	Diarrhea-predominant irritable bowel syndrome	DD91.01	Phase 3	[8]
JNJ 67953964	DMJ8Y5N	Major depressive disorder	6A70.3	Phase 3	[9]
PHN-131	DM1SV8I	Pain	MG30-MG3Z	Phase 2/3	[10]
CR-845	DMJYTUQ	Pain	MG30-MG3Z	Phase 2/3	[11]
Carfentanil	DM7ADGX	N. A.	N. A.	Phase 2	[12]
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Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

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Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Opioid receptor kappa (OPRK1)	TTQW87Y	OPRK_HUMAN	Agonist	[2]

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References

1	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800005881)
2	Effects of R-84760, a selective kappa-opioid receptor agonist, on nociceptive reflex in isolated neonatal rat spinal cord. Eur J Pharmacol. 1998 Feb 19;343(2-3):171-7.
3	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4	Drug design and synthesis of a novel kappa opioid receptor agonist with an oxabicyclo[2.2.2]octane skeleton and its pharmacology. Bioorg Med Chem Lett. 2010 Jan 1;20(1):121-4.
5	In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2). Bioorg Med Chem Lett. 2010 Dec 15;20(24):7331-6.
6	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7	Pharmacological profiles of opioid ligands at kappa opioid receptors. BMC Pharmacol. 2006 Jan 25;6:3.
8	Emerging drugs for irritable bowel syndrome. Expert Opin Emerg Drugs. 2006 May;11(2):293-313.
9	Kappa Opioid Receptor Antagonists as Potential Therapeutics for Mood and Substance Use Disorders. Handb Exp Pharmacol. 2022;271:473-491.
10	Nalbuphine: an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic. J Pharmacol Exp Ther. 1988 Jan;244(1):391-402.
11	Peptide Kappa Opioid Receptor Ligands: Potential for Drug Development. AAPS J. 2009 June; 11(2): 312-322.
12	Wax PM, Becker CE, Curry SC: Unexpected gas casualties in Moscow: a medical toxicology perspective. Ann Emerg Med. 2003 May;41(5):700-5.