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

General Information of Drug (ID: DMR2TZK)

Drug Name

GR-82334 Drug Info

Synonyms

GR 82334; 129623-01-4; Physalaemin(1-11), D-pro(9)(spiro-gamma-lactam)leu(10)-trp(11)-; Physalemin, 9-deglycine-10-((5S)-6-oxo-L-alpha-(2-methylpropyl)-1,7-diazaspiro(4.4)nonane-7-acetic acid)-11-L-tryptophanamide-; SCHEMBL7945525; gr82334; DTXSID10156209; MFCD00214619; AKOS024456738; LS-184749; B5161; GR 82334, > pGlu-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-Pro(spiro-; A-lactam-Leu-Trp-NH2

Indication

Disease Entry	ICD 11	Status	REF
Vomiting	MD90	Terminated	[1]

Cross-matching ID

PubChem CID: 16130972
CAS Number: CAS 129623-01-4
TTD Drug ID: DMR2TZK

Molecule-Related Drug Atlas

Molecule Type:

DTT

Drug Status:

Approved Drug(s)

Clinical Trial Drug(s)

Download the Complete Related Drug List

Drug(s) Targeting Substance-P receptor (TACR1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Aprepitant	DM053KT	Depression	6A70-6A7Z	Approved	[3]
Selegiline	DM6034S	Major depressive disorder	6A70.3	Approved	[4]
Rolapitant	DM8XP26	Chemotherapy-induced nausea	MD90	Approved	[5]
Netupitant	DMEKAYI	Chemotherapy-induced nausea	MD90	Phase 3	[5]
Serlopitant	DM5VH6U	Prurigo nodularis	EC91.0	Phase 3	[6]
LY-686017	DM7WORZ	Atopic dermatitis	EA80	Phase 3	[7]
Elinzanetant	DMC6EFI	Hot flushes	GA30	Phase 3	[8]
CP-122721	DMSWLM5	Major depressive disorder	6A70.3	Phase 2	[9]
FR139317	DMEL5SV	Hypertension	BA00-BA04	Phase 2	[4]
VOFOPITANT HYDROCHLORIDE	DMQMYP5	Vomiting	MD90	Phase 2	[10]
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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
Substance-P receptor (TACR1)	TTZPO1L	NK1R_HUMAN	Antagonist	[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 800005872)
2	Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions. Life Sci. 1992;51(26):PL277-80.
3	Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists. J Med Chem. 2009 May 14;52(9):3039-46.
4	Clinical pipeline report, company report or official report of GlaxoSmithKline (2009).
5	Netupitant and palonosetron trigger NK1 receptor internalization in NG108-15 cells. Exp Brain Res. 2014 Aug;232(8):2637-44.
6	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7	Stress-related neuropeptides and alcoholism: CRH, NPY and beyond. Alcohol. 2009 November; 43(7): 491-498.
8	Elinzanetant (NT-814), a Neurokinin 1,3 Receptor Antagonist, Reduces Estradiol and Progesterone in Healthy Women. J Clin Endocrinol Metab. 2021 Jul 13;106(8):e3221-e3234.
9	A review of drug options in age-related macular degeneration therapy and potential new agents. Expert Opin Pharmacother. 2006 Dec;7(17):2355-68.
10	Efficacy and safety of casopitant mesylate, a neurokinin 1 (NK1)-receptor antagonist, in prevention of chemotherapy-induced nausea and vomiting in patients receiving cisplatin-based highly emetogenicchemotherapy: a randomised, double-blind, placebo-controlled trial. Lancet Oncol. 2009 Jun;10(6):549-58.