GR 82334

Modify Date: 2024-01-10 14:06:43

GR 82334 Structure
GR 82334 structure
Common Name GR 82334
CAS Number 129623-01-4 Molecular Weight 1386.55000
Density N/A Boiling Point N/A
Molecular Formula C69H91N15O16 Melting Point N/A
MSDS USA Flash Point N/A

 Use of GR 82334


GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist[1]. GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats[1].

 Names

Name 3-Bromocytisine

 GR 82334 Biological Activity

Description GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist[1]. GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats[1].
Related Catalog
In Vivo GR 82334 (intrathecal administration; 0.1 nmol-1 nmol) excites rats unnary bladder motihty at 1 nmol but not at 0.1 nmol, and the reflex chemonociceptive is reduced by the topical application of capsaicin (4 μg/50 ul)[1]. GR 82334 (10 nM-1 µM; injected between vertebrae L4 and L5) has no effect at 10 nM in neither species, increases heat-induced foot withdrawal latency in mice at doses >100 nM, but no such increase in naked mole-rats, where doses >100 nM evoke a tendency for decreased latency[2]. Animal Model: 3-6 month-old, male C57BL/6 mice and 6-18 month-old naked mole-rats[2] Dosage: 10 nM, 100 nM, and 1 µM Administration: Lntrathecal injection between vertebrae L4 and L5  Result: Increased heat-induced foot withdrawal latency in mice.
References

[1]. A Lecci,et al.Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions. Life Sci

[2]. Antje Brand, et al.  Functional neurokinin and NMDA receptor activity in an animal naturally lacking substance P: the naked mole-rat.PLoS One. 2010 Dec 21;5(12):e15162.

 Chemical & Physical Properties

Molecular Formula C69H91N15O16
Molecular Weight 1386.55000
Exact Mass 1385.68000
PSA 479.25000
LogP 3.53680

 Safety Information

Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR NONH for all modes of transport

 Articles29

More Articles
Effect of tachykinins on ascending and descending reflex pathway in rat small intestine.

Acta Pharmacol. Sin. 23(4) , 289-95, (2002)

To examine the effect of tachykinins on the ascending reflex pathway in rat small intestine, we used different selective neurokinin (NK) receptor antagonists (RA): a) NK1-RA: GR-82334 and CP-96.345, b...

Substance P modulates localized calcium transients and membrane current responses in murine colonic myocytes.

Br. J. Pharmacol. 138(7) , 1233-43, (2003)

1. Neurokinins contribute to the neural regulation of gastrointestinal (GI) smooth muscles. We studied responses of murine colonic smooth muscle cells to substance P (SP) and NK(1) and NK(2) agonists ...

Characterization of receptors for two Xenopus gastrointestinal tachykinin peptides in their species of origin.

Naunyn Schmiedebergs Arch. Pharmacol. 370(1) , 35-45, (2004)

Two tachykinin peptides, bufokinin and Xenopus neurokinin A (X-NKA) were recently isolated from Xenopus laevis. In this study we investigated the tachykinin receptors in the Xenopus gastrointestinal t...