GR 82334

Names

[ Name ]:
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]:

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

[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

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...

Related Compounds

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