GR 82334 是一种有效的、特异性的可逆速激蛋白NK1受体(tachykinin NK1 receptor)拮抗剂。GR 82334通过阻断NK1受体的作用,抑制大鼠神经肽P物质诱导的致敏作用。
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].
分子量:1386.55
分子式:C69H91N15O16
CAS 号:129623-01-4
序列:Glp-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-{d-Pro(spiro-γ-lactam)Leu}-Trp-NH2
外观与性状: 白色粉末状固体
消光系数: -
来源: 人工化学合成,仅限科学研究使用,不得用于人体。
纯度: 95%、98%
盐体系: 可选TFA、HAc、HCl或其它
生成周期: 2-3周
储存条件: 负80℃至负20℃
参考文献:
Functional neurokinin and NMDA receptor activity in an animal naturally lacking substance P: the naked mole-rat【DOI: 10.1371/journal.pone.0015162】