pGlu-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-Pro(spiro-γ-lactam-Leu-Trp-NH2结构式
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常用名 | pGlu-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-Pro(spiro-γ-lactam-Leu-Trp-NH2 | 英文名 | GR 82334 |
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| CAS号 | 129623-01-4 | 分子量 | 1386.55000 | |
| 密度 | N/A | 沸点 | N/A | |
| 分子式 | C69H91N15O16 | 熔点 | N/A | |
| MSDS | 美版 | 闪点 | N/A |
用途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。 |
| 中文名 | pGlu-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-Pro(spiro-γ-lactam-Leu-Trp-NH2 |
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| 英文名 | 3-Bromocytisine |
| 描述 | 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。 |
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| 相关类别 | |
| 体内研究 | GR 82334(鞘内给药；0.1 nmol-1 nmol)在1 nmol但不在0.1 nmol时刺激大鼠无名膀胱,并且局部应用辣椒素(4μg/50μl)可降低反射性化学伤害性[1]。GR 82334(10 nM-1µM；在椎骨L4和L5之间注射)在10 nM处对两种动物都没有影响,在剂量>100 nM时增加小鼠热诱导的足部退缩潜伏期,但在裸鼹鼠中没有这种增加,剂量>100 nM引起潜伏期缩短的趋势[2]。动物模型：3-6月龄雄性C57BL/6小鼠和6-18月龄裸鼹鼠[2]剂量：10nm,100nm,1µM给药：L4和L5椎骨间注射。结果：小鼠热诱导的足退缩潜伏期增加。 |
| 参考文献 |
| 分子式 | C69H91N15O16 |
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| 分子量 | 1386.55000 |
| 精确质量 | 1385.68000 |
| PSA | 479.25000 |
| LogP | 3.53680 |
| 个人防护装备 | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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| 危险品运输编码 | NONH for all modes of transport |
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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... |
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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 ... |
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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... |
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