| 中文名称 | GR 82334 |
|---|---|
| 中文同义词 | |
| 英文名称 | GR 82334 |
| 英文同义词 | GR 82334;PGLU-ALA-ASP-PRO-ASN-LYS-PHE-TYR-PRO(SPIRO-GAMMA-LACTAM)-LEU-TRP-NH2;[[(S,S)PRO-LEU(SPIRO-GAMMA-LACTAM)]9,10, TRP11]PHYSALAEMIN (1-11);pglu-ala-asp-pro-asn-lys-phe-tyr-pro(spiro-γ-lactam-leu-trp-nh2;L-Tryptophanamide, 5-oxo-L-prolyl-L-alanyl-L-α-aspartyl-L-prolyl-L-asparaginyl-L-lysyl-L-phenylalanyl-L-tyrosyl-(αS,5S)-α-(2-methylpropyl)-6-oxo-1,7-diazaspiro[4.4]nonane-7-acetyl- |
| CAS号 | 129623-01-4 |
| 分子式 | C69H91N15O16 |
| 分子量 | 1386.55 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 129623-01-4.mol |
| 结构式 |  |
GR 82334 性质
| 沸点 | 1788.6±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.42±0.1 g/cm3(Predicted) |
| 储存条件 | −20°C |
| 形态 | 粉末 |
| 酸度系数(pKa) | 4.31±0.19(Predicted) |
| 水溶解性 | Soluble to 1 mg/ml in water |
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).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.
| Animal Model: | 3-6 month-old, male C57BL/6 mice and 6-18 month-old naked mole-rats |
| 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. |
安全信息
| 安全说明 | 22-24/25 |
|---|---|
| WGK Germany | 3 |
| 提供商 | 语言 |
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英文
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