129623-01-4
129623-01-4 结构式
基本信息
英文别名
GR 82334pglu-ala-asp-pro-asn-lys-phe-tyr-pro(spiro-γ-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-GAMMA-LACTAM)-LEU-TRP-NH2
物理化学性质
沸点1788.6±65.0 °C(Predicted)
密度1.42±0.1 g/cm3(Predicted)
储存条件−20°C
酸度系数(pKa)4.31±0.19(Predicted)
形态粉末
水溶解性Soluble to 1 mg/ml in water
序列{Glp}-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-{d-Pro(spiro-γ-lactam)Leu}-Trp-NH2
常见问题列表
生物活性
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。体内研究
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. |