129623-01-4
129623-01-4 結(jié)構(gòu)式
基本信息
英文別名
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
常見問題列表
生物活性
GR 82334 是一種有效的、特異性的可逆速激蛋白 NK1 受體 (tachykinin NK1 receptor) 拮抗劑。GR 82334 通過阻斷 NK1 受體的作用,抑制大鼠神經(jīng)肽 P 物質(zhì)誘導的致敏作用。體內(nèi)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. |