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129623-01-4

英文名稱 GR 82334
CAS 129623-01-4
分子式 C69H91N15O16
分子量 1386.55
MOL 文件 129623-01-4.mol
129623-01-4 結(jié)構(gòu)式 129623-01-4 結(jié)構(gòu)式

基本信息

英文別名
GR 82334
pglu-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

物理化學性質(zhì)

儲存條件−20°C
形態(tài)粉末
水溶解性Soluble to 1 mg/ml in water

安全數(shù)據(jù)

安全說明22-24/25
WGK Germany3

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.
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