GR 82334

发表于由

GR 82334;

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 82334amp;;

GR 82334 Chemical Structure

CAS No. : 129623-01-4

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生物活性

GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist[1]. GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats[1].
体内研究
(In Vivo)

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)[1].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 3-6 month-old, male C57BL/6 mice and 6-18 month-old naked mole-rats[2]
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.

分子量

1386.55

Formula

C69H91N15O16
CAS 号

129623-01-4
Sequence Shortening

{Glp}ADPNKFY-{Aaa}-LW-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. A Lecci,et al.Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions. Life Sci

    [2]. Antje Brand, et al.  Functional neurokinin and NMDA receptor activity in an animal naturally lacking substance P: the naked mole-rat.PLoS One. 2010 Dec 21;5(12):e15162.