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GR 64349

GR 64349用途

GR 64349 是有效的、高度选择性的神经激肽 2 (NK2) 受体的肽类拮抗剂,其在大鼠结肠中测得的EC50 值为 3.7 nM。GR 64349 对 NK1 和NK3 受体的选择性要低1000 和 300 倍以上。

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GR 64349名称

[ CAS 号 ]:
137593-52-3

[ 英文名 ]:
GR 64349

[英文别名 ]:

1-Lithio-2-methylnaphthalin, lithium
1-lithio-2-methylnaphthalene

GR 64349生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> 神经激肽受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 神经激肽受体

[参考文献]

[1]. Y Chang, et al. Tachykinin receptor subtypes in the isolated guinea pig heart and their role in mediating responses to neurokinin A. J Pharmacol Exp Ther. 2000 Jul;294(1):147-54.

[2]. M J Deal, et al. Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists. J Med Chem. 1992 Oct 30;35(22):4195-204.

GR 64349物理化学性质

[ 密度 ]:
1.31g/cm3

[ 沸点 ]:
1342.8ºC at 760mmHg

[ 分子式 ]:
C₄₂H₆₈N₁₀O₁₁S

[ 分子量 ]:
921.11500

[ 闪点 ]:
765.9ºC

[ 精确质量 ]:
920.47900

[ PSA ]:
372.87000

[ LogP ]:
1.98680

GR 64349MSDS

GR 64349安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

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GR 64349文献

Endogenous modulation of excitatory amino acid responsiveness by tachykinin NK1 and NK2 receptors in the rat spinal cord.

Br. J. Pharmacol. 115(6) , 1013-9, (1995)

1. The effects of selective tachykinin (neurokinin, NK) NK1 and NK2 receptor antagonists have been examined on spinal neurones in alpha-chloralose anaesthetized, spinalized rats. They were tested for ...

Tachykinin receptor types: Classification and membrane signalling mechanisms.

Neurochem. Int. 18 , 149-165, (1991)

The use of selective agonists in both functional and binding studies has provided unequivocal evidence for the existence of three types of tachykinin receptor (NK(1), NK(2) and NK(3)); there is also p...

Receptor-selective, peptidase-resistant agonists at neurokinin NK-1 and NK-2 receptors: new tools for investigating neurokinin function.

Neuropeptides 19 , 127-135, (1991)

The pharmacological profiles of two novel neurokinin agonists have been investigated. delta Ava[L-Pro9,N-MeLeu10]SP(7-11) (GR73632) and [Lys3,Gly8-R-gamma-lactam-Leu9] NKA(3-10) (GR64349) are potent a...

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