N-Allylnormetazocine hydrochloride

N-Allylnormetazocine hydrochloride用途

(+)-N-烯丙基去甲唑啉((+)-SKF 10047)盐酸盐是一种苯并吗啡类阿片类药物,具有类似精神病的作用。(+)-N-烯丙基去甲唑嗪盐酸盐是一种阿片受体拮抗剂,σ1和σ2阿片受体的Ki值分别为300 nM和27μM。(+)-N-烯丙基去甲唑啉盐酸盐可用于神经疾病的研究[1][2]。

点击显示

N-Allylnormetazocine hydrochloride名称

[ CAS 号 ]:
133005-41-1

[ 英文名 ]:
N-Allylnormetazocine hydrochloride

[英文别名 ]:

(+)-N-Allylnormetazocine hydrochloride

N-Allylnormetazocine hydrochloride生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 阿片受体

信号通路 >> 神经信号通路 >> 阿片受体

研究领域 >> 神经疾病

[体外研究]

(+)-N-烯丙基去甲唑啉盐酸盐(1 nM)对 µ,δ 和 κ 阿片受体的抑制率分别为 28.5%,2.5% 和 31%[1]。 (+)-N-烯丙基去甲唑啉盐酸盐对 σ1 和 σ2 阿片受体的 Ki公司值分别为 300纳米和 27μM[1]

[体内研究]

(+)-N-烯丙基去甲唑嗪盐酸盐(0.3,1,3,10和 30 mg/kg腹腔注射,每次实验前10分钟) 剂量依赖性地增加解离性麻醉药苯环利定 (PCP)的反应[2]。

[参考文献]

[1]. May EL, et al. Synthesis and in vitro and in vivo activity of (-)-(1R,5R,9R)- and (+)-(1S,5S,9S)-N-alkenyl-, -N-alkynyl-, and -N-cyanoalkyl-5, 9-dimethyl-2'-hydroxy-6,7-benzomorphan homologues. J Med Chem. 2000 Dec 28;43(26):5030-6.

[2]. Brady KT, et al. Stereoisomers of N-allylnormetazocine: phencyclidine-like behavioral effects in squirrel monkeys and rats. Science. 1982 Jan 8;215(4529):178-80.

N-Allylnormetazocine hydrochloride物理化学性质

[ 分子式 ]:
C₁₇H₂₄ClNO

[ 分子量 ]:
293.83200

[ 精确质量 ]:
293.15500

[ PSA ]:
23.47000

[ LogP ]:
3.84230

N-Allylnormetazocine hydrochloride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

N-Allylnormetazocine hydrochloride文献

Allosteric modulation of sigma-1 receptors elicits anti-seizure activities.

Br. J. Pharmacol. 172 , 4052-65, (2015)

Application of orthosteric sigma-1 receptor agonists as anti-seizure drugs has been hindered by questionable efficacy and potential adverse effects. Here, we have investigated the anti-seizure effects...

Sigma1 recognition sites in rabbit iris-ciliary body: topical sigma1-site agonists lower intraocular pressure.

J. Pharmacol. Exp. Ther. 289 , 1362, (1999)

In this study, we examined the presence of sigma1 and sigma2 sites in the rabbit iris-ciliary body by receptor binding and investigated their effects on intraocular pressure (IOP) in albino rabbits. T...

sigma receptor ligands attenuate N-methyl-D-aspartate cytotoxicity in dopaminergic neurons of mesencephalic slice cultures.

Eur. J. Pharmacol. 388 , 139-146, (2000)

We investigated the potential neuroprotective effects of several sigma receptor ligands in organotypic midbrain slice cultures as an excitotoxicity model system. When challenged with 100-microM N-meth...

更多文献