盐酸美加明

生物活性靶点体外研究体内研究盐酸美加明试剂级价格

盐酸美加明

CAS号:826-39-1
英文名:Mecamylamine hydrochloride
中文名:盐酸美加明
CBNumber:CB0215071
分子式:C11H22ClN
分子量:203.75
MOL File:826-39-1.mol

盐酸美加明化学性质

熔点 :>240°C (dec.)
储存条件 :2-8°C
溶解度 :ethanol: 122 mg/mL
酸度系数(pKa) :pKa 11.2(H2O,t undefined,I=0.1) (Uncertain)
形态 :Solid
颜色 :White to off-white
稳定性 :Hygroscopic
CAS 数据库 :826-39-1(CAS DataBase Reference)
EPA化学物质信息 :Bicyclo[2.2.1]heptan-2-amine, N,2,3,3-tetramethyl-, hydrochloride (1:1) (826-39-1)

安全信息

危险品标志 :Xn
危险类别码 :22-36/37/38
安全说明 :36/37/39
危险品运输编号 :UN 2811 6.1/PG 3
WGK Germany :3
RTECS号 :RB6900000
危险等级 :6.1
海关编码 :2921300000

盐酸美加明性质、用途与生产工艺

生物活性 Mecamylamine hydrochloride 是一种具有口服活性，非选择性，非竞争性 nAChR 拮抗剂，具有抗神经疾病作用。Mecamylamine hydrochloride 是一种神经节阻滞剂，有潜力用于高血压研究。Mecamylamine hydrochloride 可以很容易地穿过血脑屏障。
靶点

nAChR
体外研究

Mecamylamine blocks muscle nAChRs in a use- and voltagedependent manner. Mecamylamine blocks the nicotinic currents via trapping mechanism. The main feature of this block is the phenomenon of block relief, which might be revealed by combined action of depolarization and activation of nAChRs. The experimental study of the Mecamylamine action on muscle nAChRs revealed that: (1) Mecamylamine (1-20 μM) reduces evoked end-plate currents (EPC) amplitude with Hill’s constant equal to 1.2 and IC ₅₀ = 7.8 μM at holding potential –70 mV; (2) the calculated depth of its interaction with the muscle nAChR channel is almost half of the one of neuronal nAChRs (0.37 compare to 0.72 for neuronal nAChRs); (3) simultaneous membrane depolarization and repetitive activation of postsynaptic nAChRs by motor nerve stimulation produced rapid block relief dependent on the degree of depolarization, number of conditioning signals and Mecamylamine concentration, and only slightly depended on the rate of stimulation.

体内研究

Mecamylamine (0.5-1 mg/kg; Intraperitoneal injection; C57BL/6J mice) has antidepressant-like effects in both the TST and FST and these effects are dependent on bothβ2 andα7 subunits.

Animal Model:	C57BL/6J mice (3-4 months) forced swim test (FST) and tail suspension test (TST)
Dosage:	0.5 mg/kg, 0.75 mg/kg, 1 mg/kg
Administration:	Intraperitoneal injection
Result:	Significantly decreased immobility time in the TST at the 1.0-mg/kg dose but did not alter baseline locomotor activity. Also significantly decreased time immobile in the FST.