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162760-96-5

中文名称 WAY-100635;WAY 100635; WAY100635
英文名称 CYCLOHEXANECARBOXAMIDE, N-[2-[4-(2-METHOXYPHENYL)-1-PIPERAZINYL]ETHYL]-N-2-PYRIDINYL-, HYDROCHLORIDE (1:3)
CAS 162760-96-5
分子式 C25H34N4O2
分子量 422.56
MOL 文件 162760-96-5.mol
162760-96-5 结构式 162760-96-5 结构式

基本信息

中文别名
化合物 T21561
N-(2-(4-(2-甲氧基苯基)哌嗪-1-基)乙基)-N-(吡啶-2-基)环己甲酰胺
英文别名
WAY 100635
WAY100635
WAY100635 TRIHYDROCHLORIDE
WAY-100635
WAY 100635
WAY100635
Cyclohexanecarboxamide,N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-
N-{2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxaMide
CYCLOHEXANECARBOXAMIDE, N-[2-[4-(2-METHOXYPHENYL)-1-PIPERAZINYL]ETHYL]-N-2-PYRIDINYL-, HYDROCHLORIDE (1:3)
CYCLOHEXANECARBOXYLIC ACID (2-[4-(2-METHOXY-PHENYL)-PIPERAZIN-1-YL]-ETHYL)-PYRIDIN-2-YL-AMIDE TRIHYDROCHLORIDE

物理化学性质

熔点>145oC (dec.)
沸点594.8±50.0 °C(Predicted)
密度1.154±0.06 g/cm3(Predicted)
储存条件Sealed in dry,Room Temperature
溶解度少许溶于甲醇和水
酸度系数(pKa)6.84±0.10(Predicted)
形态固体
颜色灰白色至淡黄色
稳定性吸湿性

常见问题列表

生物活性
WAY-100635 是一种有效且具有选择性的 5-hydroxytryptamine 1A (5-HT1A) 受体拮抗剂,其 IC50 值为 0.91 nM,Ki 值为 0.39 nM。WAY-100635 对于 5-HT1A 和 α1-肾上腺素的 pIC50 值分别为 8.9 和 6.6。WAY-100635 也是一种有效的多巴胺 D4 受体激动剂。
靶点

5-HT 1A Receptor

8.87 (pIC 50 )

5-HT 1A Receptor

9.71 (pA2)

体外研究

The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D 2L or D 4.4 receptors.
WAY-100635 displays 940, 370, and 16 nM binding affinities at D 2L , D 3 , and D 4.2 receptors, respectively. Saturation analyses demonstrat that the K d of [ 3 H] WAY-100635 at D 4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D 4.4 cells with EC 50 of 9.7 nM. WAY-100635 possesses high affinity for D 4.4 receptor (3.3 nM) .

体内研究

WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) treatment abolishes the reduction of the severity of abstinence signs induced by Rhodiola rosea administration in nicotine-dependent rat.

Animal Model: Male Sprague-Dawley rats (220-240 g)
Dosage: 1 mg/kg
Administration: Subcutaneous injection (Pharmacokinetic study)
Result: Reduced total abstinence score, increased immobility time and the burying behavior was increased.
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