WAY-100635;WAY 100635; WAY100635
中文名称 | WAY-100635;WAY 100635; WAY100635 |
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中文同义词 | 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;化合物 T21561;WAY-100635,5-HT1A受体拮抗剂 |
英文名称 | CYCLOHEXANECARBOXAMIDE, N-[2-[4-(2-METHOXYPHENYL)-1-PIPERAZINYL]ETHYL]-N-2-PYRIDINYL-, HYDROCHLORIDE (1:3) |
英文同义词 | 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;Cyclohexanecarboxamide,N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinyl-;WAY-100635;WAY 100635; WAY100635;WAY100635 TRIHYDROCHLORIDE;N-{2-[4-(2-Methoxyphenyl)piperazin-1-yl]ethyl}-N-(pyridin-2-yl)cyclohexanecarboxaMide;WAY 100635;WAY100635;cyclohexanecarboxami |
CAS号 | 162760-96-5 |
分子式 | C25H34N4O2 |
分子量 | 422.56 |
EINECS号 | |
相关类别 | G蛋白偶联受体&G蛋白 |
Mol文件 | 162760-96-5.mol |
结构式 |
WAY-100635;WAY 100635; WAY100635 性质
熔点 | >145oC (dec.) |
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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 | 甲醇(微溶)、水(微溶) |
形态 | 固体 |
酸度系数(pKa) | 6.84±0.10(Predicted) |
颜色 | 灰白色至浅黄色 |
稳定性 | 吸湿性 |
5-HT 1A Receptor 8.87 (pIC 50 ) |
5-HT 1A Receptor 9.71 (pA2) |
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) .
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. |