162760-96-5 WAY-100635

• 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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