WAY-100635

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WAY-100635

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

162760-96-5

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，K_i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。

生物活性

WAY-100635 is a potent and selective 5-HT_1AReceptor antagonist with a pIC₅₀of 8.87, an apparent pA₂of 9.71. WAY-100635 is a potent and selective5-hydroxytryptamine 1A (5-HT1A) receptorantagonist with anIC₅₀value of 0.91 nM andK_ivalue of 0.39 nM. WAY-100635 haspIC₅₀values for5-HT1Aand α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potentdopamineD₄receptoragonist^[1]^[2]^[3].

IC₅₀& Target

5-HT_1AReceptor

8.87 (pIC₅₀)

5-HT_1AReceptor

9.71 (pA2)

体外研究
(In Vitro)

The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D_2Lor D_4.4receptors^[1].
WAY-100635 displays 940, 370, and 16 nM binding affinities at D_2L, D₃, and D_4.2receptors, respectively. Saturation analyses demonstrat that theK_dof [³H] WAY-100635 at D_4.2receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D_4.4cells withEC₅₀of 9.7 nM. WAY-100635 possesses high affinity for D_4.4receptor (3.3 nM)^[1].

体内研究
(In Vivo)

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^[2].

Animal Model:	Male Sprague-Dawley rats (220-240 g)^[2]
Dosage:	1 mg/kg
Administration:	Subcutaneous injection (Pharmacokinetic study)
Result:	Reduced total abstinence score, increased immobility time and the burying behavior was increased.

分子量

422.56

Formula

C₂₅H₃₄N₄O₂

CAS 号

162760-96-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.