WAY-100635

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效且选择性的 5-HT1A 受体拮抗剂；也可作为 D4 受体的有效完全激动剂。

A potent and selective 5-HT1A receptor antagonist; also acts as potent full agonist at the D4 receptor; completely prevents not only the hyperpolarization, with an IC50 of 1.3 nM, but also the decrease in membrane input resistance produced by 5-HT and 5-carboxamidotryptamine with IC50 of 22.5 μM and 50 nM, respectively. Anxiety Phase 1 Discontinued.

The functional properties and binding affinities of WAY-100635 are evaluated in HEK 293 cells stably expressing dopamine D2L or D4.4 receptors.WAY-100635 displays 940, 370, and 16 nM binding affinities at D2L, D3, and D4.2 receptors, respectively. Saturation analyses demonstrat that the Kd of [3H] WAY-100635 at D4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D4.4 cells with EC50 of 9.7 nM. WAY-100635 possesses high affinity for D4.4 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.

WAY 100635 | WAY100635

GPCR/G Protein

5-HT Receptor

5-HT Receptor

Neurological Disease

Anxiety

162760-96-5

422.563

C25H34N4O2

>98% (HPLC)

10 mM in DMSO

O=C(C1CCCCC1)N(CCN2CCN(C3=CC=CC=C3OC)CC2)C4=NC=CC=C4

N-(2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl)-N-(pyridin-2-yl)cyclohexanecarboxamide

(-20℃)

With Ice Pack

≥ 2 years