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].

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].

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].

422.56

C₂₅H₃₄N₄O₂

162760-96-5

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