WAY-100635 is a potent and selective 5-HT_1A Receptor antagonist with a pIC₅₀ of 8.87, an apparent pA₂ of 9.71. WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC₅₀ value of 0.91 nM and K_i value of 0.39 nM. WAY-100635 has pIC₅₀ values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 is also a potent dopamine D₄ receptor agonist^[1][2][3]. IC50 & Target: pIC50 Value: 8.87 (5-HT_1A Receptor)^[1]. In Vitro: 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^[1].
WAY-100635 displays 940, 370, and 16 nM binding affinities at D_2L, D₃, and D_4.2 receptors, respectively. Saturation analyses demonstrat that the K_d of [³H] WAY-100635 at D_4.2 receptors is 2.4 nM. WAY-100635 is potent agonist in HEK-D_4.4 cells with EC₅₀ of 9.7 nM. WAY-100635 possesses high affinity for D_4.4 receptor (3.3 nM) ^[1]. 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].