WAY-100635 is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 of 0.91 nM and Ki of 0.39 nM. It exhibits pIC50 values of 8.9 and 6.6 for 5-HT1A and α1-adrenergic receptors, respectively. Moreover, WAY-100635 acts as a potent agonist of the dopamine D4 receptor [1] [2] [3].

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 has binding affinities of 940, 370, and 16 nM on D 2L, D 3, and D 4.2 receptors, respectively. Saturation analyses shows 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) [1].

Treatment with WAY-100635 (1 mg/kg; subcutaneous injection; male Sprague-Dawley rats) 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.