5-HT1A modulator 1 exhibits high affinities for the 5-HT1A, α1-adrenergic receptor, and D2 receptor (IC50s = 2 nM, 10 nM, and 40 nM).

D2 receptor:40 nM, 5-HT1B receptor:300 nM, α1-adrenoceptor:10 nM, SPLA2:2 nM, 5-HT2C receptor:4000 nM, 5-HT2A receptor:500 nM

5-HT1A modulator 1 displays affinities for the 5-HT1B, 5-HT2A, and 5-HT2C (IC50s = 300 nM, 500 nM, and 4000 nM)[1].

5-HT1A modulator 1 (1 mg/kg; i.p) shows 94% antagonist action at 5-HT2A subtype in mice. 5-HT1A modulator 1 (1 mg/kg; i.p) completely blocks the stereotypes and the climbing. In rats, 5-HT1A modulator 1 (2 and 4 mg/kg; p.o) shows a respective 63% and 58% of antagonism and the antagonism is complete (103% and 108%) at doses of 8 and 16 mg/kg. 5-HT1A modulator 1 significantly reduces hyperactivity by 50%[1].

Binding was determined using membranes prepared from bovine hippocampus. Receptors were labeled with 0.5 nM [3H]-8-OH-DPAT by incubating with 11 concentrations of test compounds (1-10^5 nM) for 30 min at 25°C. Nonspecific binding was determined using 10 μM buspirone. Competition experiments were analyzed using the iterative nonlinear least squares curve fitting program Inplot 4, GraphPad. IC50 values were calculated using the Cheng-Prusoff equation.

Inject Swiss mice with test compounds (e.g. 5-HT1A modulators 1, 0.25 and 1 mg/kg i.p) prior to injection of 5-HTP (400 mg/kg i.p). Count the number of head twitches that occurred during the 10 minutes starting 10 minutes after the injection of 5HTP. Cyproheptadine was used as reference compound. Wistar rats (n=6) were used. 5-HT1A Modulator 1 was tested at pharmacological doses (1 and 2 mg/kg i.p) and high doses (32 and 64 mg/kg i.p). The intensity of forepaw pedaling was expressed as a percentage of the maximum possible score. The 5-HT1A agonist 8-OH-DPAT induced forepaw trampling and was used as a reference compound.