Agonist activity at human GPR52 expressed in HEK293 cells assessed as increase in cAMP levels incubated for 15 mins by Glosensor cAMP assay relative to N-(2-hydroxyethyl)-1-(4-(3-(trifluoromethyl)benzyl)pyridin-2-yl)indoline-4-carboxamide
Agonist activity at GPR52 (unknown origin) expressed in CHO-K1 or HEK293 cells assessed as intracellular cAMP accumulation incubated for 1 hr by HTRF assay
In vivo agonist activity at GPR52 in po dosed C57BL/6 mouse assessed as inhibition of basal locomotor activity measured for 60 mins starting at 15 mins post-drug challenge
In vivo agonist activity at GPR52 in C57BL/6 mouse assessed as inhibition of basal locomotor activity at 10 mg/kg, po measured for 60 mins starting at 15 mins post-drug challenge
Antipsychotic activity in Sprague-Dawley rat assessed as inhibition of amphetamine-stimulated locomotor activity at 0.5 to 20 mg/kg, po administered 15 mins prior to amphetamine stimulation and measured for 30 to 60 mins post-drug dosage
Antipsychotic activity in Sprague-Dawley rat assessed as inhibition of amphetamine-induced disruption of prepulse inhibition at 5 to 20 mg/kg, po administered 15 mins prior to amphetamine challenge and measured after 15 mins
Antipsychotic activity in Sprague-Dawley rat assessed as inhibition of MK801-induced disruption of prepulse inhibition at 5 to 20 mg/kg, po administered 15 mins prior to amphetamine challenge and measured after 15 mins
Antipsychotic activity in 129Sv/Ev mouse assessed as inhibition of MK801-induced disruption of prepulse inhibition at 10 mg/kg, po co-administered with haloperidol at 15 mins prior to MK801 challenge and measured after 15 mins
Induction of hyperprolactinemia in Sprague-Dawley rat assessed as increase in prolactin release in plasma at 1 to 100 mg/kg, po measured after 60 mins by ELISA
Inhibition of haloperidol-induced hyperprolactinemia in Sprague-Dawley rat assessed as reduction in prolactin release in plasma at 10 mg/kg, po administered 30 mins prior to 0.3 mg/kg haloperidol challenge and measured after 60 mins by ELISA