tcsc6782 NRA-0160

NRA-0160 is a selective dopamine D4 receptor antagonist, with a K_i value of 0.48 nM and with negligible affinity for dopamine D2 receptor (K_i: >10000 nM), D3 receptor (K_i: 39 nM), rat 5-HT2A receptor (K_i: 180 nM) and rat α1 adrenoceptor (K_i: 237 nM).

IC50 & Target: Ki: 0.48 nM (D4 receptor), 39 nM (D3 receptor), 180 nM (Rat 5-HT2A receptor), 237 nM (Rat α1 adrenoceptor)^[2]

In Vivo: NRA0160 (0.1, 1, or 3 mg/kg, i.p.) has no effect on PCP-induced hyperlocomotion, stereotypy or ataxia in SD rats. NRA0160, at any dose, does not reduce cumulated counts of locomotion and cumulated scores of stereotypy emerging, and has no effect on extracellular glutamate levels and locomotor activity emerged after saline injection^[1]. NRA0160 dose-dependently and significantly reverses the effects of MAP on both A9 and Al0 dopamine neurons. NRA0160 is slightly more potent in reversiig the effects of MAP on A10 (ED₅₀ = 1.0 mg/kg) than on A9 dopamine neurons (ED₅₀ = 1.3 mg/kg). NRA0160 reverses the effect of AP0 on both A9 and A10 dopamine neurons. ED₅₀ values for the effects of NRA0160 on APO-induced inhibition of A9 and A10 dopamine neurons are 1.3 mg/kg and 0.5 mg/kg, respectively^[2].