NGD94-1

NGD94-1 is a potent and selective dopamine D4 receptor antagonist. NGD94-1 shows high affinity for the cloned human D4.2 receptor (K_i = 3.6 nM). NGD94-1 modulates the cognitive functions of the frontostriatal system and regulates dopaminergic transmission in Phencyclidine (PCP)-induced monkeys. NGD94-1 can be used for neurological disease research^[1][2]. In Vitro:NGD 94-1 shows >600-fold selectivity for the D4.2 receptor over many other targets; however, its selectivity is significantly lower over the 5-HT1A (~50-fold) and 5-HT3 (~200-fold) receptors^[2].
NGD 94-1 induces inhibition of cAMP accumulation in HEK293/D4 cells, but does not affect Forskolin (HY-15371)-stimulated cAMP formation in non-transfected HEK293 cells, demonstrating that its inhibitory action is specifically mediated through the transfected dopamine D4 receptors^[3]. In Vivo:NGD94-1 (1-5 mg/kg, i.m., 45 min prior to testing) reverses the cognitive deficits, and increases the accumulation of HVA in the cisternal cerebrospinal fluid of PCP pre-treated monkeys^[1].