Biological Activity
SCH 23390 hydrochloride is a potent dopamine receptor D1 antagonist with Ki values of 0.2 and 0.3 nM for the D1 and D5.
In Vitro
The commercially available hydrochloride salt has a molecular weight of 324.25 and is a white solid soluble in water (8 mg/mL), DMSO (3 mg/mL), or ethanol (2 mg/mL)[1]. SCH 23390 also shows high affinity (Ki=9.3 nM) at h5-HT2C sites[2]. SCH23390 blocks endogenous GIRK currents induced by either somatostatin or D3 dopamine receptors in AtT-20 cells (IC50=268 nM)[3].
In Vivo
SCH 23390 has been a major tool in gaining a better understanding of the role of the dopamine system. SCH 23390 is a very short-acting compound with an elimination half-life of around 25 min following administration of 0.3 mg/kg i.p. in the rat[1]. The repeated administration of SCH 23390 (0.05 mg/kg s.c., thrice daily for 21 days) enhances the steady-state density of dopamine D1 receptors in the striatum (+30%) and substantia nigra (+24%). This treatment also increases the production rates of dopamine D1 receptors in the striatum (+44%) and substantia nigra (+54%)[4]. Systemic SCH 23390 reduces saccharin seeking evidenced by a significant reduction in active lever responding and a significant reduction in the number of active lever-contingent deliveries of the tone + light cue following pretreatment with 10 μg/kg SCH 23390[5].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.