UCM-1306，5MG，SML3749-5MG，Sigma

Biochem/physiol Actions

Orally active dopamine receptor D1-selective postive allosteric modulator (PAM) in vitro and in vivo.

UCM-1306 is an orally active dopamine receptor D1-selective postive allosteric modulator (PAM) void of D1 agonist activity. UCM-1306 potentiates dopamine (DA)-induced cAMP in the SK-N-MC neuroblastoma cell line with endogenous D1R (EC50/Emax = 60 nM/45% with [DA] = EC70; Emax = 55% with [DA] = 10 μM), but not D5R, by modulating DA affinity for the receptor, while displaying low binding competition against orthosteric ligands. UCM-1306 augments cocaine (20 mg/kg s.c.)-induced locomotion (1 mg/kg i.p.) and enhances L-DOPA (100-400 mg/kg i.p.) recovery of decreased locomotor activity in reserpinized (2.5 mg/kg s.c.) mice in vivo (30 mg/kg p.o.).