(±)-trans-10,11-Dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine hydrochloride

Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity[1][2][3][4].

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

IC50: 10 nM (D1 dopamine receptor), D5 dopamine receptor, 660 nM (D2 dopamine receptor)[1]

Dihydrexidine hydrochloride has poor oral bioavailability and a relatively short half-life of 1 to 2 h[3]. Dihydrexidine hydrochloride (3 mg/kg; i.p.) produces prominent dopamine D1 receptor agonist effects in vivo[4]. Animal Model: Adult male Sprague–Dawley rats (275-300 g)[4] Dosage: 3 mg/kg Administration: Intraperitoneal injection Result: Produces prominent dopamine D1 receptor agonist effects in vivo.

[1]. Lovenberg TW, et al. Dihydrexidine, a novel selective high potency full dopamine D-1 receptor agonist. Eur J Pharmacol. 1989 Jul 4;166(1):111-3.

[2]. Mottola DM, et al. Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist. J Pharmacol Exp Ther. 1992 Jul;262(1):383-93.

[3]. Salmi P,et al. Dihydrexidine--the first full dopamine D1 receptor agonist. CNS Drug Rev. 2004 Fall;10(3):230-42.

[4]. Gleason, S. D., et al. Effects of dopamine D1 receptor agonists in rats trained to discriminate dihydrexidine. Psychopharmacology, 2006;186(1), 25–31.