Dihydrexidine hydrochloride

• CAT Number: I026138
• CAS Number: 137417-08-4
• Molecular Formula: C17H18ClNO2
• Molecular Weight: 303.78
• Purity: ≥95%

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]. Dihydrexidine hydrochloride can stimulate YAP phosphorylation[5].
Dihydrexidine (DAR-0100) strongly increased YAP phosphorylation in U2OS cells[5].
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].

Reference

[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.
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[2]. Mottola DM, et al. Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist. J Pharmacol Exp Ther. 1992 Jul;262(1):383-93.
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[3]. Salmi P,et al. Dihydrexidine–the first full dopamine D1 receptor agonist. CNS Drug Rev. 2004 Fall;10(3):230-42.
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[4]. Gleason, S. D., et al. Effects of dopamine D1 receptor agonists in rats trained to discriminate dihydrexidine. Psychopharmacology, 2006;186(1), 25–31.
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[5]. Yu FX, et al. Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling. Cell. 2012;150(4):780-791.
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