| Bioactivity | 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]. |
| Invitro | Dihydrexidine (DAR-0100) strongly increased YAP phosphorylation in U2OS cells[5]. |
| In Vivo | 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: |
| Name | Dihydrexidine hydrochloride |
| CAS | 137417-08-4 |
| Formula | C17H18ClNO2 |
| Molar Mass | 303.78 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 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. [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. [5]. Yu FX, et al. Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling. Cell. 2012;150(4):780-791. |