(±)-trans-10,11-Dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine hydrochloride
(±)-trans-10,11-Dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine hydrochloride Basic information
- Product Name:
- (±)-trans-10,11-Dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine hydrochloride
- Synonyms:
-
- CAS:
- 137417-08-4
- MF:
- C17H18ClNO2
- MW:
- 303.79
- Mol File:
- 137417-08-4.mol
(±)-trans-10,11-Dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine hydrochloride Chemical Properties
- storage temp.
- 2-8°C
- solubility
- Soluble to 10 mM in water and to 50 mM in DMSO
- form
- Solid
- color
- Light yellow to yellow
(±)-trans-10,11-Dihydroxy-5,6,6a,7,8,12b-hexahydrobenzo[a]phenanthridine hydrochloride Usage And Synthesis
Uses
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].
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: | 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. |
IC 50
D1 Receptor: 10 nM (IC50)
storage
Desiccate at +4°C
References
[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. DOI:10.1016/0014-2999(89)90690-0
[2] Mottola DM, et al. Dihydrexidine, a novel full efficacy D1 dopamine receptor agonist. J Pharmacol Exp Ther. 1992 Jul;262(1):383-93. PMID:1352553
[3] Salmi P,et al. Dihydrexidine--the first full dopamine D1 receptor agonist. CNS Drug Rev. 2004 Fall;10(3):230-42. DOI:10.1111/j.1527-3458.2004.tb00024.x
[4] Gleason, S. D., et al. Effects of dopamine D1 receptor agonists in rats trained to discriminate dihydrexidine. Psychopharmacology, 2006;186(1), 25–31. DOI:10.1007/s00213-006-0342-2
[5] Yu FX, et al. Regulation of the Hippo-YAP pathway by G-protein-coupled receptor signaling. Cell. 2012;150(4):780-791. DOI:10.1016/j.cell.2012.06.037
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