| Bioactivity | (+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) is a dopamine D1 receptor agonist with an EC50 of 72± 21 nM. |
| Target | EC50: 72±21 nM (Dopamine D1 receptor) |
| Invitro | (+)-Dihydrexidine hydrochloride (DHX) is a high-potency, bioavailable D1 dopamine receptor agonist. (+)-Dihydrexidine is screened for activity against 40 other binding sites, and is inactive (IC50 greater than 10 microM) against all except D2 dopamine receptors (IC50=130 nM) and alpha 2 adrenoreceptors (IC50=230 nM). Dihydrexidine competes stereoselectively and potently for D1 binding sites in rat striatal membranes labeled with [3H]SCH23390 with an IC50 of about 10 nM compared to about 30 nM for the prototypical D1 agonist SKF38393[2]. |
| In Vivo | To examine the functional state of striatal neurons in response to D1 receptor activation, AC5+/+ and AC5-/- mice are injected with the D1 agonist (+)-Dihydrexidine (30 mg/kg, i.p.) and obtained the dorso-lateral striatum and NAc, separately, 45 min later for RT-PCR analysis. These experiments reveal that (+)-Dihydrexidine -triggered induction of the immediate early genes, c-fos, egr-1, and junB, in the NAc is markedly enhanced in AC5-/- mice compared with that in AC5+/+ mice, while the induction in the dorso-lateral striatum is suppressed in AC5-/- mice[3]. |
| Name | (+)-Dihydrexidine hydrochloride |
| CAS | 158704-02-0 |
| Formula | C17H18ClNO2 |
| Molar Mass | 303.78 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Lewis MM, et al. Homologous desensitization of the D1A dopamine receptor: efficacy in causing desensitizationdissociates from both receptor occupancy and functional potency. J Pharmacol Exp Ther. 1998 Jul;286(1):345-53. [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]. Kim KS, et al. Adenylyl cyclase-5 activity in the nucleus accumbens regulates anxiety-related behavior. J Neurochem. 2008 Oct;107(1):105-15. |
(+)-Dihydrexidine hydrochloride
CAS: 158704-02-0 F: C17H18ClNO2 W: 303.78
(+)-Dihydrexidine hydrochloride ((+)-DAR-0100 hydrochloride) is a dopamine D1 receptor agonist with an EC50 of 72± 21 n
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