| Bioactivity | SKF-82958 ((±)-SKF 82958) is a dopamine D1 receptor full agonist (K0.5=4 nM), displays selective for D1 over D2 receptors (K0.5=73 nM). SKF-82958 induces dopamine D1 receptor-dependent adenylate cyclase activity in rat striatal membranes (EC50=491 nM)[1]. |
| In Vivo | SKF-82958 ((±)-SKF 82958) (0.003-0.1 mg/kg; i.p.) results in dose-dependent increases in responding on the SKF-82958 appropriate lever, with full substitution following administration of the SKF-82958 training dose 0.03 mg/kg. Increasing the dose of SKF-82958 also results in a significant reduction in response rate[2].SKF-82958 (0.5-2.0 mg/kg; i.p) significantly suppresses pilocarpine-induced jaw movements[3]. Animal Model: |
| Name | SKF-82958 |
| CAS | 80751-65-1 |
| Formula | C19H20ClNO2 |
| Molar Mass | 329.82 |
| 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]. Mottola DM, et al. Conformational analysis of D1 dopamine receptor agonists: pharmacophore assessment and receptor mapping. J Med Chem. 1996;39(1):285-296. [2]. Haile CN, et al. The dopamine D(1) receptor agonist SKF-82958 serves as a discriminative stimulus in the rat. Eur J Pharmacol. 2000;388(2):125-131. [3]. Mayorga AJ, et al. Striatal and nigral D1 mechanisms involved in the antiparkinsonian effects of SKF-82958 (APB): studies of tremulous jaw movements in rats. Psychopharmacology (Berl). 1999;143(1):72-81. |