A dopamine D1 receptor agonist
SKF 82958 is a dopamine D1 receptor agonist (K0.5 = 4 nM in a radioligand binding assay).1 It is selective for dopamine 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). SKF 82958 (3 mg/kg) prevents and reverses fentanyl-induced respiratory depression, without affecting analgesia, in cats.2 It also increases locomotion and rearing in rats.3
1.Mottola, D.M., Laiter, S., Watts, V.J., et al.Conformational analysis of D1 dopamine receptor agonists: Pharmacophore assessment and receptor mappingJ. Med. Chem.39(1)285-296(1996) 2.Lalley, P.M.D1-dopamine receptor agonists prevent and reverse opiate depression of breathing but not antinociception in the catAm. J. Physiol. Regul. Integr. Comp. Physiol.289(1)R45-R51(2005) 3.Swanson, C.J., Heath, S., Stratford, T.R., et al.Differential behavioral responses to dopaminergic stimulation of nucleus accumbens subregions in the ratPharmacol. Biochem. Behav.58(4)933-945(1997)
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