| Description |
Ropinirole (SKF 101468) is an orally active, potent D3/D2 receptor agonist with a Ki of 29 nM for D2 receptor. Ropinirole has pEC50s of 7.4, 8.4 and 6.8 for hD2, hD3 and hD4 receptors, respectively. Ropinirole has no affinity for the D1 receptors. Ropinirole has the potential for Parkinson's disease[1][2].
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| Related Catalog |
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| Target |
D2 Receptor:29 nM (Ki)
hD2 Receptor:7.4 (pEC50)
hD3 Receptor:8.4 (pEC50)
hD4.4 Receptor:6.8 (pEC50)
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| In Vitro |
Ropinirole has affinity for D3 receptors of 10-20 fold higher than the D2 and D4 receptors. Ropinirole is weakly active at alpha 2-adrenoceptors and 5-HT2 receptors but inactive at 5-HT1, benzodiazepine and gamma-aminobutyric acid receptors or alpha 1 and beta-adrenoceptors[1][2].
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| In Vivo |
Ropinirole (0.1-10 mg/kg; i.p.) decreases intracranial self-stimulation (ICSS) thresholds and induces anxiolytic- and antidepressive-like effects without affecting motor activity or spatial memory[2].
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| References |
[1]. Eden, R.J., et al., Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist. Pharmacol Biochem Behav, 1991. 38(1): p. 147-54. [2]. Mavrikaki M, et al. Ropinirole regulates emotionality and neuronal activity markers in the limbic forebrain. Int J Neuropsychopharmacol. 2014 Dec;17(12):1981-93.
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