Rotigotine

Rotigotine has a 10-fold selectivity for D3 (pK_i 9.2) receptors compared with D2, D4 and D5 (pK_i 8.5-8.0) and a 100-fold selectivity compared with D1 receptors (pK_i 7.2). In functional studies, Rotigotine behaves as full agonist at all dopamine receptors but notably the potency for stimulation of D1 receptors is similar to that for D2 and D3 receptors (pEC₅₀ respectively: 9.0, 9.4-8.6, 9.7). Rotigotine (10 µM) decreases the number of THir neurons by 40% in primary mesencephalic cell culture. Rotigotine (0.01 µM) slightly protects dopaminergic neurons against MPP⁺ toxicity, significantly protects dopaminergic neurons against rotenone-induced cell death, and significantly inhibits ROS production by rotenone.

Dopamine Receptor Inhibitors Related Products:

Ropinirole hydrochloride; Quetiapine fumarate; Paliperidone; Amisulpride; ONC206; Sulpiride; SKF-38393 HCl; Rotigotine Hydrochloride

[1]. Wood M, et al. Rotigotine is a potent agonist at dopamine D1 receptors as well as at dopamine D2 and D3 receptors. Br J Pharmacol. 2015 Feb;172(4):1124-35.

[2]. Scheller D, et al. The in vitro receptor profile of rotigotine: a new agent for the treatment of Parkinson's disease. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):73-86.