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Bromocriptine is a dopamine receptor agonist (Kis = 1,659, 12.2, 12.2, 59.7, and 1,691 nM for dopamine D1, D2, D3, D4, and D5 receptors, respectively).1 It also binds to the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT1D (Kis = 12.9 and 10.7 nM, respectively), as well as α1-adrenergic receptors (Kis = 1.12-4.17 nM).1,2 Bromocriptine (5 mg/kg) restores locomotor activity, without inducing dyskinesia, in a macaque model of Parkinson’s disease induced by MPTP.3 Formulations containing bromocriptine have been used in the treatment of Parkinson's disease, hyperprolactinemia-associated dysfunctions, and acromegaly.
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1. A review of the receptor-
2. Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes. J. Pharmacol. Exp. Ther. 303(2), 791-804 (2002).
3. Effects of chronic treatment of MPTP monkeys with bromocriptine alone or in combination with SKF 38393. Eur. J. Pharmacol. 185(2-3), 209-215 (1990).
Distinct interactions of cannabinol and its cytochrome P450-