Bromocriptine-13C-d3 is intended for use as an internal standard for the quantification of bromocriptine by GC- or LC-MS. 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.
1.Kvernmo, T., HÄrtter, S., and BÜrger, E.A review of the receptor-binding and pharmacokinetic properties of dopamine agonistsClin. Ther.28(8)1065-1078(2006) 2.Millan, M.J., Maiofiss, L., Cussac, D., et al.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 subtypesJ. Pharmacol. Exp. Ther.303(2)791-804(2002) 3.Rouillard, C., BÉdard, P.J., and De Paolo, T.Effects of chronic treatment of MPTP monkeys with bromocriptine alone or in combination with SKF 38393Eur. J. Pharmacol.185(2-3)209-215(1990)