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Domperidone is a dopamine D2 receptor antagonist (Ki = 0.3 nM in CHO cells expressing the rat receptor).1,2 It is selective for dopamine D2 over D3 receptors (Ki = 9.5 nM).1 Domperidone (0.5-5 μg/kg) inhibits dipropyl dopamine-induced femoral vasodilation in dogs, indicating dopamine D2 receptor antagonist activity, and has no effect on dopamine-induced vasodilation in the renal vascular bed in dogs when administered at doses up to 5 mg/kg, indicating a lack of activity at dopamine D1 receptors.2 Domperidone (0.5 mg/kg) prevents dopamine-induced decreases in gastric antral motility induced by pentagastrin (Item No. 28546) in dogs.3 It inhibits apomorphine-induced emesis in dogs (ED50 = 0.031 mg/kg, p.o.).4 Domperidone also increases serum levels of prolactin in male rats.5
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1. Molecular cloning and characterization of a novel dopamine receptor (D3) as a target for neuroleptics. Nature 137(6289), 146-151 (1990).
2. Selective DA2 versus DA1 antagonist activity of domperidone in the periphery. Eur. J. Pharmacol. 89(1-2), 137-141 (1983).
3. Effect of dopamine on pentagastrin-
4. Antiemetic specificity of dopamine antagonists. Psychopharmacology (Berl.) 78(3), 210-213 (1982).
5. Effects of a series of substituted benzamides on rat prolactin secretion and 3H-