Dopamine D2 receptor antagonists

Prolactin is peptide hormone secreted by the pituitary gland. It acts on prolactin receptors in breast tissue where it stimulates production of casein and lactalbu-min. It also acts on the testes and ovaries to inhibit the effects of gonadotrophins. Since the secretion of prolactin is under tonic dopaminergic inhibition by the hypothalamus, dopamine D2-receptor antagonists... 

Derivatives of (S) N-[(l-ethyl-2-pyrrohdinyl)methyl]-6-methoxy benzamide 3 are dopamine D2 receptor antagonists. Samanta et al. obtained the following MLR QSAR for 49 derivatives with the general structure 3 [30] ... 

Risperidone-induced hyperprolactinemia has been reported to resolve with quetiapine, a low-potency dopamine D2 receptor antagonist (1037). 

Cocaine Dopamine D2 receptor antagonist Antagonist of the uptake site... 

Mehta MA, Manes FF, Magnolfi G, Sahakian BJ, Robbins TW (2004) Impaired set-shifting and dissociable effects on tests of spatial working memory following the dopamine D2 receptor antagonist sulpiride in human volunteers. Psychopharmacology (in press)... 

An example may help to clarify this statement Figure 13.4 shows the 10 highest-ranking compounds that were retrieved from the COBRA database by a topological pharmacophore similarity search (CATS method, see below). The query structure was Haloperidol, a dopamine (D2) receptor antagonist. Not surprisingly classic variations of the query structure are found in ranks 1 and 2. These are not very... 

The neuroleptic malignant syndrome has also been reported in association with the antidepressants trimipra-mine (SEDA-21, 11) (83), desipramine (SEDA-17, 18), and amoxapine (SEDA-16, 9 SEDA-17, 18) (84). Amoxapine in particular has significant dopamine D2 receptor antagonistic properties. In most cases the patients were taking several other drugs, but there have been reports of the syndrome in association with amoxapine or desipramine alone. 

Risperidone is an atypical benzisoxazole neuroleptic drug. It is a dopamine D2 receptor antagonist, with... 

Domperidone is a dopamine D2-receptor antagonist with prokinetic and antiemetic properties. It acts primarily on dopamine receptors in the gastrointestinal tract to enhance gastric and oesophageal sphincter tone, gastric emptying and propulsion of intestinal contents. 

Whenever symptoms are severe enough to impair the child s ability to function, drug therapy should be initiated. Haloperi-dol and pimozide (dopamine [D2] receptor antagonists) are approved by the FDA and are highly effective with a relatively rapid onset. Clonidine is significantly less effective but has no risk of extrapyra-midal side effects. Psychotherapy and behavioral treatment are useful adjuncts. " ... 

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