The human dopamine D2(Longer) receptor has a high-affinity state and inhibits adenylyl cyclase.
Brain dopamine D2 receptors are the main targets for antipsychotic and anti-Parkinsonian drugs. The dopamine D2 receptor has three forms, D2(Short), D2(Long) and D2(Longer). D2(Longer) is a newly found splice variant which contains two additional amino acids (valine and glutamine) in the third cytoplasmic loop of the receptor. To determine whether D2(Longer) was functional, the cDNA was transfected into CHO cells. D2(Longer) revealed a high-affinity state for dopamine ( approximately 1.5 nM), and mediated dopamine-inhibited adenylyl cyclase.
Liu
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Department of Pharmacology, Medical Sciences Building, 8 Taddle Creek Road, University of Toronto, M5S 1A8, Toronto, Canada.
George
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Seeman
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D000067956:Adenylyl Cyclase Inhibitors; D000262:Adenylyl Cyclases / Q000378:metabolism; D017398:Alternative Splicing / Q000235:genetics; D000818:Animals; D001667:Binding, Competitive; D016466:CHO Cells; D005576:Colforsin / Q000037:antagonists & inhibitors / Q000494:pharmacology; D006224:Cricetinae; D004298:Dopamine / Q000378:metabolism / Q000494:pharmacology; D018492:Dopamine Antagonists / Q000378:metabolism / Q000494:pharmacology; D004789:Enzyme Activation / Q000187:drug effects; D006165:Guanylyl Imidodiphosphate / Q000378:metabolism / Q000494:pharmacology; D006801:Humans; D017448:Receptors, Dopamine D2 / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D013134:Spiperone / Q000378:metabolism / Q000494:pharmacology; D013816:Thermodynamics
D000067956:Adenylyl Cyclase Inhibitors; D018492:Dopamine Antagonists; D017448:Receptors, Dopamine D2; D005576:Colforsin; D006165:Guanylyl Imidodiphosphate; D013134:Spiperone; D000262:Adenylyl Cyclases; D004298:Dopamine