The human dopamine D2(Longer) receptor has a high-affinity state and inhibits adenylyl cyclase

I S Liu; S R George; P Seeman

doi:10.1016/s0169-328x(00)00064-4

The human dopamine D2(Longer) receptor has a high-affinity state and inhibits adenylyl cyclase

Brain Res Mol Brain Res. 2000 May 5;77(2):281-4. doi: 10.1016/s0169-328x(00)00064-4.

Authors

I S Liu¹, S R George, P Seeman

Affiliation

¹ Department of Pharmacology, Medical Sciences Building, 8 Taddle Creek Road, University of Toronto, M5S 1A8, Toronto, Canada.

PMID: 10837924
DOI: 10.1016/s0169-328x(00)00064-4

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Adenylyl Cyclase Inhibitors*
Adenylyl Cyclases / metabolism
Alternative Splicing / genetics
Animals
Binding, Competitive
CHO Cells
Colforsin / antagonists & inhibitors
Colforsin / pharmacology
Cricetinae
Dopamine / metabolism
Dopamine / pharmacology
Dopamine Antagonists / metabolism
Dopamine Antagonists / pharmacology
Enzyme Activation / drug effects
Guanylyl Imidodiphosphate / metabolism
Guanylyl Imidodiphosphate / pharmacology
Humans
Receptors, Dopamine D2 / chemistry
Receptors, Dopamine D2 / genetics
Receptors, Dopamine D2 / metabolism*
Spiperone / metabolism
Spiperone / pharmacology
Thermodynamics

Substances

Adenylyl Cyclase Inhibitors
Dopamine Antagonists
Receptors, Dopamine D2
Colforsin
Guanylyl Imidodiphosphate
Spiperone
Adenylyl Cyclases
Dopamine