Article
Constitutive activities and inverse agonism in dopamine receptors.
Advances in pharmacology (San Diego, Calif.) - 1 Jan 2014
Zhang Boyang, Albaker Awatif, Plouffe Bianca, Lefebvre Caroline, Tiberi Mario
Abstract excerpt
The concept of activation in the absence of agonists has been demonstrated for many GPCRs and is now solidified as one of the principal aspects of GPCR signaling. In this chapter, we review how dopamine receptors demonstrate this ability. Although difficult to prove in vivo due to the presence of endogenous dopamine and lack of subtype-selective inverse agonists and "pure" antagonists (neutral ligands), in vitro...
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