Abstract
Zn2+ is abundant in the brain, where it plays a role in the function of a number of enzymes, structural proteins, and transcription factors. Zn2+ is also found in synaptic vesicles and is released into synapses achieving concentrations in the range of 100 to 300 μM [Proc Natl Acad Sci USA1997;94:13386–13387; Mol Pharmacol1997;51:1015–1023]. Therefore, Zn2+may play a physiological role in regulating the function of postsynaptic channels and receptors. We characterized the effect of Zn2+ on the functional properties of the β2-adrenergic receptor (β2AR). We found that physiological concentrations of Zn2+ increased agonist affinity and enhanced cAMP accumulation stimulated by submaximal concentrations of the βAR agonist isoproterenol. These results provide evidence that Zn2+ released at nerve terminals may modulate signals generated by the β2AR in vivo.
- The American Society for Pharmacology and Experimental Therapeutics
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Allosteric Modulation of β2-Adrenergic Receptor by Zn2+
