TY - JOUR T1 - Allosteric Modulation of β<sub>2</sub>-Adrenergic Receptor by Zn<sup>2+</sup> JF - Molecular Pharmacology JO - Mol Pharmacol SP - 65 LP - 72 DO - 10.1124/mol.61.1.65 VL - 61 IS - 1 AU - Gayathri Swaminath AU - Jacqueline Steenhuis AU - Brian Kobilka AU - Tae Weon Lee Y1 - 2002/01/01 UR - http://molpharm.aspetjournals.org/content/61/1/65.abstract N2 - 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. ER -