Article
Constitutive precoupling to G(i) and increased agonist potency in the alpha(2B)-adrenoceptor.
Biochemical and biophysical research communications - 11 Jul 2003
Ge Huifang, Scheinin Mika, Kallio Jaana
Abstract excerpt
The human alpha(2B)-adrenoceptor (alpha(2B)-AR) was mutated by substituting the D(3.49) aspartate in position 109 with an alanine (alpha(2B)-D109A) in the conserved DRY sequence at the cytoplasmic face of TM3. We studied the effects of the mutation on agonist binding and on receptor activation in CHO cells, including possible inverse agonism monitored by measuring intracellular Ca(2+) concentrations...
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