The 1-adrenergic receptor ( 1AR) is known to be localized to synapses and to modulate synaptic plasticity in many brain regions, but the molecular mechanisms determining 1AR subcellular localization are not fully understood. Using overlay and pull-down techniques, we found that the 1AR carboxyl terminus associates with MAGI-2 (membrane-associated guanylate kinase inverted-2), a protein also kno...

and 2–adrenergic receptors are known to exhibit substantial cross-talk and mutual regulation in tissues where they are expressed together. We have found that the 1-adrenergic receptor ( 1AR) and 2A-adrenergic receptor ( 2AAR) heterodimerize when coexpressed in cells. Immunoprecipitation studies with differentially tagged 1AR and 2AAR expressed in HEK-293 cells revealed robust co-immunoprecipita...

Zhang F, Steinberg SF. S49G and R389G polymorphisms of the 1adrenergic receptor influence signaling via the cAMP-PKA and ERK pathways. Physiol Genomics 45: 1186–1192, 2013. First published October 22, 2013; doi:10.1152/physiolgenomics.00087.2013.—Two functionally important 1-adrenergic receptor ( 1AR) polymorphisms have been identified. The R389G polymorphism influences coupling to the Gs-cAMP ...

The androgen receptor (AR) mediates the developmental, physiologic, and pathologic effects of androgens including 5α-dihydrotestosterone (DHT). However, the mechanisms whereby AR regulates growth suppression and differentiation of luminal epithelial cells in the prostate gland and proliferation of malignant versions of these cells are not well understood, though they are central to prostate dev...

Intermolecular interactions between members of both similar and divergent G protein–coupled receptor subfamilies have been shown in various experimental systems. Here, we demonstrate heterodimerization of predominant -adrenergic receptor ( AR) subtypes expressed in the heart, 1AR, and 2AR, and its physiological relevance. In intact adult-mouse cardiac myocytes lacking native 1AR and 2AR, coexpr...

Gene Common Name: 1 Adrenergic Receptor ( 1AR) Introductory Information: The 1-adrenergic receptor ( 1AR) is a G-protein-coupled receptor that was first characterized by its pharmacological specificity. The gene for this receptor (ADRB1) was cloned in 1987 from a placental cDNA library and subsequently mapped to chromosome 10q24-q26 (10q25.3). The intronless gene consists of 1,714 bp and codes ...

The sympathetic nervous system modulates cardiac contractility and rate by activating -adrenergic receptors ( AR) expressed on cardiac myocytes and specialized cells in the sinoatrial node and the conduction system. Recent clinical studies have suggested that -adrenergic receptors also play a role in cardiac remodeling that occurs in the pathogenesis of cardiomyopathy. Both 1 and 2 adrenergic r...

adrenoceptor ( AR) signaling is finely regulated to mediate the sympathetic nervous system control of cardiovascular function. In neonatal cardiac myocytes, 1AR activates the conventional Gs cAMP pathway, whereas 2AR sequentially activates both the Gs and Gi pathways to regulate the myocyte contraction rate. Here, we show that phosphodiesterase 4D (PDE4D) selectively impacts signaling by 2AR in...

The title compound, C19H22N2O3, {systematic name (1aR,4E,7aS,8E,10aS,10bR)-1a,5-dimethyl-8-[(pyrimidin-5-yl)-methylid-ene]-2,3,6,7,7a,8,10a,10b-octa-hydro-oxireno[2',3':9,10]cyclo-deca-[1,2-b]furan-9(1aH)-one} was obtained from the reaction of parthenolide [systematic name (1aR,7aS,10aS,10bR,E)-1a,5-dimethyl-8-methyl-ene-2,3,6,7,7a,8,10a,10b-octa-hydro-oxireno[2',3':9,10]cyclodeca-[1,2-b]furan-...