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Description

Full-length human ADRB1 cDNA encoding the beta1 adrenoceptor, The endogenous catecholamines epinephrine and norepinephrine have profound effects on smooth muscle activity, cardiac function, carbohydrate and fat metabolism, hormone secretion, neurotransmitter release, and central nervous system actions. These activities are mediated by GPCRs belonging to two subfamilies, the alpha- and beta-adrenergic receptors (Bylund et al., 1994). The three members of the beta-adrenergic receptor family, beta1, beta2 and beta3, couple to Gs to increase cAMP upon activation. In the heart, the beta1 receptor constitutes 70-80% of the beta-adrenergic receptors. Activation of cardiac beta-adrenergic receptors acutely increases heart rate, cardiac output, and cardiac automaticity, and chronically increases cardiac myocyte apoptosis. In failing hearts, the beta1 subtype is downregulated and desensitized, probably as a result of increased catecholamine levels. As a result, beta-adrenergic receptor antagonists (beta blockers) are effective in the treatment of congestive heart failure and arrhythmia (Lohse et al., 2003). Millipore's beta1 adrenoceptor membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression, thus, they are ideal HTS tools for screening of antagonists of beta1 adrenoceptor interactions. The membrane preparations exhibit a Kd of 2.6 nM for [125I]-(-) Iodocyanopindolol (ICYP). With 5 µ,g/well beta1 Adrenoceptor Membrane Prep and 0.25 nM [125I]-(-)ICYP, a greater than 15-fold signal-to-background ratio was obtained.