ChemiSCREEN Membrane Preparation Recombinant Human alpha1B Adrenergic Receptor

Descrição detalhada : 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-adrenoceptors (Bylund et al., 1994). The three members of the alpha1 subclass of adrenoceptors, alpha1A, alpha1B and alpha1D, couple to Gq, and promote contraction of vascular and urinary tract smooth muscle, relaxation of intestinal smooth muscle, increased contractile force in the heart, and glycogenolysis and gluconeogenesis in the liver. The different subtypes have overlapping distributions and variably contribute to these effects depending on species and tissue. Overexpression of a constitutively active alpha1B mutant in the heart of transgenic mice resulted in cardiac hypertrophy with increased heart weight/body weight ratios. Analysis of alpha1B knock out mice has provided evidence that alpha1B is a mediator of blood pressure and aortic contractile responses induced by alpha1 agonists (Milano et al., 1994). The locomotor and rewarding effects of pysochostimulants and opiates were suppressed in mice lacking alpha1B-adrenergic receptors (Drouin et al. 2002). Millipore's alpha1B 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 agonists and antagonists of alpha1B. The membrane preparations exhibit a Kd of 0.8 nM for [3H]-Prazosin. With 1 nM [3H]-Prazosin, 5mug/well alpha1B Membrane Prep typically yields greater than 5-fold signal-to-background ratio., Full-length human ADRA1B cDNA encoding alpha1B adrenergic
Armazenamento : -80°C
Embalagem : 1X1EA