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 alpha2 adrenergic receptor subfamily members, consisting of alpha2A, alpha2B, and alpha2C, couple primarily to Gi to inhibit cAMP production, and play an important role in regulation of cardiovascular and CNS function. Experiments with alpha2A-selective agonists and mice lacking alpha2A demonstrate that activation of alpha2A results in hypotension, sedation, analgesia, and hypothermia (Kable et al., 2000). Chemicon's alpha2A 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 at alpha2A. The membrane preparations exhibit a Kd of 5.4 nM for [3H]-MK-912. With 5 nM [3H]-MK-912, 5 µg/well alpha2A Membrane Prep typically yields greater than 20-fold signal-to-background ratio.
Application: Radioligand binding assay and GTPgammaS binding.
Biochem Physiol Actions: Target Sub-Family: Adrenergic
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