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Beschreibung

Human D3 Receptor, Dopamine is a catecholamine neurotransmitter that functions in the CNS to control locomotor, cognitive, emotional and neurendocrine processes, and in the periphery to modulate cardiovascular, renal and gastrointestinal processes. The biological activities of dopamine are mediated by a family of five GPCRs. The D1 and D5 subtypes couple to Gs to increase intracellular cAMP, whereas the D2, D3 and D4 subtypes couple to Gi to reduce cAMP (Missale et al., 1998). The dopamine D3 receptor is expressed in phylogenetically older regions of the brain, suggesting that it plays a role in cognitive and emotional functions. It has been the target of potential drugs for psychotic disorders and Parkinson's disease. Chemicon's D3 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 D3 interactions and its ligands. The membrane preparations exhibit a Kd of 0.1 nM for [125I]-Iodospiperone. With 5.0ug/well D3 membrane prep and 0.1 nM [125I]-Iodospiperone, a greater than 4-fold signal-to-background ratio was obtained.

Strukturformel

SAF-HTS103M

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