Modelling of Drug–Receptor Interactions: Stereoselectivity of 5-Hydroxytryptamine and Dopamine Receptors in the Brain

作者: ULI HACKSELL , ANETTE M. JOHANSSON , ANDERS KARLÉN , KRISTINA LUTHMAN , CHARLOTTA MELLIN

DOI: 10.1016/B978-0-12-136670-4.50011-4

关键词: Metabotropic receptorClass C GPCRRhodopsin-like receptors5-HT2 receptorD1-like receptorNeurotransmitter receptorBiologyBiochemistryD2-like receptorDrug receptor

摘要: Publisher Summary Neurotransmitters such as dopamine (DA) and serotonin (5-HT) are achiral fairly flexible molecules that act on a variety of biological targets. DA stimulates D1-receptors pre- postsynaptic D2-receptors 5-HT interacts with at least seven subtypes 5-HT-receptors. These neurotransmitters nonselective, is, they interact also other neurotransmitter receptors, drugs pharmacological profiles not useful therapeutic agents. This chapter discusses the nonselective actions surprising when considering many their receptors belong to G-protein coupled receptor super family. There considerable amino acid homologies between in this class. The putative transmembrane regions, which appear be common all bound could responsible for ligand binding, have very similar sequences. Also, various transmit chemical message from by mechanisms. It is well-established strategy among medicinal chemists introduce structural modifications order obtain desired selectivity.

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