Title: Modelling of Drug–Receptor Interactions: Stereoselectivity of 5-Hydroxytryptamine and Dopamine Receptors in the Brain
Abstract: Neurotransmitters such as dopamine (DA) and serotonin (5-HT) are achiral and fairly flexible molecules that act on a variety of biological targets. DA stimulates D1-receptors and pre- and postsynaptic D2-receptors and 5-HT interacts with at least seven subtypes of 5-HT-receptors. These neurotransmitters are nonselective, that is, they interact also with other neurotransmitter receptors, and drugs with such pharmacological profiles are not useful as therapeutic agents. This chapter discusses that the nonselective actions of the neurotransmitters are not surprising when considering that many of their receptors belong to the G-protein coupled receptor super family. There are considerable amino acid homologies between receptors in this class. The seven putative transmembrane regions, which appear to be common to all G-protein bound receptors and could be responsible for ligand binding, have very similar amino acid sequences. Also, the various receptors appear to transmit the chemical message from the neurotransmitter by similar mechanisms. It is a well-established strategy among medicinal chemists to introduce structural modifications in neurotransmitters in order to obtain drugs with the desired pharmacological selectivity.
Publication Year: 1990
Publication Date: 1990-01-01
Language: en
Type: book-chapter
Indexed In: ['crossref']
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Cited By Count: 2
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