Literature DB >> 1449511

Conversion of the human 5-HT1D beta serotonin receptor to the rat 5-HT1B ligand-binding phenotype by Thr355Asn site directed mutagenesis.

M A Metcalf1, R W McGuffin, M W Hamblin.   

Abstract

The human 5-HT1D beta serotonin receptor and its rat homolog (also called the 5-HT1B receptor) share 93% amino acid identity, yet display markedly different pharmacological specificities. Comparison of deduced amino acid sequences among these and other recently cloned receptors suggested that this phenotypic difference might be attributable to a single human threonine355/rat asparagine351 amino acid difference in the putative seventh membrane spanning regions. We now report that Thr355Asn mutagenesis of the human 5-HT1D beta receptor alters the binding characteristics of the recombinant receptor in [3H]5-HT binding assays to a profile very similar to that of the rat 5-HT1B binding site. These results confirm that this single amino acid difference is responsible for the majority of the known pharmacological discrepancies between human and rat observed for 5-HT1D beta (5-HT1B) receptors.

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Year:  1992        PMID： 1449511     DOI： 10.1016/0006-2952(92)90092-w

Source DB:  PubMed          Journal:  Biochem Pharmacol        ISSN： 0006-2952            Impact factor:   5.858


  9 in total

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Journal:  Br J Pharmacol       Date:  2001-07       Impact factor: 8.739

Review 3.  Structure and function of serotonin G protein-coupled receptors.

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4.  Pharmacology of cloned human 5-HT1D receptor-mediated functional responses in stably transfected rat C6-glial cell lines: further evidence differentiating human 5-HT1D and 5-HT1B receptors.

Authors:  P J Pauwels; C Palmier; T Wurch; F C Colpaert
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Review 5.  Regulation of dorsal raphe nucleus function by serotonin autoreceptors: a behavioral perspective.

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6.  Serotonin receptors contribute to dopamine depression of lateral inhibition in the nucleus accumbens.

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7.  Binding properties of the naturally occurring human 5-HT1A receptor variant with the Ile28Val substitution in the extracellular domain.

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8.  Two amino acids, located in transmembrane domains VI and VII, determine the selectivity of the peptide agonist SMS 201-995 for the SSTR2 somatostatin receptor.

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Review 9.  The 5-HT1B receptor - a potential target for antidepressant treatment.

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Journal:  Psychopharmacology (Berl)       Date:  2018-03-15       Impact factor: 4.530
  9 in total

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