Molecular cloning and pharmacological characterization of serotonin 5-HT(3A) receptor subtype in dog

European Journal of Pharmacology
Thomas N JensenBjarke Ebert

Abstract

In order to establish if the canine 5-hydroxytryptamine type 3A (5-HT(3A)) receptors share the pharmacological profile with human 5-HT(3A) receptors, we cloned and performed a molecular pharmacological characterization of the canine 5-HT(3A) receptor. The 5-HT(3A) cDNA was cloned from canine brain by polymerase chain reaction amplification. It encodes a 483 amino acid peptide that exhibits from 80% (mice) to 90% (ferrets) identity to other sequenced mammalian 5-HT(3A) receptors. The receptor agonists 5-hydroxytryptamine (5-HT) and meta-chlorophenylbiguanide (mCPBG) showed little differences between the two species, whereas 2-methyl-5-hydroxytryptamine (2-Me-5-HT) was ten times weaker at canine receptors than at human receptors. The potencies at the canine 5-HT(3) receptors were 9.9 microM (5-HT), 79 microM (2-Me-5-HT) and 0.8 microM (mCPBG). The selective, competitive receptor antagonist ondansetron was ten times more potent at human receptors compared to canine receptors (K(b)=0.9 nM), while (+)-tubocurarine was 1000-fold more potent at canine receptors (K(b)=3.0 nM) than at human receptors. Examination of the presumed ligand binding extracellular domain revealed one residue, where the canine receptor differs from all previous...Continue Reading

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Citations

Mar 2, 2011·Pharmacology & Therapeutics·Tina K Machu
Sep 2, 2008·Neuropharmacology·Nicholas M BarnesJohn A Peters
Aug 28, 2007·Pharmazie in unserer Zeit·André RexHeidrun Fink
Feb 18, 2014·British Journal of Pharmacology·Stephen P H AlexanderUNKNOWN CGTP Collaborators
Oct 4, 2014·The Journal of Pharmacology and Experimental Therapeutics·Martin Lochner, Andrew J Thompson
Feb 17, 2017·Frontiers in Synaptic Neuroscience·Claire N J MeunierPhilippe M Fossier
Apr 20, 2010·Respiratory Physiology & Neurobiology·Michelle E BartmanStephen M Johnson

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