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5-HT1B 5-HT1D & 5-HT2

Key message: 5-HT1B, 5-HT1D and 5-HT2C receptors contribute to the profiles of CNS agents. 5-HT2B antagonism is a new target for modulating dopaminergic function. 

  • 5-HT1B and 5-HT1D receptors exhibit distinct pharmacology and marked constitutive activity in vitro.
  • 5-HT2C receptor antagonism influences monomine neurotransmitter release and may underlie the therapeutic activity of the antidepressant, agomelatine (Valdoxan ®).
  • Central 5-HT2B receptors have been little characterised but influence dopamine release in nucleus accumbens.
# Article Title
1 S32212: a novel 5-HT2C receptor inverse agonist / alpha2 adrenoceptor antagonist and potential antidepressant. 1. A mechanistic characterization.
2 Inverse agonists and serotonergic transmission: from recombinant, human serotonin 5-HT1B receptors to G-protein coupling and function in corticolimbic structures in vivo. (REVIEW) PDF
3 h5-HT1B receptor-mediated constitutive Galphai3-protein activation in stably transfected Chinese hamster ovary cells: an antibody capture assay reveals protean efficacy of 5-HT. PDF
4 Constitutive activity at serotonin 5-HT1D receptors: detection by homologous GTPgammaS versus [35S]-GTPgammaS binding isotherms.
5 Differential activation of Gq/11 and Gi3 proteins at 5-hydroxytryptamine2C receptors revealed by antibody capture assays: influence of receptor reserve and relationship to agonist-directed trafficking. PDF
6 The novel melatonin agonist agomelatine (S20098) is an antagonist at 5-hydroxytryptamine2C receptors, blockade of which enhances the activity of frontocortical dopaminergic and adrenergic pathways. PDF
7 Serotonin(2C) receptors tonically suppress the activity of mesocortical dopaminergic and adrenergic, but not serotonergic, pathways: a combined dialysis and electrophysiological analysis in the rat.
8 Characterization of phospholipase C activity at h5-HT2C compared with h5-HT2B receptors: influence of novel ligands upon membrane-bound levels of [3H]phosphatidylinositols.
9 Agonist-directed trafficking of signalling at serotonin 5-HT2A, 5-HT2B and 5-HT2C-VSV receptors mediated Gq/11 activation and calcium mobilisation in CHO cells.
10 The central serotonin(2B) receptor: a new pharmacological target to modulate the mesoaccumbens dopaminergic pathway activity.
11 Inverse agonism and constitutive activity as functional correlates of serotonin h5-HT1B receptor/G-protein stoichiometry. PDF
12 An innovative method for rapid characterisation of phospholipase C activity: SB242,084 competitively antagonises 5-HT2C receptor-mediated [3H]phosphatidylinositol depletion.
13 The "selective" dopamine D1 receptor antagonist, SCH23390, is a potent and high efficacy agonist at cloned human serotonin2C receptors.
14 Binding profile of the novel 5-HT1B/1D receptor antagonist, [3H]GR 125,743, in guinea-pig brain: a comparison with [3H]5-carboxamidotryptamine.
15 Specific labelling of serotonin 5-HT1B receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization.
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