A proposed new nomenclature for 5-HT receptors

Humphrey, P. P. A.; Hartig, Paul; Hoyer, Daniel

doi:10.1016/0165-6147(93)90016-d

Cited by 534 publications

(216 citation statements)

References 16 publications

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“…This inhibitory effect was blocked by pretreatment with methiothepin ( Figure 4). The selective 5-HT2 receptor agonist, m-CPP (Humphrey et al, 1993), was without effect on the pressor responses evoked by sympathetic stimulation (Figure 3). Increases in blood pressure after sympathetic stimulation were significantly potentiated in the 1-phenylbiguanide-perfused group.…”

Section: Resultsmentioning

confidence: 98%

Inhibitory 5‐hydroxytryptamine receptors involved in pressor effects obtained by stimulation of sympathetic outflow from spinal cord in pithed rats

Morán

Velasco

Salvador

et al. 1994

British J Pharmacology

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1 A study was made of the effects of 5-hydroxytryptamine (5-HT) on pressor response induced in vivo by electrical stimulation of the sympathetic outflow from the spinal cord of pithed rats. All animals had been pretreated with atropine. Intravenous infusion of 5-hydroxytryptamine at doses of 10 and 20 jig kg-' min-' reduced the pressor effects obtained by electrical stimulation at intervals of 10 min over the 1 h of infusion. 2 This inhibitory action of 5-HT was depressed by cyproheptadine and methiothepin but was not modified by ketanserin or MDL-72222. By contrast, the inhibitory action of 5-HT was lost in pithed rats that had been pretreated with exogenous noradrenaline.3 The 5-HT, receptor agonist 5-carboxamidotryptamine (5-CT) caused an inhibition of the pressor response, whereas the 5-HT3 receptor agonist, 1-phenylbiguanide, produced a variable but significant increase in the pressor response. The 5-HT2 receptor agonist, m-CPP, did not modify the pressor sympathetic response. 4 Our results suggest that 5-hydroxytryptamine interferes with sympathetic neurotransmission by inhibiting pressor effects as a result of stimulation of the complete sympathetic outflow, and that this inhibition is mainly through a presynaptic 5-HT1 mechanism.

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Section: Resultsmentioning

confidence: 98%

Inhibitory 5‐hydroxytryptamine receptors involved in pressor effects obtained by stimulation of sympathetic outflow from spinal cord in pithed rats

Morán

Velasco

Salvador

et al. 1994

British J Pharmacology

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“…Molecular biological data have confirmed the existence of multiple serotonin receptors, including both ligand-gated receptors (5-HT3) and G protein-coupled receptors (GPRs) [4]. This later class can be split into three classes [5,6], reflecting the second messenger system to which the receptor is coupled: the 5-HT2 subfamily which is coupled to the activation of the phospholipase C, the 5-HTI family which interacts negatively with the adenylyl cyclase, and the family including 5-HT4, 5-HT6 and 5-HT7 receptor subtypes which interacts positively with the adenylyl cyclase.…”

Section: Introductionmentioning

confidence: 99%

The human serotonin 5‐HT2B receptor: Pharmacological link between 5‐HT2 and 5‐HT1D receptors

et al. 1994

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The human serotonin 5-HT2B receptor, isolated from a human liver cDNA library, was transfected in COS-I cells. Its pharmacological profile shows divergence with serotonin 5-HT2B receptors of other species. In particular, although strong correlation is observed between the human and the rat 5-HT2B receptor pharmacology, the correlation is almost as significant for the mouse 5-HT2B and the human 5-HT1D receptor agonists. The major sites of expression of its mRNA are in the human liver and kidney, with detectable expression in lung and heart. Therefore, this human 5-HT2B receptor could account for functions attributed to the peripheral 5-HTI D/5-HT2-1ike receptors, especially in the cardiovascular system. Thus, its detailed original pharmacology is of prime importance for therapeutic drug development.

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“…The present study was designed to characterize the receptors mediating the indirect excitatory response to 5-HT in the guinea-pig isolated trachea by use of selective antagonists of various 5-HT receptor subtypes. The new nomenclature for 5-HT receptors recently proposed (Humphrey et al, 1993) will be used throughout the text.…”

Section: Introductionmentioning

confidence: 99%

A pharmacological analysis of receptors mediating the excitatory response to 5‐hydroxytryptamine in the guinea‐pig isolated trachea

Lucchelli

Santagostino-Barbone

Barbieri

et al. 1994

British J Pharmacology

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1 Experiments were carried out to characterize the receptors mediating the indirect excitatory response to 5-hydroxytryptamine (5-HT) in the guinea-pig isolated trachea. 2 5-HT caused concentration-dependent contractions of tracheal strips, and the resulting concentration-response curve was biphasic in nature. The first phase was obtained with agonist concentrations in the range of 0.01-3 nM and achieved a maximum which was 30% of the total 5-HT response, while the second phase was in the range 1O nM-L M. 3 Atropine (0.1I M) and tetrodotoxin (TTX: 0.3 LM) significantly reduced both phases of the 5-HT curve. Morphine (10 gIM), which can act to inhibit neuronal acetylcholine release, abolished the first phase and reduced the second phase. This suggests that the first phase is mainly neurogenic (cholinergic) in nature, while the second phase is in part neurogenic and in part due to direct activation of the effector 6 Our results suggest that neural 5-HT2A and, to a lesser extent, 5-HT3 receptor subtypes mediate the first phase of the 5-HT curve in the guinea-pig trachea. The second phase is mediated by 5-HT2A receptors, which are probably located at both the neural and muscular level. No evidence for the participation of 5-HT, receptors in the 5-HT response has been obtained.

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A proposed new nomenclature for 5-HT receptors

Cited by 534 publications

References 16 publications

Inhibitory 5‐hydroxytryptamine receptors involved in pressor effects obtained by stimulation of sympathetic outflow from spinal cord in pithed rats

Inhibitory 5‐hydroxytryptamine receptors involved in pressor effects obtained by stimulation of sympathetic outflow from spinal cord in pithed rats

The human serotonin 5‐HT2B receptor: Pharmacological link between 5‐HT2 and 5‐HT1D receptors

A pharmacological analysis of receptors mediating the excitatory response to 5‐hydroxytryptamine in the guinea‐pig isolated trachea

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