Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine

Bradley, Philip; Engel, G.; Feniuk, W.; Fozard, John R.; Humphrey, P. P. A.; Middlemiss, Derek N.; Mylecharane, Ewan J.; Richardson, B. P.; Saxena, Pramod R.

doi:10.1016/0028-3908(86)90207-8

Cited by 1,223 publications

(497 citation statements)

References 79 publications

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“…Nevertheless, pharmacological characterization of 5-HT receptors was instrumental in the design of the antimigraine drug sumatriptan (Humphrey et al, 1988;Saxena & Ferrari, 1992), an agonist at a novel, but heterogeneous group of 5-HT receptors, then called`5-HT 1 -like' (Bradley et al, 1986). The term`5-HT 1 -like' has since become redundant , because this group has been shown to comprise of receptors where sumatriptan has either a high (5-HT 1B , 5-HT 1D and 5-ht 1F ) or low (5-HT 7 ) a nity (Peroutka & McCarthy, 1989;Waeber et al, 1990;Hoyer et al, 1994).…”

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confidence: 99%

Molecular cloning, sequence analysis and pharmacological properties of the porcine 5‐HT_1D receptor

Bhalla

Sharma

Wurch

et al. 2000

British J Pharmacology

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confidence: 99%

Molecular cloning, sequence analysis and pharmacological properties of the porcine 5‐HT_1D receptor

Bhalla

Sharma

Wurch

et al. 2000

British J Pharmacology

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“…The dopamine D2-receptor antagonist domperidone used in conventional antiemetic therapy has no effect against chemotherapeutic agents-induced emesis (3). A high dose of metoclopram ide was reported to antagonize the serotonin (5-HT) M receptor (4) which was subsequently redesignated as the 5-HT3 receptor (5). Metoclopramide has antiemetic effects against chemotherapeutic agent-induced emesis; however, it can produce extrapyramidal side-effects which have been attributed to its dopamine receptor blocking activity (6).…”

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The Effects of Orally Administered Y-25130, a Selective Serotonin3-Receptor Antagonist, on Chemotherapeutic Agent-Induced Emesis

Haga¹,

Inaba²,

Shoji³

et al. 1993

Japanese Journal of Pharmacology

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ABSTRACT-The antiemetic effects of orally administered Y-25130, a potent and selective 5-HT3-receptor antagonist, were compared with those of ondansetron, granisetron, metoclopramide and domperidone. Y-25130 (0.1-1.0 mg/kg) dose-dependently prolonged the latency to the first vomiting and decreased the number of vomitings induced by cisplatin in dogs. The antiemetic effect of Y-25130 against cisplatin-in duced vomiting was more potent than that of metoclopramide and ondansetron, but it showed little differ ence from that of granisetron. The emesis induced by the combined treatment of doxorubicin and cyclophosphamide was also inhibited by Y-25130 (0.1-1 mg/kg) in ferrets. The antiemetic effect of Y-25130 was more potent than that of metoclopramide, almost the same as that of granisetron and less potent than that of ondansetron. Because of a notable difference of potency ranking between Y-25130 and ondansetron in these two tests, a third test was performed to evaluate the inhibitory effect of Y-25130 in ferrets on cisplatin-induced emesis in comparison with that of ondansetron. The antiemetic effect of Y-25130 on cisplatin-induced emesis in ferrets was very similar to that of ondansetron. Domperidone did not inhibit these cytotoxic agents-induced emeses. These results suggest that Y-25130 is an orally active antiemetic com pound against cisplatin and doxorubicin/cyclophosphamide-induced emeses; and its the antiemetic potency is similar to those of granisetron and ondansetron, but superior to those of metoclopramide and domperidone.

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“…In contrast, even high doses of the dopamine antagonists, domperidone (Motilium; Janssen Pharmaceuticals) or alizapride, have little or no ability to prevent cis-platininduced emesis (Tonato et al, 1985;Saller & Hellenbrecht, 1985). Mechanisms other than dopamine receptor antagonism have therefore been implicated in this antiemetic action of metoclopramide (McRitchie et al, 1984).Secondly, metoclopramide is an antagonist of 5-hydroxytryptamine (5-HT) acting on 5-HT3 receptors (previously known as 5-HT M-receptors; see Bradley et al, 1986 for definition of this receptor) located in the peripheral nervous system (Fozard, 1984a); the effective concentrations of metoclopramide are higher than those required to antagonise dopamine receptors or to stimulate gut motility (Sanger, 1984). We subsequently suggested that such high doses of metoclopramide may prevent cis-platin-induced emesis by means of antagonising 5-HT3 receptors .…”

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confidence: 99%

“…Secondly, metoclopramide is an antagonist of 5-hydroxytryptamine (5-HT) acting on 5-HT3 receptors (previously known as 5-HT M-receptors; see Bradley et al, 1986 for definition of this receptor) located in the peripheral nervous system (Fozard, 1984a); the effective concentrations of metoclopramide are higher than those required to antagonise dopamine receptors or to stimulate gut motility (Sanger, 1984). We subsequently suggested that such high doses of metoclopramide may prevent cis-platin-induced emesis by means of antagonising 5-HT3 receptors .…”

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Evidence that 5-hydroxytryptamine3 receptors mediate cytotoxic drug and radiation-evoked emesis

Miner

Sanger²,

Turner³

1987

Br J Cancer

113

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Summary The involvement of 5-hydroxytryptamine (5-HT) 5-HT3 receptors in the mechanisms of severe emesis evoked by cytotoxic drugs or by total body irradiation have been studied in ferrets. Anti-emetic compounds tested were domperidone (a dopamine antagonist), metoclopramide (a gastric motility stimulant and dopamine antagonist at conventional doses, a 5-HT3 receptor antagonist at higher doses) and BRL 24924 (a potent gastric motility stimulant and a 5-HT3 receptor antagonist). Domperidone or metoclopramide prevented apomorphine-evoked emesis, whereas BRL 24924 did not. Similar doses of domperidone did not prevent emesis evoked by cis-platin or by total body irradiation, whereas metoclopramide or BRL 24924 greatly reduced or prevented these types of emesis. Metoclopramide and BRL 24924 also prevented emesis evoked by a combination of doxorubicin and cyclophosphamide. These results are discussed in terms of a fundamental role for 5-HT3 receptors in the mechanisms mediating severely emetogenic cancer treatment therapies.There have recently been two important advances relating to the improvement of anti-emetic treatment given to patients undergoing anti-cancer therapies. Firstly, it was found that, unlike conventional doses of metoclopramide (Maxolon; Beecham Pharmaceuticals) which antagonise dopamine receptors and stimulate gastric motility, high doses of the drug greatly reduced cis-platin-evoked emesis (Gralla et al., 1981). In contrast, even high doses of the dopamine antagonists, domperidone (Motilium; Janssen Pharmaceuticals) or alizapride, have little or no ability to prevent cis-platininduced emesis (Tonato et al., 1985;Saller & Hellenbrecht, 1985). Mechanisms other than dopamine receptor antagonism have therefore been implicated in this antiemetic action of metoclopramide (McRitchie et al., 1984).Secondly, metoclopramide is an antagonist of 5-hydroxytryptamine (5-HT) acting on 5-HT3 receptors (previously known as 5-HT M-receptors; see Bradley et al., 1986 for definition of this receptor) located in the peripheral nervous system (Fozard, 1984a); the effective concentrations of metoclopramide are higher than those required to antagonise dopamine receptors or to stimulate gut motility (Sanger, 1984). We subsequently suggested that such high doses of metoclopramide may prevent cis-platin-induced emesis by means of antagonising 5-HT3 receptors .The involvement of 5-HT3 receptors in the mechanisms of emesis have now been further investigated using chemo-and radio-emetic stimuli in the ferret. The ferret has previously been shown to be suitable for studying emesis evoked by cisplatin (Florczyk et al., 1982;), a combination of doxorubicin and cyclophosphamide (Schurig et al., 1984) or by whole-body irradiation (Andrews et al., 1986;Gylys & Gidda, 1986

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Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine

Cited by 1,223 publications

References 79 publications

Molecular cloning, sequence analysis and pharmacological properties of the porcine 5‐HT_1D receptor

Molecular cloning, sequence analysis and pharmacological properties of the porcine 5‐HT_1D receptor

The Effects of Orally Administered Y-25130, a Selective Serotonin3-Receptor Antagonist, on Chemotherapeutic Agent-Induced Emesis

Evidence that 5-hydroxytryptamine3 receptors mediate cytotoxic drug and radiation-evoked emesis

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Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine

Cited by 1,223 publications

References 79 publications

Molecular cloning, sequence analysis and pharmacological properties of the porcine 5‐HT1D receptor

Molecular cloning, sequence analysis and pharmacological properties of the porcine 5‐HT1D receptor

The Effects of Orally Administered Y-25130, a Selective Serotonin3-Receptor Antagonist, on Chemotherapeutic Agent-Induced Emesis

Evidence that 5-hydroxytryptamine3 receptors mediate cytotoxic drug and radiation-evoked emesis

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Molecular cloning, sequence analysis and pharmacological properties of the porcine 5‐HT_1D receptor

Molecular cloning, sequence analysis and pharmacological properties of the porcine 5‐HT_1D receptor