Clinical evaluation of 5-HT3 receptor antagonists as anti-emetics
Article Abstract:
Ondansetron and granisetron are two 5-HT3-selective receptor antagonists that effectively inhibit the occurrence of emesis in patients undergoing cancer treatment. Clinical trials show that no adverse reactions have been observed with the use of the two drugs. However, several test patients have experienced mild headaches. The lack of side-effects can be attributed to the inability of both drugs to interact with dopamine D2 receptors. Moreover, the anti-emetic effects of ondansetron and granisetron cannot be directly measured using plasma concentrations. Also, increasing the drug dose does not lead to better anti-emetic effects.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1991
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The 5-HT(sub 4) receptor: a place in the sun
Article Abstract:
The serotonin receptor, 5-hydroxytryptamine4 (5-HT4), shows varied tissue localizations and mechanisms of action. 5-HT4 receptors can be found in the central nervous system, gastrointestinal tract, heart and endocrine system where they promote cholinergic effects with concomitant release of transmitters. Benzamides and benzimidazolones are two selective agonists of 5-HT4 receptors while ICS205930, DAU6215, DAU6285 and SDZ205557 are interacting antagonists. The role of 5-HT4 receptors is yet unknown but its presence in the brain and gastrointestinal tract marks possible physiological functions.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1992
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A subfamily of 5-HT(sub 1D) receptor genes
Article Abstract:
The subfamily of 5-hydroxytryptamine(sub 1D) (5-HT1D) receptor system exhibits similarities and differences among related subgroup elements. Alpha 5-HT1D, beta 5-HT1D and 5-HT1B are three clones of the 5-HT1D subgroup which feature different functional mechanisms and pharmacological interactions. Alteration of amino acid sequencing of hydroxytryptamine receptor homologues can greatly affect pharmacological binding similarity. The present inability to distinguish the action of alpha and beta 5-HT1D prevents determination of their respective roles in neuropharmacology.
Publication Name: Trends in Pharmacological Sciences
Subject: Pharmaceuticals and cosmetics industries
ISSN: 0165-6147
Year: 1992
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