Serotonin receptors classification

As an example, using the NC-IUPHAR classification scheme, the human 5-HT3 serotonin receptor would be identified with an RC of 1.1 5HT 1 5HT3 HUMAN 00 and the human GluR3 receptor would have an RC of 1.2 GLU 3 GLUR3 HUMAN 00. In comparison, the respective codes under the TC system would be 1. A.9.2.1 and 1. A. 10.1.4. 

Study and classification of serotonin receptors has resulted in the design and synthesis of highly selective medicines such as Sumatriptan, for the treatment of migraine, Ondansetron for the suppression of the nausea and vomiting caused by cancer chemotherapy and radiotherapy, and Alosetron for treatment of irritable bowel syndrome. 

Based on one current classification system, fourteen serotonin receptor subtypes have been described for the peripheral and central actions of 5-HT. A brief summary is provided in Table 18.1 but the reader is referred to the appropriate pharmacological literature for details. Only the 5-HT3 receptor is a ligand-gated ion channel the remaining subfamilies are G-protein coupled receptors. It is also worth noting that the situation is more complicated based on the presence of additional receptors which... 

Hoyer D, Clarke DE, Fozard JR et al (1994) International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev 46 157-204... 

Hoyer D, Qarke DE, Eozard JR, et al. International union of pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol Rev 1994 46 157-203. 

Dopamine induces biochemical and physiological effects in the mammalian neostriatum. The occurrence of a D-l dopamine receptor (in the classification scheme of Kebabian and Caine) accounts for the ability of dopamine to enhance cyclic AMP formation. The occurrence of a D-2 dopamine receptor accounts for the ability of dopamine to inhibit cyclic AMP formation brought about by stimulation of a D-l dopamine receptor. Dopamine receptors mediate the regulation of (1) the release or turnover of acetylcholine (postsynaptic dopamine receptor) and (2) the release or turnover of dopar mine (presynaptic autoreceptor). Both receptors can be classified as D-2 dopamine receptors. Indications for the occurrence of dopamine receptors affecting the release or turnover of GABA, glutamate, serotonin and several neuropeptides are evaluated. 

No recognised classification system exists for atypical antipsychotics.Tentative terms based on receptor binding profiles have been applied to certain drug groupings.for example broad spectrum atypicals for clozapine, olanzapine and quetiapine. whilst risperidone and ziprasidone have been described as high affinity serotonin-dopamine antagonists . 

A critical update on therapeutic potential. Trends Pharmacol. Sci.. 14.265-270. Hoyer, D. et al. (1994) International Union of Pharmacology classification of receptors for 5-hydro) tryptamine (Serotonin). Pharmacol. Rev. 46.157-203. Alexander. S.PH. etal. (1998) Receptors and ion channel nomenclature supplement. Ninth Edition. Trends Pharmacol. ScL.Suppl.. 19.1-98. 

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