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Glaxo Wellcome
Pharmacology Guide

Neurotransmitters and other chemical signalling agents

5-HYDROXYTRYPTAMINE (5HT; serotonin)
Precursors: Tryptophan (a) -> 5-hydroxytryptophan
(b) -> 5HT
Synthesising enzymes: (a) Tryptophan hydroxylase,
(b) 5HTP decarboxylase
Metabolising enzymes: Monoamine oxidase (MAO)
Metabolite: 5HIAA
Receptor subtypes Agonists Antagonists Second messenger
5HT(1A) 8-OH-DPAT Way 100135,
SDZ 216-525
(-ve) cAMP
5HT(1B) CP 93129 Cyanopindolol (-ve) cAMP
5HT(1C) now re-classified as 5HT(2C)
5HT(1D) 5CT, sumatriptan Methiothepin,
methysergide
(-ve) cAMP
5HT(1D-alpha) MB
5HT(1DB) MB (human homologue of the rodent 5HT1B receptor)
5HT(1E-alpha) MB (-ve) cAMP
5HT(1EB) MB (-ve) cAMP
5HT(1F) MB (-ve) cAMP
5HT(2A)
(old 5HT(2))
DOI Ketanserin PI
5HT(2B)
(rat fundus)
DOI Ketanserin PI
5HT(2C)
(old 5HT1C)
mCPP Mesulergine PI
5HT(3) 2-Me-5HT Ondansetron,
granisetron
(+ve)g(cation)
5HT(4) 5MeOTrp,
cisapride
GR 113808 (+ve)cAMP
5HT(5) MB (binds bufotenine)

NB: (+ve) indicates increase; (-ve) indicates decrease.

Reviews
Peroutka, S. (1992) Neuropharmacol. 31, 609-613.
Zifa, E. and Fillion, G. (1992) Pharmacol. Revs. 44, 401-458.
Harrington, M.A., Zhong, P., Garlow, S.J. and Ciaranello, R.D. (1992) J. Clin. Psychiatr. 53 (Oct. suppl.) 8-27.


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