WordNet

(biochemistry) a drug that can combine with a receptor on a cell to produce a physiological reaction
a muscle that contracts while another relaxes; "when bending the elbow the biceps are the agonist"
someone involved in a contest or battle (as in an agon)
a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response
a neurotransmitter involved in e.g. sleep and depression and memory (同)5-hydroxytryptamine

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=sense organ / 受信装置

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/06 22:14:05」(JST)

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Serotonin

A serotonin receptor agonist is a compound that activates serotonin receptors, in a manner similar to serotonin.

Non-selective agonists: Psilocin and DMT are serotonin analogs found in certain plants or mushrooms. These compounds act on a variety of serotonin receptor types.

5-HT_1A agonists

Azapirones such as buspirone, gepirone, and tandospirone are 5-HT_1A agonists marketed primarily as anxiolytics, but also recently as antidepressants.

5-HT_1B agonists

Triptans such as sumatriptan, rizatriptan, and naratriptan, are 5-HT_1B receptor agonists that are used to abort migraine and cluster headache attacks.

5-HT_1D agonists

In addition to being 5-HT_1B agonists, triptans are also agonists at the 5-HT_1D receptor, which contributes to their antimigraine effect caused by vasoconstriction of blood vessels in the brain.

5-HT_1F agonists

LY-334,370 was a selective 5-HT_1F agonist that was being developed by Eli Lilly and Company for the treatment of migraine and cluster headaches. Development is slow however due to toxicity detected in animal test subjects.

5-HT_2A agonists

Psychedelic drugs like LSD, mescaline, and 2C-B, act as 5-HT_2A agonists. Their action at this receptor is responsible for their "psychedelic" effects. Some of these drugs, act as agonists for other 5HT receptor subtypes. Not all 5-HT_2A agonists are psychoactive.^[1]

5-HT_2B agonists

Drugs that act as agonists on this receptor are implicated in the progression of cardiac fibrosis.^[2] Fenfluramine, Pergolide and Cabergoline have been withdrawn from some markets for this reason.^[3] Some psychedelic drugs, including LSD and Psilocin, have been shown to activate this receptor directly.^[4] MDMA has been reported to be both a potent direct agonist^[5] and have an indirect effect by increasing plasma serotonin levels.^[6]

5-HT_2C agonists

Lorcaserin is a thermogenic and anorectic weight-loss drug which acts as a selective 5-HT_2C agonist.

5-HT₄ agonists

Cisapride and Tegaserod are 5-HT₄ partial receptor agonist that were used to treat disorders of gastrointestinal motility. Prucalopride is a highly selective 5-HT₄ receptor agonist that can be used to treat certain disorders of gastrointestinal motility. Other 5-HT₄ agonists have shown potential to be nootropic type drugs via promoting acetylcholine release.

5-HT₇ agonists

AS-19 (drug) is a 5-HT₇ receptor agonist that has been used only in research.

References

^ Aghajanian, M.D., G.K.; G.J. Marek, M.D., Ph.D. (1999). "Serotonin and Hallucinogens". Neuropharmacology 21 (2S): 16S. doi:10.1016/s0893-133x(98)00135-3. Cite uses deprecated parameter |coauthors= (help); |access-date= requires |url= (help)
^ Hutcheson, J. D., Setola, V., Roth, B. L., & Merryman, W. D. (2011). Serotonin receptors and heart valve disease—it was meant 2B. Pharmacology & therapeutics, 132(2), 146-157.
^ Brea, J., Castro-Palomino, J., Yeste, S., Cubero, E., Párraga, A., Domínguez, E., & Loza, M. I. (2010). Emerging Opportunities and Concerns for Drug Discovery at Serotonin 5-HT2B Receptors. Current topics in medicinal chemistry, 10(5), 493-503.
^ Halberstadt, A. L., & Geyer, M. A. (2011). Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens. Neuropharmacology, 61(3), 364-381.
^ Hutcheson, J. D., Setola, V., Roth, B. L., & Merryman, W. D. (2011). Serotonin receptors and heart valve disease—it was meant 2B. Pharmacology & therapeutics, 132(2), 146-157.
^ Zolkowska, D., Rothman, R. B., & Baumann, M. H. (2006). Amphetamine analogs increase plasma serotonin: implications for cardiac and pulmonary disease. Journal of Pharmacology and Experimental Therapeutics, 318(2), 604-610.

External links

IUPHAR GPCR Database - 5-HT receptor family
MeSH list of agents 82017366
Serotonin agonists at the US National Library of Medicine Medical Subject Headings (MeSH)

UpToDate Contents

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English Journal

Effects of the 5-HT(6) receptor agonist ST 1936 on depression- and anhedonia-like experimental models.

Scheggi S, Marchese G, Borsini F, Bordi F, De Montis MG.SourceDepartment of Neuroscience, University of Siena, Via Moro 4, 53100 Siena, Italy.
Behavioural brain research.Behav Brain Res.2011 Oct 10;224(1):35-43. Epub 2011 May 27.
Serotonin 5-HT(6) receptor agonists and antagonists have been proposed as possible useful compounds in the treatment of psychiatric disorders such as depression. This study was aimed at characterizing ST 1936, a new 5-HT(6) receptor agonist, as a possible antidepressant/anti-anhedonic drug by studyi
PMID 21645553

Desmosterol replaces cholesterol for ligand binding function of the serotonin(1A) receptor in solubilized hippocampal membranes: Support for nonannular binding sites for cholesterol?

Singh P, Jafurulla M, Paila YD, Chattopadhyay A.AbstractThe serotonin(1A) receptor is an important member of the G-protein coupled receptor family, and is involved in the generation and modulation of a variety of cognitive and behavioral functions. Solubilization of the hippocampal serotonin(1A) receptor by CHAPS is accompanied by loss of cholesterol that results in a reduction in specific agonist binding activity. Replenishment of cholesterol to solubilized membranes restores membrane cholesterol content and significantly recovers specific agonist binding. In order to test the stringency of cholesterol requirement, we solubilized native hippocampal membranes followed by replenishment with desmosterol. Desmosterol is the immediate biosynthetic precursor of cholesterol in the Bloch pathway differing only in a double bond at the 24th position. Our results show that replenishment with desmosterol restores ligand binding of serotonin(1A) receptors. This is consistent with earlier results showing that desmosterol can replace cholesterol in a large number of cases. However, these results appear to be contradictory to our earlier findings, performed by sterol manipulation utilizing methyl-β-cyclodextrin, in which we observed that replacing cholesterol with desmosterol is unable to restore specific ligand binding of the hippocampal serotonin(1A) receptor. We discuss the possible molecular mechanism, in terms of nonannular lipid binding sites around the receptor, giving rise to these differences.
Biochimica et biophysica acta.Biochim Biophys Acta.2011 Oct;1808(10):2428-34. Epub 2011 Jul 5.
The serotonin(1A) receptor is an important member of the G-protein coupled receptor family, and is involved in the generation and modulation of a variety of cognitive and behavioral functions. Solubilization of the hippocampal serotonin(1A) receptor by CHAPS is accompanied by loss of cholesterol tha
PMID 21763272

Japanese Journal

Decreased Motility of the Lower Esophageal Sphincter in a Rat Model of Gastroesophageal Reflux Disease May Be Mediated by Reductions of Serotonin and Acetylcholine Signaling

Saegusa Yayoi,Takeda Hiroshi,Muto Shuichi,Oridate Nobuhiko,Nakagawa Koji,Sadakane Chiharu,Nahata Miwa,Harada Yumi,Iizuka Mizuki,Hattori Tomohisa,Asaka Masahiro
Biological & Pharmaceutical Bulletin 34(5), 704-711, 2011
… The in vivo motility proximal to LES (% motility index) in conscious rats was decreased by atropine treatment and increased by cisapride (5-HT4 receptor agonist) treatment. … Acetylcholine- and serotonin (5-HT)-induced LES contraction and sodium nitroprusside-induced relaxation in LES strips of GERD rats markedly decreased compared to sham-operated rats. …
NAID 130000657784

セロトニン1A受容体アゴニストのSAMマウスへの影響

NIIMI Kimie,TAKAHASHI Eiki,ITAKURA Chitoshi
Experimental Animals 59(4), 441-447, 2010
… The hallucinogenic chemical 1-[2,5-dimethoxy-4-iodophenyl]-2-aminopropane (DOI), a serotonin receptor 2A (5-HT2AR) agonist, evokes extracellular signal-regulated kinase 1/2 (ERK1/2) signaling and head-twitch behavior. … We previously reported that the senescence accelerated-prone mouse 6 (SAMP6) exhibited altered emotional behavior and increased levels of a serotonin-biosynthesizing enzyme compared to the senescence accelerated-resistant mouse 1 (SAMR1); …
NAID 130000298604

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リンク元	「セロトニン受容体刺激薬」「5-HT agonist」「serotonin agonist」「serotonergic agonist」「5-HT2 agonist」
関連記事	「receptor agonist」「serotonin receptor」「serotonin」