5-HT4受容体刺激薬、5-HT4刺激薬、5-HT4アゴニスト

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)
the 8th letter of the Roman alphabet (同)h

PrepTutorEJDIC

hydrogenの化学記号
鉛筆の硬度 / 《俗》heroin

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/07/03 21:59:17」(JST)

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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:[edit]

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:[edit]

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:[edit]

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:[edit]

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 was halted however due to toxicity detected in animal test subjects. Lasmiditan has successfully completed Phase II clinical trials in early 2010.

5-HT_2A agonists:[edit]

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_2C agonists:[edit]

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

5-HT₄ agonists:[edit]

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:[edit]

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

References[edit]

^ Aghajanian, M.D., G.K.; G.J. Marek, M.D., Ph.D. (1999). "Serotonin and Hallucinogens". Neuropharmacology 21 (No. 2S): 16S. |accessdate= requires |url= (help)

External links[edit]

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)

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English Journal

Effects of prenatal stress and monoaminergic perturbations on the expression of serotonin 5-HT₄ and adrenergic β₂ receptors in the embryonic mouse telencephalon.

Chen A, Kelley LD, Janušonis S.SourceDepartment of Psychological and Brain Sciences, University of California, Santa Barbara, CA 93106-9660, USA.
Brain research.Brain Res.2012 Jun 12;1459:27-34. Epub 2012 Apr 19.
The serotonin 5-HT(4) receptor (5-HT(4)R) is coded by a complex gene that produces four mRNA splice variants in mice (5-HT(4(a))R, 5-HT(4(b))R, 5-HT(4(e))R, 5-HT(4(f))R). This receptor has highly dynamic expression in brain development and its splice variants differ in their developmental trajectori
PMID 22564922

The effects of 5-HT4 receptor agonist, mosapride citrate, on visceral hypersensitivity in a rat model.

Lee JW, Sung KW, Lee OY, Lee SE, Sohn CI.SourceDivision of Gastroenterology, Hanil General Hospital, Seoul, Korea.
Digestive diseases and sciences.Dig Dis Sci.2012 Jun;57(6):1517-24. Epub 2012 Mar 17.
BACKGROUND AND AIMS: Mosapride citrate is known to affect gastric motility. However, whether mosapride citrate has any effect on visceral pain in the colon or rectum is not certain. The aim of this study was to assess the effects of mosapride citrate on visceral pain in a rat visceral hypersensitivi
PMID 22427128

Japanese Journal

迷走神経機能不全下での知覚神経感作とセロトニン4受容体作動薬mosaprideによる鎮痛効果

古田貞由,松本健次郎,堀江俊治 [他]
日本緩和医療薬学雑誌 4(3), 93-98, 2011-10
NAID 40019043862

Effects of Mosapride Citrate, a 5-HT_4-Receptor Agonist, on Gastric Distension-Induced Visceromotor Response in Conscious Rats

SETO Yasuhiro,YOSHIDA Naoyuki,KANEKO Hiroshi
Journal of pharmacological sciences 116(1), 47-53, 2011-05-20
… Mosapride citrate (mosapride), a prokinetic agent with 5-HT4–receptor agonistic activity, is known to enhance gastric emptying and alleviate symptoms in patients with functional dyspepsia (FD). … Additionally, a major metabolite M1 of mosapride, which possesses 5-HT3–receptor antagonistic activity, inhibited gastric distension–induced VMR. …
NAID 10029893898