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 neurotransmitter involved in e.g. sleep and depression and memory (同)5-hydroxytryptamine

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/12/09 15:01:23」(JST)

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A serotonin receptor agonist is a compound that activates serotonin receptors, mimicking the effect of the neurotransmitter serotonin. There are various serotonin receptors and ligands.

5-HT_1A receptor

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

5-HT_1B receptor

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 receptor

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 receptor

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 receptor

Psychedelic drugs such as LSD, mescaline, psilocin, DMT, and 2C-B act as 5-HT_2A agonists. Their action at this receptor is responsible for their hallucinogenic effects.

It is now known that many of these drugs act as agonists at many other 5HT receptors in addition to the 5-HT2A including the 5-HT2C and others. Not all 5-HT_2A agonists are psychoactive.^{[citation needed]}

5-HT_2C receptor

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

5-HT₄ receptor

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 receptor

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

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)

This drug article relating to the gastrointestinal system is a stub. You can help Wikipedia by expanding it.

This drug article relating to the nervous system is a stub. You can help Wikipedia by expanding it.

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1. セロトニンモジュレータ：薬理学、投与、および副作用 serotonin modulators pharmacology administration and side effects
2. セロトニン - ノルエピネフリン再取り込み阻害剤（SNRIs）：薬理学、投与、および副作用 serotonin norepinephrine reuptake inhibitors snris pharmacology administration and side effects
3. 成人における過敏性腸症候群の治療 treatment of irritable bowel syndrome in adults
4. 成人の顔面紅潮に対するアプローチ approach to flushing in adults
5. セロトニン症候群 serotonin syndrome

English Journal

Similar anxiolytic effects of agonists targeting serotonin 5-HT1A or cannabinoid CB receptors on zebrafish behavior in novel environments.

Connors KA1, Valenti TW2, Lawless K3, Sackerman J3, Onaivi ES3, Brooks BW4, Gould GG5.Author information 1Department of Environmental Science, Institute of Biomedical Studies, Baylor University, Waco, TX 76798-7266, USA.2Department of Environmental Science, The Institute of Ecological, Earth, and Environmental Science, Baylor University, Waco, TX 76798-7266, USA(1); Syngenta Crop Protection LLC, Greensboro, NC 27419, USA(2).3Department of Biology, William Paterson University, Wayne, NJ 07470, USA.4Department of Environmental Science, Institute of Biomedical Studies, Baylor University, Waco, TX 76798-7266, USA; Department of Environmental Science, The Institute of Ecological, Earth, and Environmental Science, Baylor University, Waco, TX 76798-7266, USA(1).5Department of Physiology and Center for Biomedical Neuroscience, The University of Texas Health Science Center at San Antonio, San Antonio, TX 78229-3900, USA. Electronic address: gouldg@uthscsa.edu.AbstractThe discovery that selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine are present and bioaccumulate in aquatic ecosystems have spurred studies of fish serotonin transporters (SERTs) and changes in SSRI-sensitive behaviors as adverse outcomes relevant for risk assessment. Many SSRIs also act at serotonin 5-HT1A receptors. Since capitalizing on this action may improve treatments of clinical depression and other psychiatric disorders, novel multimodal drugs that agonize 5-HT1A and block SERT were introduced. In mammals both 5-HT1A and CB agonists, such as buspirone and WIN55,212-2, reduce anxious behaviors. Immunological and behavioral evidence suggests that 5-HT1A-like receptors may function similarly in zebrafish (Danio rerio), yet their pharmacological properties are not well characterized. Herein we compared the density of [(3)H] 8-hydroxy-2-di-n-propylamino tetralin (8-OH-DPAT) binding to 5-HT1A-like sites in the zebrafish brain, to that of similarly Gαi/o-coupled cannabinoid receptors. [(3)H] 8-OH-DPAT specific binding was 176±8, 275±32, and 230±36fmol/mg protein in the hypothalamus, optic tectum, and telencephalon. [(3)H] WIN55,212-2 binding density was higher in those same brain regions at 6±0.3, 5.5±0.4 and 7.3±0.3pm/mg protein. The aquatic light-dark plus maze was used to examine behavioral effects of 5-HT1A and CB receptor agonists on zebrafish novelty-based anxiety. With acute exposure to the 5-HT1A partial-agonist buspirone (50mg/L), or dietary exposure to WIN55,212-2 (7μg/week) zebrafish spent more time in and/or entered white arms more often than controls (p<0.05). Acute exposure to WIN55,212-2 at 0.5-50mg/L reduced mobility. These behavioral findings suggest that azipirones, like cannabinoid agonists, have anxiolytic and/or sedative properties on fish in novel environments. These observations highlight the need to consider potential ecological risks of azapirones and multimodal antidepressants in the future.
Aquatic toxicology (Amsterdam, Netherlands).Aquat Toxicol.2014 Jun;151:105-13. doi: 10.1016/j.aquatox.2013.12.005. Epub 2013 Dec 12.
The discovery that selective serotonin reuptake inhibitors (SSRIs) such as fluoxetine are present and bioaccumulate in aquatic ecosystems have spurred studies of fish serotonin transporters (SERTs) and changes in SSRI-sensitive behaviors as adverse outcomes relevant for risk assessment. Many SSRIs a
PMID 24411165

N-acetylcysteine modulates hallucinogenic 5-HT2A receptor agonist-mediated responses: Behavioral, molecular, and electrophysiological studies.

Lee MY1, Chiang CC2, Chiu HY3, Chan MH4, Chen HH5.Author information 1Department of Pharmacology and Toxicology, Tzu Chi University, 701, Section 3, Chung-Yang Road, Hualien 97004, Taiwan.2School of Medicine, Tzu Chi University, 701, Section 3, Chung-Yang Road, Hualien 97004, Taiwan.3Department of Pharmacy, Hualien, Tzu Chi General Hospital, 707, Section 3, Chung-Yang Road, Hualien 97004, Taiwan.4Institute of Neuroscience, National Changchi University, 64, Sec. 2, ZhiNan Road, Wenshan District, Taipei City 11605, Taiwan; Research Center for Mind, Brain, and Learning, National Changchi University, 64, Sec. 2, ZhiNan Road, Wenshan District, Taipei City 11605, Taiwan.5Department of Pharmacology and Toxicology, Tzu Chi University, 701, Section 3, Chung-Yang Road, Hualien 97004, Taiwan; Center for Neuropsychiatric Research, National Health Research Institutes, 35 Keyan Road, Zhunan, Miaoli County 35053, Taiwan. Electronic address: hwei5514@gmail.com.AbstractN-acetylcysteine (NAC) has been reported to reverse the psychotomimetic effects in the rodent phencyclidine model of psychosis and shown beneficial effects in treating patients with schizophrenia. The effect of NAC has been associated with facilitating the activity of cystine-glutamate antiporters on glial cells concomitant with the release of non-vesicular glutamate, which mainly stimulates the presynaptic metabotropic glutamate receptor subtype 2 receptors (mGluR2). Recent evidence demonstrated that functional interactions between serotonin 5-HT2A receptor (5-HT2AR) and mGluR2 are responsible to unique cellular responses when targeted by hallucinogenic drugs. The present study determined the effects of NAC on hallucinogenic 5-HT2AR agonist (±)1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (DOI)-elicited behavioral and molecular responses in mice and DOI-evoked field potentials in the mouse cortical slices. NAC significantly attenuated DOI-induced head twitch response and expression of c-Fos and Egr-2 in the infralimbic and motor cortex and suppressed the increase in the frequency of excitatory field potentials elicited by DOI in the medial prefrontal cortex. In addition, the cystine-glutamate antiporter inhibitor (S)-4-carboxyphenylglycine (CPG) and the mGluR2 antagonist LY341495 reversed the suppressing effects of NAC on DOI-induced head twitch and molecular responses and increased frequency of excitatory field potentials, supporting that NAC attenuates the 5-HT2AR-mediated hallucinogenic effects via increased activity of cystine-glutamate antiporter followed by activation of mGluR2 receptors. These findings implicate NAC as a potential therapeutic agent for hallucinations and psychosis associated with hallucinogen use and schizophrenia.
Neuropharmacology.Neuropharmacology.2014 Jun;81:215-23. doi: 10.1016/j.neuropharm.2014.02.006. Epub 2014 Feb 15.
N-acetylcysteine (NAC) has been reported to reverse the psychotomimetic effects in the rodent phencyclidine model of psychosis and shown beneficial effects in treating patients with schizophrenia. The effect of NAC has been associated with facilitating the activity of cystine-glutamate antiporters o
PMID 24534112

Inhibitory effect of the selective serotonin 5-HT3 receptor antagonist ramosetron on duodenal acidification-induced gastric hypersensitivity in rats.

Nakata-Fukuda M1, Hirata T2, Keto Y2, Yamano M2, Yokoyama T2, Uchiyama Y3.Author information 1Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan; Department of Cell Biology and Neuroscience, Juntendo University Graduate School of Medicine, 2-1-1 Hongo, Bunkyo-ku, Tokyo 113-8421, Japan. Electronic address: mari.nakata@astellas.com.2Pharmacology Research Labs., Drug Discovery Research, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan.3Department of Cell Biology and Neuroscience, Juntendo University Graduate School of Medicine, 2-1-1 Hongo, Bunkyo-ku, Tokyo 113-8421, Japan.AbstractIrritable bowel syndrome (IBS) and functional dyspepsia (FD) are both functional gastrointestinal disorders and frequently co-occur in patients. While one cause of FD appears to be gastric hypersensitivity, whether the hypersensitivity is affected by IBS treatments remains unclear, given the lack of appropriate animal models for testing. Here, we established an experimental model of duodenal acidification-induced gastric hypersensitivity in conscious rats. The model involved duodenal acidification induced by the infusion of hydrochloric acid into the proximal duodenum, with the nociceptive response being determined as the change in mean arterial pressure (MAP) during gastric distension via an indwelling latex balloon. Using our model we evaluated the effects of duodenal acidification, increased distension pressure, and orally administered therapeutic agents for IBS with diarrhea (IBS-D). Duodenal acidification enhanced the pressor response during gastric distension, and pretreatment with the opioid κ-receptor agonist fedotozine (10mg/kg, intra-arterial) inhibited the pressor response. Pressure levels of 15-60mmHg increased MAP in response to gastric distension. The serotonin 5-HT3 receptor antagonist ramosetron (30μg/kg) inhibited MAP increase induced by duodenal acidification, with no other IBS-D therapeutic agents showing any effect. In contrast, the serotonin 5-HT3 receptor agonist m-chlorophenylbiguanide (1mg/kg) significantly enhanced the pressor response during gastric distension. These findings indicate that the serotonin 5-HT3 receptor plays a key role in duodenal acidification-induced gastric hypersensitivity in rats, suggesting that ramosetron may reduce FD symptoms by ameliorating sensitized gastric perception.
European journal of pharmacology.Eur J Pharmacol.2014 May 15;731:88-92. doi: 10.1016/j.ejphar.2014.02.040. Epub 2014 Mar 13.
Irritable bowel syndrome (IBS) and functional dyspepsia (FD) are both functional gastrointestinal disorders and frequently co-occur in patients. While one cause of FD appears to be gastric hypersensitivity, whether the hypersensitivity is affected by IBS treatments remains unclear, given the lack of
PMID 24632457

Japanese Journal

うつ病治療における5-HT_1A受容体部分アゴニストを用いた「増強療法」が海馬神経新生に与える影響についての基礎的検討

森征慶
福岡大学薬学集報 15(0), 65-71, 2015-03
NAID 110009882360

Industrial Info. 統合失調症治療薬

廣瀬毅
細胞 45(3), 132-136, 2013-03
NAID 40019691702

Anti-emetic Effect of Mosapride Citrate Hydrate, a 5-HT_4 Receptor Agonist, on Selective Serotonin Reuptake Inhibitors (SSRIs)-Induced Emesis in Experimental Animals

MINE Yukiko,OKU Seiko,YOSHIDA Naoyuki
Journal of pharmacological sciences 121(1), 58-66, 2013-01-20
NAID 10031147587

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★リンクテーブル★

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