5-HT1A受容体刺激薬、5-HT1A作動薬、5-HT1A刺激薬、5-HT1A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)

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/10/20 16:57:02」(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receptor are implicated in the progression of cardiac fibrosis.^[2] Fenfluramine, Pergolide and Cabergoline have been withdrawn from some markets for this reason.^[3] Some psychedelic drugs, including LSD and Psilocin, have been shown to activate this receptor directly.^[4] MDMA has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. |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

Serotonin-mediated central fatigue underlies increased endurance capacity in mice from lines selectively bred for high voluntary wheel running.

Claghorn GC1, Fonseca IA2, Thompson Z1, Barber C1, Garland T Jr3.
Physiology & behavior.Physiol Behav.2016 Jul 1;161:145-54. doi: 10.1016/j.physbeh.2016.04.033. Epub 2016 Apr 19.
Serotonin (5-hydroxytryptamine; 5-HT) is implicated in central fatigue, and 5-HT1A pharmaceuticals are known to influence locomotor endurance in both rodents and humans. We studied the effects of a 5-HT1A agonist and antagonist on both forced and voluntary exercise in the same set of mice. This coho
PMID 27106566

Serotonin antagonists fail to alter MDMA self-administration in rats.

Schenk S1, Foote J2, Aronsen D2, Bukholt N2, Highgate Q2, Van de Wetering R2, Webster J2.
Pharmacology, biochemistry, and behavior.Pharmacol Biochem Behav.2016 Jun 2;148:38-45. doi: 10.1016/j.pbb.2016.06.002. [Epub ahead of print]
Acute exposure to ±3,4-methylenedioxymethamphetamine (MDMA) preferentially increases release of serotonin (5-HT), and a role of 5-HT in many of the behavioral effects of acute exposure to MDMA has been demonstrated. A role of 5-HT in MDMA self-administration in rats has not, however, been adequatel
PMID 27264435

The novel 5-HT1A receptor agonist, NLX-112 reduces l-DOPA-induced abnormal involuntary movements in rat: A chronic administration study with microdialysis measurements.

McCreary AC1, Varney MA2, Newman-Tancredi A3.
Neuropharmacology.Neuropharmacology.2016 Jun;105:651-60. doi: 10.1016/j.neuropharm.2016.01.013. Epub 2016 Jan 9.
Although l-DOPA alleviates the motor symptoms of Parkinson's disease (PD), it elicits troublesome l-DOPA-induced dyskinesia (LID) in a majority of PD patients after prolonged treatment. This is likely due to conversion of l-DOPA to dopamine as a 'false neurotransmitter' from serotoninergic neurons.
PMID 26777281

Japanese Journal

Effects of the 5-HT₁A Receptor Agonist Tandospirone on ACTH-Induced Sleep Disturbance in Rats

Tsutsui Ryuki,Shinomiya Kazuaki,Sendo Toshiaki [他]
Biological & pharmaceutical bulletin 38(6), 884-888, 2015-06
NAID 40020471456

抑肝散による不眠の漢方治療 (特集睡眠障害と漢方治療)

小曽根基裕
漢方と最新治療 24(1), 15-21, 2015-02
NAID 40020377051

Effects of the 5-HT1A Receptor Agonist Tandospirone on ACTH-Induced Sleep Disturbance in Rats

Tsutsui Ryuki,Shinomiya Kazuaki,Sendo Toshiaki,Kitamura Yoshihisa,Kamei Chiaki
Biological and Pharmaceutical Bulletin 38(6), 884-888, 2015
… The aim of this study was to compare the effect of the serotonin (5-HT)1A receptor agonist tandospirone versus that of the benzodiazepine hypnotic flunitrazepam in a rat model of long-term adrenocorticotropic hormone (ACTH)-induced sleep disturbance. … The effect of tandospirone on sleep patterns was antagonized by the 5-HT1A receptor antagonist WAY-100635. …
NAID 130005072657