WordNet

a drug that neutralizes or counteracts the effects of another drug
a muscle that relaxes while another contracts; "when bending the elbow the triceps are the antagonist"
a neurotransmitter involved in e.g. sleep and depression and memory (同)5-hydroxytryptamine

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対立する人,敵対者,競争相手(opponent)

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/09 13:19:19」(JST)

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A serotonin antagonist is a drug used to inhibit the action at serotonin (5-HT) receptors.

Types

5-HT_2A antagonists

Antagonists of the 5-HT_2A receptor are sometimes used as atypical antipsychotics (contrast with typical antipsychotics, which are purely dopamine antagonists). They include:

Cyproheptadine blocks 5-HT_2A, H1 and is a mild anticholinergic.
Methysergide is a 5-HT_2A antagonist and nonselective 5-HT₁ receptor blocker. It causes retroperitoneal fibrosis and mediastinal fibrosis.^{[citation needed]}
Quetiapine blocks 5-HT_2A, 5-HT_1A, dopamine receptors D₁ and D₂, histamine receptor H1, and A1 adrenoreceptors.

5-HT_2A/2C antagonists

ketanserin Antihypertensive. Blocks 5-HT_2A, 5-HT_2C and Alpha 1 (A1) adrenoreceptors.
Risperidone antipsychotic
Trazodone antidepressant
Clozapine antipsychotic. Blocks 5-HT_2A, 5-HT_2C and D₄ receptors.

5-HT₃ antagonists

Another subclass consists of drugs selectively acting at the 5-HT₃ receptors, and thus are known as 5-HT₃ antagonists. They are efficacious in treating chemotherapy-induced emesis and postoperative nausea and vomiting.^[1] They include:

Dolasetron
Granisetron
Ondansetron
Palonosetron
Tropisetron

Other 5-HT₃ antagonists are used for the treatment of irritable bowel syndrome:

Alosetron
Cilansetron

Non-selective 5-HT antagonists

Please note, that although some non-selective serotonin antagonists may have an particular affinity for a specific 5-HT receptor (and thus may be listed above e.g. methysergide), they still may also possess a generalised non-selective action.

Methysergide
Chlorpromazine
Cyproheptadine
Pizotifen
Oxetorone
Spiperone
Ritanserin
Parachlorophenylalanine
Metergoline
Propranolol
Mianserin

Serotonin antagonists acting as antihistamines for allergic conditions

Carbinoxamine
Cyproheptadine
Methdilazine
Promethazine
Pizotifen is a 5-HT_2C antagonist, H1 blocker and anticholinergic useful in migraine prophylaxis.^{[citation needed]} Also used in the treatment of migrane.
oxetorone Also used in the treatment of migrane.
Oxatomide

Others

Feverfew Is a herb traditionally used for migraines.
Fenclonine An inhibitor of serotonin synthesis that has been used in the treatment of carcinoid syndrome.
Reserpine Depletes serotonin stores in the brain, heart, and many other organs and has been used in hypertension and psychosis

References

^ Lindley, C.; Blower, P. (2000). "Oral serotonin type 3-receptor antagonists for prevention of chemotherapy-induced emesis". American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists 57 (18): 1685–1697. PMID 11006796.

External links

Serotonin Antagonists at the US National Library of Medicine Medical Subject Headings (MeSH)
MeSH list of agents 82012702

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

UpToDate Contents

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1. 制吐剤の特性 characteristics of antiemetic drugs
2. 麻酔後ケア病棟における合併症発生の概要 overview of complications occurring in the post anesthesia care unit
3. 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
4. 化学療法誘発性悪心および嘔吐の予防および治療 prevention and treatment of chemotherapy induced nausea and vomiting
5. セロトニン症候群 serotonin syndrome

English Journal

Applications of yeast-based signaling sensor for characterization of antagonist and analysis of site-directed mutants of the human serotonin 1A receptor.

Nakamura Y1, Ishii J2, Kondo A3.
Biotechnology and bioengineering.Biotechnol Bioeng.2015 Sep;112(9):1906-15. doi: 10.1002/bit.25597. Epub 2015 Jun 30.
The monoamine neurotransmitter serotonin (5-HT) regulates a wide spectrum of human physiology through the 5-HT receptor family. One such receptor, the 5-HT1A receptor (HTR1A), is the most widely studied subtype and represents a significant molecular target in medicinal and therapeutic fields. Yeast-
PMID 25850571

Serotonin Receptor Agonist 5-Nonyloxytryptamine Alters the Kinetics of Reovirus Cell Entry.

Mainou BA1, Ashbrook AW2, Smith EC1, Dorset DC3, Denison MR4, Dermody TS5.
Journal of virology.J Virol.2015 Sep 1;89(17):8701-12. doi: 10.1128/JVI.00739-15. Epub 2015 Jun 24.
Mammalian orthoreoviruses (reoviruses) are nonenveloped double-stranded RNA viruses that infect most mammalian species, including humans. Reovirus binds to cell surface glycans, junctional adhesion molecule A (JAM-A), and the Nogo-1 receptor (depending on the cell type) and enters cells by receptor-
PMID 26109733

Androgen metabolites impact CSF amines and axonal serotonin via MAO-A and -B in male macaques.

Bethea CL1, Phu K2, Kim A2, Reddy AP2.
Neuroscience.Neuroscience.2015 Aug 20;301:576-89. doi: 10.1016/j.neuroscience.2015.06.020. Epub 2015 Jun 16.
A number of studies have shown that mutations or deletions of the monoamine oxidase-A (MAO-A) gene cause elevated CNS serotonin and elevated impulsive aggression in humans and animal models. In addition, low cerebrospinal fluid (CSF) 5-hydroxyindole acetic acid (5HIAA) has been documented in a limit
PMID 26086546

Japanese Journal

Effect of Selective Serotonin Reuptake Inhibitors via 5-HT_<1A> Receptors on L-DOPA-Induced Rotational Behavior in a Hemiparkinsonian Rat Model

INDEN Masatoshi,ABE Mari,MINAMINO Hideaki,TAKATA Kazuyuki,YOSHIMOTO Kanji,TOOYAMA Ikuo,KITAMURA Yoshihisa
Journal of pharmacological sciences 119(1), 10-19, 2012-05-20
… On the other hand, selective serotonin reuptake inhibitors (SSRIs) including fluoxetine have gained tremendous popularity in the treatment of depression in PD. … antagonist. …
NAID 10030760133

Effect of Aripiprazole on Anxiety Associated With Ethanol Physical Dependence and on Ethanol-Induced Place Preference

SHIBASAKI Masahiro,KUROKAWA Kazuhiro,MIZUNO Koji,OHKUMA Seitaro
Journal of pharmacological sciences 118(2), 215-224, 2012-02-20
… These decreases were reversed by treatment of aripiprazole, which were inhibited by WAY100635, a serotonin 5-HT<SUB>1A</SUB> … receptor antagonist. …
NAID 10030454888

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★リンクテーブル★

リンク元	「セロトニン拮抗薬」「セロトニン遮断薬」「抗セロトニン薬」「セロトニン受容体遮断薬」「5-HT antagonist」
関連記事	「serotonin」