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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2015/07/16 18:28:46」(JST)

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Terguride (INN) is a serotonin antagonist. It is used for the treatment of hyperprolactinemia. Terguride is an oral, potent antagonist of 5-HT2B and 5-HT2A (serotonin) receptors. Serotonin stimulates the proliferation of pulmonary artery smooth muscle cells, and induces fibrosis in the wall of pulmonary arteries. Together, this causes vascular remodeling and narrowing of the pulmonary arteries. These changes result in increased vascular resistance and PAH. Due to the potential anti-proliferative and anti-fibrotic activity of terguride, this potential medicine could offer the hope of achieving reversal of pulmonary artery vascular remodeling and attenuation of disease progression.^[1]

In May 2008, terguride was granted orphan drug status for the treatment of pulmonary arterial hypertension.^[2] In May 2010 Pfizer purchased world-wide rights for the drug.^[3]

References

^ Janssen W, Schymura Y, Novoyatleva T, Kojonazarov B, Boehm M, Wietelmann A, Luitel H, Murmann K, Krompiec DR, Tretyn A, Pullamsetti SS, Weissmann N, Seeger W, Ghofrani HA, Schermuly RT. 5-HT2B Receptor Antagonists Inhibit Fibrosis and Protect from RV Heart Failure. Biomed Research International. 2015;2015:438403. doi 10.1155/2015/438403 PMID 25667920
^ Presseportal (Swiss press portal, in German)
^ TheDay.com 5/10/2010

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English Journal

Pharmacological Profile of 2-Bromoterguride at Human Dopamine D2, Porcine Serotonin 5-HT2A and α2C-Adrenergic Receptors, and its Antipsychotic-Like Effects in Rats.

Jantschak F, Brosda J, Franke RT, Fink H, Moller D, Hubner H, Gmeiner P, Pertz HH.Source1 Free University of Berlin;
The Journal of pharmacology and experimental therapeutics.J Pharmacol Exp Ther.2013 Jul 17. [Epub ahead of print]
Dopaminergic, serotonergic and adrenergic receptors are targets for therapeutic actions in schizophrenia. Dopamine D2 receptor partial agonists such as aripiprazole represent a treatment option for patients with this severe disorder. The ineffectiveness of terguride, another D2 receptor partial agon
PMID 23863695

Pathways in pulmonary arterial hypertension: the future is here.

Sitbon O, Morrell N.SourceUniversité Paris-Sud, Hôpital de Bicêtre, Le Kremlin-Bicêtre, France.
European respiratory review : an official journal of the European Respiratory Society.Eur Respir Rev.2012 Dec 1;21(126):321-7. doi: 10.1183/09059180.00004812.
It is well established that the endothelin, nitric oxide and prostacyclin pathways play an important role in the development of pulmonary arterial hypertension (PAH). Indeed, the therapeutic options currently available for the management of PAH all act on one of these mechanistic pathways. However,
PMID 23204120

Antiserotonergic properties of terguride in blood vessels, platelets, and valvular interstitial cells.

Kekewska A, Görnemann T, Jantschak F, Glusa E, Pertz HH.SourceInstitute of Pharmacy, Free University of Berlin, Berlin, Germany.
The Journal of pharmacology and experimental therapeutics.J Pharmacol Exp Ther.2012 Feb;340(2):369-76. doi: 10.1124/jpet.111.187906. Epub 2011 Nov 2.
Serotonin (5-hydroxytryptamine; 5-HT) is involved in heart valve tissue fibrosis, pulmonary arterial fibrosis, and pulmonary hypertension. We aimed at characterizing the antiserotonergic properties of the ergot alkaloid derivative terguride [1,1-diethyl-3-(6-methyl-8α-ergolinyl)urea] by using funct
PMID 22049464

Japanese Journal

腹腔鏡下子宮筋腫核出術後に高プロラクチン血症が改善した一例

山中郁仁,内山響子,秋元太志,太枝美帆,恐神博行,山中雅,逸見博文,井上万梨絵,遠藤俊明
日本産科婦人科内視鏡学会雑誌 27(2), 441-445, 2011
… She had been taking cabergoline followed by terguride for nearly two years, but her hyperprolactinemia failed to respond to the deopamine agonists despite a gradual increase of their dosages. …
NAID 130002049870

随証漢方療法で生児を獲得した卵巣機能不全不妊症100例の漢方医学的ならびに西洋医学的解析

假野隆司,土方康世,清水正彦 [他],河田佳代子,日笠久美,後山尚久
日本東洋醫學雜誌 59(1), 35-45, 2008-01-20
目的:不妊症における漢方療法の適応は卵巣機能不全不妊症と考えられる。同疾患に対する集学的不妊治療における,漢方治療の適応を検討した。方法:卵巣機能不全不妊症患者で,随証漢方治療により,妊娠成立し生児を分娩できた漢方妊娠100症例を対象とした。1)漢方医学的診断について,種々の疾患による不妊症症例2737例をコントロール群として比較した。両群の特徴,虚実・陰陽・表裏・寒熱(八綱)・気血水に関する診断 …
NAID 110006596069

テルグリドの高プロラクチン血症治療効果のドパミンD_2受容体結合占有を考慮したPK/PD解析

山田安彦,入月直子,高柳理早 [他],山本康次郎,澤田康文,伊賀立二
藥學雜誌 123(4), 255-260, 2003-04-01
… Terguride has been widely used for the treatment of hyperprolactinemia via partial agonistic action on dopamine D_2 receptors in the pituitary. … The present study analyzed retrospectively the dopamine D_2 receptor binding occupancy (φ) of terguride. … The average φ value was estimated to be 14.1% after oral administration of the average/standard therapeutic dose of terguride. …
NAID 110003666108

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「テルグリド」

Terguride
Systematic (IUPAC) name
	N,N-diethyl-N'-[(8α)-6-methylergolin-8-yl]urea
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	℞ (Prescription only);
Routes of; administration	Oral
Identifiers
CAS Registry Number	37686-84-3
ATC code	G02CB06
PubChem	CID: 443951
IUPHAR/BPS	56
UNII	21OJT43Q88
KEGG	D01348
Chemical data
Formula	C20H28N4O
Molecular mass	340.46 g/mol
	SMILES CCN(CC)C(=O)N[C@H]1C[C@H]2[C@@H](CC3=CNC4=CC=CC2=C34)N(C1)C ;
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　　[★]

英: terguride
商: テルロン
関: プロラクチン

[1] Janssen W, Schymura Y, Novoyatleva T, Kojonazarov B, Boehm M, Wietelmann A, Luitel H, Murmann K, Krompiec DR, Tretyn A, Pullamsetti SS, Weissmann N, Seeger W, Ghofrani HA, Schermuly RT. 5-HT2B Receptor Antagonists Inhibit Fibrosis and Protect from RV Heart Failure. Biomed Research International. 2015;2015:438403. doi 10.1155/2015/438403 PMID 25667920

[2] Presseportal (Swiss press portal, in German)

[3] TheDay.com 5/10/2010

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terguride