ＧＲ‐５５５６２とは？わかりやすく解説

GR-55562
臨床データ
別名	GR55562; GR-55,562; GR55,562
薬物クラス	Serotonin 5-HT1B and 5-HT1D receptor antagonist; Selective serotonin 5-HT1B antagonist
識別子
	IUPAC名 3-[3-(dimethylamino)propyl]-4-hydroxy-N-(4-pyridin-4-ylphenyl)benzamide ;
CAS登録番号	159533-26-3;
PubChem CID	128018;
IUPHAR/BPS	113;
ChemSpider	113523;
UNII	QPY74DMU5M;
ChEBI	CHEBI:92813;
ChEMBL	ChEMBL119264;
CompTox; ダッシュボード (EPA)	DTXSID701150576 ;
化学的および物理的データ
化学式	C23H25N3O2
分子量	375.47 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CN(C)CCCC1=C(C=CC(=C1)C(=O)NC2=CC=C(C=C2)C3=CC=NC=C3)O ;
	InChI InChI=1S/C23H25N3O2/c1-26(2)15-3-4-19-16-20(7-10-22(19)27)23(28)25-21-8-5-17(6-9-21)18-11-13-24-14-12-18/h5-14,16,27H,3-4,15H2,1-2H3,(H,25,28) ; Key:ZAGAUUVCYGSPBP-UHFFFAOYSA-N ;
	テンプレートを表示

GR-55562は、選択的セロトニン5-HT_1Bおよび5-HT_1D受容体アンタゴニストである^[1]。科学研究で使用される選択的セロトニン5-HT_1B受容体アンタゴニストの一つである^[2]^[3]。

関連薬物のGR-127935とは異なり、セロトニン5-HT_1B受容体のサイレントアンタゴニストである^[1]^[4]。GR-55562は、セロトニン5-HT_1D受容体と比較してセロトニン5-HT_1B受容体で約10倍の選択性を持ち、他のいくつかのセロトニン受容体には弱い親和性しか持たない^[4]。

動物ではMDMAによる向社会的行動を消失させる効果はない。逆に、セロトニン5-HT1A受容体拮抗薬WAY-100635（英語版）は、MDMAによる向社会的行動を消失させる^[5]^[6]。

出典

^ ^a ^b “5-HT_1B/1Dantagonists and depression”. Expert Opinion on Therapeutic Patents (Informa Healthcare) 7 (4): 339–352. (1997). doi:10.1517/13543776.7.4.339. ISSN 1354-3776. "However, as mentioned above, it was later found that GR-127935 is not a silent antagonist at human 5- HT1B/1D sites. More recent investigations from Glaxo and others have shown that, unlike GR-127935, GR55562 could be characterised as a silent, potent and selective h5-HT1B receptor antagonist [43]. However, so far no results have been disclosed concerning the ability of this particular compound to antagonise central presynaptic 5-HT1B receptors upon systemic administration."
^ “THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors”. British Journal of Pharmacology 176 (Suppl 1): S21–S141. (December 2019). doi:10.1111/bph.14748. PMC 6844580. PMID 31710717.
^ “Molecular biology of 5-HT receptors”. Behavioural Brain Research 195 (1): 198–213. (December 2008). doi:10.1016/j.bbr.2008.03.020. PMID 18571247.
^ ^a ^b “GR 55562 dihydrochloride Supplier”. Tocris Bioscience. 2024年10月27日閲覧。 “GR 55562 dihydrochloride is a selective competitive 5-HT1B (5-HT1Dβ) silent antagonist with pKB values of 7.3 and 6.3 for human cloned 5-HT1B and 5-HT1D receptors respectively and only weak binding at a number of other 5-HT subtypes.”
^ “Effect of drugs of abuse on social behaviour: a review of animal models”. Behavioural Pharmacology 26 (6): 541–570. (September 2015). doi:10.1097/FBP.0000000000000162. PMID 26221831.
^ “Serotonin (1A) receptor involvement in acute 3,4-methylenedioxymethamphetamine (MDMA) facilitation of social interaction in the rat”. Progress in Neuro-Psychopharmacology & Biological Psychiatry 29 (5): 648–657. (June 2005). doi:10.1016/j.pnpbp.2005.04.009. PMID 15908091.

[HalazyLamotheJorand-Lebrun1997-1] “5-HT_1B/1Dantagonists and depression”. Expert Opinion on Therapeutic Patents (Informa Healthcare) 7 (4): 339–352. (1997). doi:10.1517/13543776.7.4.339. ISSN 1354-3776. "However, as mentioned above, it was later found that GR-127935 is not a silent antagonist at human 5- HT1B/1D sites. More recent investigations from Glaxo and others have shown that, unlike GR-127935, GR55562 could be characterised as a silent, potent and selective h5-HT1B receptor antagonist [43]. However, so far no results have been disclosed concerning the ability of this particular compound to antagonise central presynaptic 5-HT1B receptors upon systemic administration."

[AlexanderChristopoulosDavenport2019-2] “THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors”. British Journal of Pharmacology 176 (Suppl 1): S21–S141. (December 2019). doi:10.1111/bph.14748. PMC 6844580. PMID 31710717.

[HannonHoyer2008-3] “Molecular biology of 5-HT receptors”. Behavioural Brain Research 195 (1): 198–213. (December 2008). doi:10.1016/j.bbr.2008.03.020. PMID 18571247.

[Tocris-4] “GR 55562 dihydrochloride Supplier”. Tocris Bioscience. 2024年10月27日閲覧。 “GR 55562 dihydrochloride is a selective competitive 5-HT1B (5-HT1Dβ) silent antagonist with pKB values of 7.3 and 6.3 for human cloned 5-HT1B and 5-HT1D receptors respectively and only weak binding at a number of other 5-HT subtypes.”

[Blanco-GandíaMateos-GarcíaGarcía-Pardo2015-5] “Effect of drugs of abuse on social behaviour: a review of animal models”. Behavioural Pharmacology 26 (6): 541–570. (September 2015). doi:10.1097/FBP.0000000000000162. PMID 26221831.

[MorleyArnoldMcGregor2005-6] “Serotonin (1A) receptor involvement in acute 3,4-methylenedioxymethamphetamine (MDMA) facilitation of social interaction in the rat”. Progress in Neuro-Psychopharmacology & Biological Psychiatry 29 (5): 648–657. (June 2005). doi:10.1016/j.pnpbp.2005.04.009. PMID 15908091.

[1]

[2]

[3]

[4]

[5]

[6]

分子式：	C₂₃H₂₅N₃O₂
その他の名称：	GR-55562、4-Hydroxy-3-[3-(dimethylamino)propyl]-N-[4-(4-pyridinyl)phenyl]benzamide
体系名：	4-ヒドロキシ-3-[3-(ジメチルアミノ)プロピル]-N-[4-(4-ピリジニル)フェニル]ベンズアミド


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ＧＲ‐５５５６２とは？ わかりやすく解説

ＧＲ‐５５５６２

GR-55562

関連項目

出典

ＧＲ‐５５５６２とは？わかりやすく解説