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̽Ἢ릪̽릪춪ʪ몫ɪ

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̽Ἢ릪̽릪춪ʪ몫ɪ
-1993-701680号-
(2003.2.11.ͱ20022303̽)
(2002.9.13.ͱ2001997̽)

1.ӫͭ
国庁1999Ҵ329発٥ϴ囲1ʪ410発٥当涪発٥ǪΪǪ몿ᡢ29条2ЮҪ当ɪ몳ȪǪʪȪ릪Ҫ

2.ª̽
1発٥発٥ڪ経薬ުܻ効󪹪医薬ԲڪǪêơ1発٥崪発٥Ϊ誦ҪĪڪ囲Ҫꡢ対ڪ広囲ʪᡢ̪ƪڪ々対体ܪ実˪ê々ڪȪڪǪ몳Ȫ㪹ڪ驪ΪǪϪʪ数˪ڪΪǪ数ڪ﷪Ҫ몳Ȫ˪êơϴ囲쪿Ҫڪ٥ᬪ説٥˪모Ȫᬪ説٥쪿1発٥ڪ発٥ڪȪǪʪȪ1発٥発٥Ȫު発٥ǪȪϴѪϪ릪ʪ

êơ1発٥発٥ڪ関発٥ǪꡢڪΪΪǡުܻ経薬ȪĪǪ몿ᡢ1発٥当発٥涪発٥ǪΪǪ롣

3.ª̽

(1)択発٥˪Ī
ݡ択発٥Ȫϡ学発٥寪˪ΪǪêơ発٥ު߾概ҷ˪概ҷ囲内ǡ発٥ʪɪ献体ܪƪƪʪ概ҷϰȪ発٥Ǫꡢܪ発٥囲ߪުΪΪǪ몿ЮҪ󪹪몳ȪǪʪΪǪ몬ܪ発٥Ǫʪ顕ʪ効ڪê󪹪発٥몤몦顕ʪ効Ȫ単発٥ު効ǪϪʪ発٥˪۪Ȫ顕ʪ춪ʪꪽ쪬発٥効ΪΪǪ몫ȪΪǪ몫諸発٥ȪܬԲ檷ɪ与檷発٥모ΪΪګ̸Ϊ当Ǫ롣

ު42条3ϡ発٥ᬪ説٥˪Ϫ発٥属寪˪Ȫ۪󪹪涪実㿪Ǫ˪発٥・ϰ効ʪЪʪʪЮҪƪȪ߾択発٥関̸֧ȡ択発٥ꡢʪЪʪʪ発٥ܪϰ発٥ΪΪ모몬発٥効˪ƪ発٥Ǫʪ顕ʪ効ʪЪʪʪ모発٥ʦڪ体観ܪҪ몳Ȫϴ몦ȪǪ롣

(2)顕ʪ効

発٥٥ڪA対顕ʪ効몫ɪ˪Ī̸ƪߪȡ発٥٥1˪ϡ発٥枢経ͧ˪ƫȫ˫-2(5-Hydroxytryptamine-2;5-HT2)体対択ܪĪ󪹪5--1-ԫګ髸Ϋ体Ӫ߫ʥ塩ªȪƪΪ誦体ߪ薬ڪ枢経ܻͧ˪体ӪΪ誦ڪ㪹۰関롯ƪꡢ4˪ϡҥ5-1-ԫګ髸Ϋ体5-HT2体対Ԫ󪹪Ȫ󪯪٪発̸򪷪対応6-体٪Ȫϫーѫ߫D-2体ӥ1ɫʫȪުȪ体󪹪롣体内˪ƪڪ枢5-HT2Ī対ڪǫ˪󪹪롣1ɫʫ対ުȪ˪ꪳ5-ڪ6体Ȫ춪ʪ圧ª絛ܪʪƪꡢ߾٥7˪ϡ発٥ڪ5-HT2体対ƪԪƪD-2体ӥ1ɫʫ対ƪުȪ体ƪ̿ܪ˪ڪ5-HT2体対ުȪ択ܪǪ롣従êơڪ̡ܻ֮状ͯܪ経薬Ī˪êڪê体ԪΪ誦枢経ͧ様々効Ǫ롯ƪꡢު٥˪ϨëȪد5-HT2体対3H-󫻫̿ꡢëȪ条体دΫーѫ߫D-2体対3H-ԫګ̿ӨëȪ脳دǪΥ1ɫʫ対3H-׫髾̿˪薬˪体Ҫ몿۰Ӫ۰˿쪿参献(Hyttel,Pharmacology&Toxicology,61,126-129,1987۰ʪ)˿ʪ5-HT2体ーѫ߫D-2体ӥ1adrenoceptor対몽̿1体̿IC50(nM)˪ڪΪȫ-1-[2-[4-[3-(4-ի뫪ի˫)-5-(ȫի뫪)-23-ҫɫ]-2ҫɫ-1H-ǫ-1-]-1-ԫګ髸󫤫]]-2-߫꫸Ϋʪ4Īڪ(ڪB)Ϊߪ対効˪Ī311˪IC50数Ҫ体ܪƪ몬˫ȫ-1-[2-[4-[5-ի뫪-3(4-ի뫪ի˫)-23-ҫɫ-1H-ǫ-1-]ԫګ髸-1-]]-2-߫꫸Ϋʪ4Īڪ(ڪC)˪ĪƪڪBΪ誦体ܪ絛ʪ

Ǫʪ顢ڪB対ƪ5-HT2ڪǪ꫿󫻫(Ritanserin) ƫի(Tefludazine)(Irindalone)ڪ194対応体々򫤫5-Ǫ۪6-Ǫڪ(ڪ号394041)顕ʪǪ몳Ȫ1実験̿˪ª몿ᡢ発٥Ȫ顕ʪ춪ʪ発٥ȪܬԲ檷ɪ与檷発٥Ǫ모顕ʪ効ꡢ顕ʪ効対体観ܪҪ모몬ڪC˪Īƪ顕ʪ効対ܡ観ܪΪߪ몦ȪǪ롣

êơ1発٥Ϫϴ囲ΪݻڪC対42条3Ҫ発٥効対ʪ몦ȪǪ롣

(3)ڪΪ誦発٥򱪵쪿ڪ対ݻ択ê択発٥˪ƪϡ択쪿ڪ発٥覆Ǫʪ顕ʪ効󪹪˪歩몿ᡢ単تڪ発٥覆顕ʪ効ȪܪȪڪΪݻ対体観ܪҪ쪿数˪ΪߪǪϡϴ囲ҪȪ関ʪ当発٥˪ϴƪƪڪ対顕ʪ効쪿몦ȪϪǪʪ

(4)̿
Ǫʪ顢ͱ旧(2001Ҵ236411号᪵Ϊ)63条62条4号42条3˪ͱ対Ҫ(歩)(1発٥ϴ囲ΪݻǪڪC発٥効対

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