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Novel 1,2,3,4-tetrahydroisoquinolines with high affinity and selectivity for the dopamine D3 receptor

التفاصيل البيبلوغرافية
العنوان: Novel 1,2,3,4-tetrahydroisoquinolines with high affinity and selectivity for the dopamine D3 receptor
المؤلفون: Michael S. Hadley, Stephen A. Smith, Kim Y. Avenell, David John Nash, Geoffrey Stemp, Kevin M. Thewlis, Martyn C. Coldwell, Clive Leslie Branch, Nigel E. Austin, Vong Antonio Kuok Keong, Graham J. Riley, Izzy Boyfield, Christopher N. Johnson, Rachel Stacey, Phillip Jeffrey, Amana Johns
المصدر: Bioorganic & Medicinal Chemistry Letters. 9:179-184
بيانات النشر: Elsevier BV, 1999.
سنة النشر: 1999
مصطلحات موضوعية: Models, Molecular, Receptors, Dopamine D2, Tetrahydroisoquinoline, Stereochemistry, Organic Chemistry, Clinical Biochemistry, Receptors, Dopamine D3, Substituent, Brain, Pharmaceutical Science, Isoquinolines, Biochemistry, Rats, chemistry.chemical_compound, chemistry, Dopamine receptor D3, Dopamine receptor D2, Drug Discovery, Animals, Molecular Medicine, Selectivity, Molecular Biology
الوصف: Using clearance and brain penetration studies as a screen, tetrahydroisoquinoline 3 was identified as a lead having low clearance in rats (CLb 20 ml/min/kg). Introduction of a 7-CF3SO2O- substituent into the tetrahydroisoquinoline, followed by replacement of the biphenylamido group of 3 by a 3-indolylpropenamido group gave 31, having high D3 receptor affinity (pKi 8.4) and 150 fold selectivity over the D2 receptor.
تدمد: 0960-894X
URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b409ae35488b0a4c092134fb6317a812
https://doi.org/10.1016/s0960-894x(98)00699-4
حقوق: CLOSED
رقم الأكسشن: edsair.doi.dedup.....b409ae35488b0a4c092134fb6317a812
قاعدة البيانات: OpenAIRE
الوصف
تدمد:0960894X