α_1-Adrenoceptor Reagents. Synthesis of Some 5,6,11,11a-Tetrahydro-1H-imidazo[1', 5' : 1,6]pyrido and 5,6,11,11b-Tetrahydro-1H-imidazo-[1', 5' : 1,2]pyrido[3,4-b]indole-1,3(2H)-diones

スポンサーリンク

概要

• 論文の詳細を見る

• Several 2-substituted 5,6,11,11a-tetrahydro-1H-imidazo[1', 5' : 1,6]pyrido (1) and 5,6,11,11b-tetrahydro-1H-imidazo[1', 5' : 1,2]pyrido[3,4-b]indole-1,3(2H)-diones (2) were synthesized and studied by 2D-NMR spectroscopy and difference nuclear Overhauser effect experiments. All the compounds were evaluated for in vitro α_1 adrenoceptor affinity by radioligand receptor binding assays. The most active derivative in displacement of [^3H]prazosin from rat cortical membranes was 1b (K_i=219 nM). At 1 μM concentration, compounds 1 and 2 had no effect on the benzodiazepine or 5-HT_<1A> receptor. The biological activity profile of 1b makes it a possible lead compound for the design of new selective α_1 adrenoceptor ligands.

• 公益社団法人日本薬学会の論文
• 1995-06-15

著者

• Morcillo M

  Univ. Nacional De Educacion A Distancia Madrid Esp

• Morcillo M.

  Facultad De Ciencias Quimicas Universidad Nacional De Educacion A Distancia

• LOPEZ-RODRIGUEZ Maria

  Departmento de Quimica Organica I, Facultad de Ciencias Quimicas, Universidad Complutense

• MORCILLO M.Jose

  Facultad de Ciencias Quimicas, Universidad Nacional de Educacion a Distancia

• BENHAMU Bellinda

  Departmento de Quimica Organica I, Facultad de Ciencias Quimicas, Universidad Complutense

• FERNANDEZ Esther

  Departmento de Quimica Organica I, Facultad de Ciencias Quimicas, Universidad Complutense

• SERRANO Jorge

  Departmento de Quimica Organica I, Facultad de Ciencias Quimicas, Universidad Complutense

• ORENSANZ Luis

  Departamento de Investigation, Hospital Ramon y Cajal

• Lopez-rodriguez Maria

  Departmento De Quimica Organica I Facultad De Ciencias Quimicas Universidad Complutense

• Orensanz Luis

  Departamento De Investigation Hospital Ramon Y Cajal

• Fernandez Esther

  Departmento De Quimica Organica I Facultad De Ciencias Quimicas Universidad Complutense

• Serrano Jorge

  Departmento De Quimica Organica I Facultad De Ciencias Quimicas Universidad Complutense

• Benhamu Bellinda

  Departmento De Quimica Organica I Facultad De Ciencias Quimicas Universidad Complutense

関連論文

• Synthesis, Structure and Cytostatic Activity of a Series of N-Substituted 3,4-Diphenyl-1H-pyrrole-2,5-diones
• Reaction of 4-(Benzoylaminomethyl)pyridine 1-Oxides with Indan-1,3-dione in the Presence of Acetic Anhydride
• α_1-Adrenoceptor Reagents. Synthesis of Some 5,6,11,11a-Tetrahydro-1H-imidazo[1', 5' : 1,6]pyrido and 5,6,11,11b-Tetrahydro-1H-imidazo-[1', 5' : 1,2]pyrido[3,4-b]indole-1,3(2H)-diones
• Reaction of 6-Hydroxytetrahydro-β-carboline-3-carboxylic Acids with Isocyanates and Isothiocyanates

スポンサーリンク