Mokrosz J L, Dereń-Wesołek A, Tatarczyńska E, Duszyńska B, Bojarski A J, Mokrosz M J, Chojnacka-Wójcik E
Department of Medicinal Chemistry, Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland.
J Med Chem. 1996 Mar 1;39(5):1125-9. doi: 10.1021/jm950662c.
A new analog of buspirone (1), i.e., 8-[4-[2-(1,2,3,4-tetrahydroisoquinolinyl)]butyl]-8-azaspiro- [4.5]decane-7,9-dione (6a), was synthesized. In was demonstrated that buspirone and its analog 6a were equipotent 5-HT(1A) ligands. Several behavioral models showed that 6a had essentially the same functional profile at 5-HT(1A) receptors as buspirone. The obtained results permit a conclusion that the basic nitrogen atom and terminal, bulky cycloimide moiety, but not the 2-pyrimidinyl group, of buspirone are directly involved in the formation of the bioactive complex with 5-Ht1A receptors.
合成了丁螺环酮（1）的一种新类似物，即8-[4-[2-(1,2,3,4-四氢异喹啉基)]丁基]-8-氮杂螺[4.5]癸烷-7,9-二酮（6a）。已证明丁螺环酮及其类似物6a是等效的5-HT(1A)配体。多个行为学模型表明，6a在5-HT(1A)受体上具有与丁螺环酮基本相同的功能特征。所得结果表明，丁螺环酮的碱性氮原子和末端庞大的环酰亚胺部分，而非2-嘧啶基，直接参与与5-Ht1A受体形成生物活性复合物。
