Kolocouris N, Fytas G, Foscolos G B, Kalliteraki I, Vamvakides A
Université d'Athènes, Département de Pharmacie, Division de Chimie Pharmaceutique, Panepistimioupoli Zografou, Athènes, Grèce.
Boll Chim Farm. 1994 Sep;133(8):516-20.
This paper describes the synthesis of alpha-(dimethylaminoethyl)-gamma, gamma-diphenyl-gamma-butyrolactone 4. The study of convulsions induced, on mice, by this compound could show the existence of antiGABAergic and cholinergic action components, but, unlike the homologous alpha- (dialkylaminomethil)-gamma-butyrolactones (with one -CH2- less on the aminoalkyl chain), no antiglycinergic component was detected. The effects of atropine on the aminolactone 4 induced convulsions (antagonism 5mn and synergy 30 mn after atropine) could suggest an activation of the glutamatergic receptors (NMDA), by indirect stimulation of their glycinergic site, by the aminolactone 4.
本文描述了α-（二甲基氨基乙基）-γ，γ-二苯基-γ-丁内酯4的合成。对该化合物诱发小鼠惊厥的研究表明，存在抗GABA能和胆碱能作用成分，但与同源的α-（二烷基氨基甲基）-γ-丁内酯（氨基烷基链上少一个-CH2-）不同，未检测到抗甘氨酸能成分。阿托品对氨基内酯4诱发惊厥的影响（阿托品给药后5分钟拮抗，30分钟协同）可能表明，氨基内酯4通过间接刺激甘氨酸能位点，激活了谷氨酸能受体（NMDA）。
