Ліганди 5-нт1а та d2 рецепторів – n-(арилпіперазиніл)бутиліміди біцикло[2.2.1]гепт-5-ен- ендо-ендо-2,3-дикарбонової кислоти та їх нейротропні властивості

• Main Authors: Andronati, S. A., Karasyova, T. L., Zamkova, A. V., Soboleva, S. G., Boyko, I. A., Kasyan, L. I., Tsimbal, D. I.
• Format: Article
• Language: Russian
• Published: National University of Pharmacy 2013
• Subjects: arylpiperazines; norbornene fragment; affinity; D2.and 5-HT1A receptors; antipsychotic and anxiolytic properties; UDC 615.214.22; 547.75; арилпиперазины; норборненовый фрагмент; аффинитет; D2 и 5 -НТ1А рецепторы; антипсихотические и анксиолитические свойства; УДК 615.214.22; арилпіперазини; норборненовий фрагмент; афінітет; D2 та 5-НТ1А рецептори; анти- психотичні та анксіолітичні властивості
• Online Access: https://ophcj.nuph.edu.ua/article/view/ophcj.13.775

It is known that hetaryl(aryl)piperazines possess important neuropharmacological (anxiolytic, antidepressant, neuroleptic, etc.) properties. In the process of studying the relationship between the structure and properties of N-(arylpiperazinyl) butylimides bicyclo[2.2.1]gept-5-en-endo-endo-2,3-dicarbonic acid (compounds 1-5) the neuropharmacological properties and their affinity for D2 and 5-HT1A receptors have been studied in this work. It has been determined by the radioligands method that arylpiperazines 1-5 possess the high affinity for D2 and 5-HT1A receptors. Compounds 1-5 have been found to have the marked sedative and neuroleptic properties. The compounds (1-5) synthesized revealed a dose-dependent pharmacological effect. In lower doses (5 mg/kg) on the model of the conflict test in rats m-tolyl derivatives had the same anxiolytic effect as buspirone (10 mg/kg); in higher doses (10 mg/kg) all compounds revealed the neuroleptic activity on the model of “Waxy flexibility” catalepsy induction. Compounds of this series in the dose of 10 mg/kg reduced the apomorphine-induced stereotypic behaviour by 33.7-86.5% in rats, as well as a refrence drug haloperidol. All of these compounds are nontoxic, the value of their LD50 ≥ 300 mg/kg.