N-(arylpiperazinyl)butylimides of bicyclo [2.2.1]gept-5-en-endo-endo-2, 3-dicarbonic acid – ligands of 5-ht1a and d2 receptors, their neurotropic properties

Authors

  • S. A. Andronati Physico-Chemical Institute. AV Bogatsky National Academy of Sciences of Ukraine, Ukraine
  • T. L. Karasyova Physico-Chemical Institute. AV Bogatsky National Academy of Sciences of Ukraine, Ukraine
  • A. V. Zamkova Physico-Chemical Institute. AV Bogatsky National Academy of Sciences of Ukraine, Ukraine
  • S. G. Soboleva Odessa National University. I. I. Mechnikov, Ukraine
  • I. A. Boyko Physico-Chemical Institute. AV Bogatsky National Academy of Sciences of Ukraine, Ukraine
  • L. I. Kasyan Dnepropetrovsk National University. O. Gonchara, Ukraine
  • D. I. Tsimbal Physico-Chemical Institute. AV Bogatsky National Academy of Sciences of Ukraine, Ukraine

DOI:

https://doi.org/10.24959/ophcj.13.775

Keywords:

arylpiperazines, norbornene fragment, affinity, D2.and 5-HT1A receptors, antipsychotic and anxiolytic properties

Abstract

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.

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Published

2013-12-02

How to Cite

(1)
Andronati, S. A.; Karasyova, T. L.; Zamkova, A. V.; Soboleva, S. G.; Boyko, I. A.; Kasyan, L. I.; Tsimbal, D. I. N-(arylpiperazinyl)butylimides of Bicyclo [2.2.1]gept-5-En-Endo-Endo-2, 3-Dicarbonic Acid – Ligands of 5-ht1a and D2 Receptors, Their Neurotropic Properties. J. Org. Pharm. Chem. 2013, 11, 72-76.

Issue

Vol. 11 No. 4(44) (2013)

Section

Original Researches

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