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ISSN 2522-9028 (Print)
ISSN 2522-9036 (Online)
DOI: https://doi.org/10.15407/fz

Fiziologichnyi Zhurnal

is a scientific journal issued by the

Bogomoletz Institute of Physiology
National Academy of Sciences of Ukraine

Editor-in-chief: V.F. Sagach

The journal was founded in 1955 as
1955 – 1977 "Fiziolohichnyi zhurnal" (ISSN 0015 – 3311)
1978 – 1993 "Fiziologicheskii zhurnal" (ISSN 0201 – 8489)
1994 – 2016 "Fiziolohichnyi zhurnal" (ISSN 0201 – 8489)
2017 – "Fiziolohichnyi zhurnal" (ISSN 2522-9028)

Fiziol. Zh. 2003; 49(1): 23-27

Action of a phenazepam metabolite, 2-amino-5-bromo-2'-chlorobenzophenone, onglycine and nmda receptors of rat hippocampal pyramidal neurones

M. V. Kopanitsa

    Ін-т фізіології ім. О. О. Богомольця НАН України, Київ



Abstract

Action of 2-amino-5-bromo-2'-chlorobenzophenone (ABPH), a metabolite of phenazepam, on currents evoked by the activation of glycine and glutamate NMDA receptors has been investigated in enzymatically isolated hippocampal rat pyramidal neurones. It is demonstrated that 3 - 10 μM ABPH caused an inhibitory effect on glycine receptors which was more prominent after pre-incubation with the drug. Peak amplitude of NMDA receptor-mediated currents was weakly potentiated after prolonged (4-6 min) incubation with 10 μM ABPH. Thus, the effects of the benzophenone metabolites should be taken into account when analysing the action of phenazepam and other benzodiazepine drugs.

Full text: (PDF, in Ukrainian)

References

  1. Андронати С.А., Авруцкий А.В., Богатский А.В., и др. Феназепам – К.: Наук. думка, 1982. – 288 с.
  2. Врублевский С.В., Валеев А.Е., Черневская Н.И. Метод быстрой смены тестирующих растворов при исследованиях изолированных клеток // Физиол. журн. – 1985. – 31, № 2. – С. 241 – 242.
  3. Копаниця М.В., Руденко О.П. Похідні N-заміщених 2-аміно-5-галогенбензофенонів прискорюють де- сенситизацію ГАМК-активованих струмів в ізо- льованих нейронах Пуркін’є щурів // Арх. клін. експерим. медицины. – 2002. – 11, № 1. – С. 22 – 25.
  4. Bond A.J., Hailey D.M., Lader M.H. Plasma concentrations of benzodiazepines // Br. J. Clin. Pharmacol. –1977. – 4, № 1. – P. 51 – 56.
  5. Kondratskaya E.L., Lishko P.V., Chatterjee S.S., Krishtal O.A. BN52021, a platelet activating factor antagonist, is a selective blocker of glycine-gated chloride channel // Neurochem. Int. – 2002. – 40, № 7. – P. 647 – 653.
  6. Kopanitsa M.V., Lambert, J.J. Modulation of GABAA receptors by 5-bromobenzophenone derivatives depends on the presence of ?-subunit. In: Abstr. 2nd Bogomoletz-Nencki Symposium «Intracellular Signalling in Excitable Cells»,1-3 September Kyiv. – 2002. – P. 9.
  7. Kopanitsa M.V., Yakubovska L.M., Rudenko O.P., Krishtal O.A. Modulation of GABAА receptor-mediated currents by benzophenone derivatives in isolated rat Purkinjeneurones // Neuropharmacology. – 2002. – 43, № 4. –P. 764 – 777.
  8. Kopanitsa M.V., Zhuk O.V., Zinkovsky V.G., Krishtal O.A. Modulation of GABAA receptor-mediated currents by phenazepam and its metabolites // Naunyn-Schmiede- bergs Arch. Pharmacol. – 2001. – 364 , № 1. – P. 1 – 8.
  9. 9. Olfson M., Pincus H.A. Use of benzodiazepines in the community // Arch. Intern. Med. – 1994. – 154, № 11. – P. 1235 – 1240.
  10. 10. Olivier H., Fitz-Gerald M.J., Babiak B. Benzodiazepines revisited // J. La. State. Med. Soc. – 1998. – 150, № 10. – P. 483 – 485.
  11. Olsen R.W., Tobin A.J. Molecular biology of GABAA receptors // FASEB J. – 1990. – 4, № 5. – P. 1469 – 1480.
  12. Turner D.M., Sapp D.W., Olsen R.W. The benzodiazepine/alcohol antagonist Ro 15-4513: binding to a GABAAreceptor subtype that is insensitive to diazepam // J. Phar-macol. Exp. Ther. – 1991. – 257, № 3. – P. 1236 – 1242.
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