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Analgesic and Psychotropic Effects of a New Bradykinin Antagonist

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Bulletin of Experimental Biology and Medicine Aims and scope

A bradykinin B1 receptors antagonist PAV-0056, an 1,4-benzodiazepin-2-one derivative, intragastrically administrated to mice at doses of 0.1 and 1 mg/kg causes analgesia in the “formalin test” not inferior to that of diclofenac sodium (10 mg/kg) and tramadol (20 mg/kg). PAV-0056 at doses of 0.1 and 10 mg/kg has no anxiolytic and central muscle relaxant effects in mice and does not damage the gastric mucosa in rats. Based on the results of the conditioned place preference test, PAV-0056 also does not induce addiction in mice.

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References

  1. Gonçalves ECD, Vieira G, Gonçalves TR, Simões RR, Brusco I, Oliveira SM, Calixto JB, Cola M, Santos ARS, Dutra RC. Bradykinin receptors play a critical role in the chronic post-ischaemia pain model. Cell Mol. Neurobiol. 2021;41(1):63-78. doi: https://doi.org/10.1007/s10571-020-00832-3

    Article  PubMed  Google Scholar 

  2. Litvitsky PP. Inflammation. Vopr. Sovrem. Pediatr. 2006;5(4):75-81. Russian.

  3. Marceau F, Bachelard H, Bouthillier J, Fortin JP, Morissette G, Bawolak MT, Charest-Morin X, Gera L. Bradykinin receptors: Agonists, antagonists, expression, signaling, and adaptation to sustained stimulation. Int. Immunopharmacol. 2020;82:106305. doi: https://doi.org/10.1016/j.intimp.2020.106305

    Article  CAS  PubMed  Google Scholar 

  4. Andronati SA, Pavlovsky VI, Golovenko MYa, Reder AS, Larionov VB, Valivodz’ IP. Synthesis and extraction efficiency from biological fluids of [214C]Propoxazepam: a potent analgesic with multifunctional mechanism of action. JCBPS. Section A. 2019;9(4):323-333. doi: https://doi.org/10.24214/jcbps.A.9.4.32333

  5. Pavlovskij VI, Khazanov VA, Stankevich SA. Patent RU No. 2701557. 1,4-Benzodiazepin-2-one derivatives and use thereof. Bull. No. 15. Published September 30, 2019.

  6. Hasani A, Soljakova M, Jakupi M, Ustalar-Ozgen S. Preemptive analgesic effects of midazolam and diclofenac in rat model. Bosn. J. Basic Med. Sci. 2011;11(2):113-118. doi: https://doi.org/10.17305/bjbms.2011.2593

    Article  CAS  PubMed  PubMed Central  Google Scholar 

  7. Bandapati S, Podila KS, Yadala VR. Comparative study of anti-nociceptive effect of venlafaxine with tramadol by tail-flick test in animal model of mice. Natl J. Physiol. Pharm. Pharmacol. 2021;11(6):633-637. doi: https://doi.org/10.5455/njppp.2021.11.11307202001022021

    Article  CAS  Google Scholar 

  8. Manual for Preclinical Studies of New Pharmacological Substances. Mironov AN, ed. Moscow, 2012. Russian.

  9. Molodavkin GM, Voronina TA, Chernyavskaya LI, Burlakova EB, Khorseva NI, Seredenin SB. Pharmacological activity of phenazepam and flunitrazepam in ultralow doses. Bull. Exp. Biol. Med. 2003;135(Suppl. 7):39-41. doi: https://doi.org/10.1023/a:1024710225445

    Article  PubMed  Google Scholar 

  10. Shi Z, Pan S, Wang L, Li S. Oleanolic acid attenuates morphine withdrawal symptoms in rodents: association with regulation of dopamine function. Drug Des. Devel. Ther. 2021;15:3685-3696. doi: https://doi.org/10.2147/DDDT.S326583

    Article  PubMed  PubMed Central  Google Scholar 

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Correspondence to V. V. Bykov.

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Translated from Byulleten’ Eksperimental’noi Biologii i Meditsiny, Vol. 176, No. 11, pp. 595-599, November, 2023

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Aliforenko, A.E., Motov, V.S., Bykov, V.V. et al. Analgesic and Psychotropic Effects of a New Bradykinin Antagonist. Bull Exp Biol Med 176, 581–584 (2024). https://doi.org/10.1007/s10517-024-06071-6

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  • DOI: https://doi.org/10.1007/s10517-024-06071-6

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