Analgesic Activity of Hexaazaisowurtzitane Derivatives.

Abstract

Pronounced analgesic activity of the innovative compound 4-(3,4-dibromthiophencarbonyl)-2,6,8,12-tetraacethyl-2,4,6,8,10,12hexaazatetracyclo[5,5,0,03, 11,05, 9] dodecane (thiowurtzine) was observed in the thermal nociceptive hot plate test and in the acute visceral and somatic deep pain model (acetic acid writhing test). In these experimental models, naloxone-sensitive thiowurtzine-induced analgesia was revealed. The absence of tropism to peripheral opioid receptors in the acetic acid writhing test was demonstrated using naloxone methiodide. Course administration of low-toxic thiowurtzine in effective doses was not associated with ulcerogenic damage to the gastric mucosa in experimental animals.

• Authors: S G Krylova, T N Povet'eva, E P Zueva, N I Suslov, E N Amosova, T G Razina, K A Lopatina, O Yu Rybalkina, Yu V Nesterova, O G Afanas'eva, E A Kiseleva, S V Sysolyatin, D A Kulagina, V V Zhdanov
• Journal: Bulletin of experimental biology and medicine (Bull Exp Biol Med) Vol. 166 Issue 4 Pg. 461-465 (Feb 2019) ISSN: 1573-8221 [Electronic] United States
• PMID: 30788739 (Publication Type: Journal Article)

Chemical References

• Analgesics
• Naloxone

Topics

• Analgesics (therapeutic use)
• Animals
• Disease Models, Animal
• Gastric Mucosa (drug effects)
• Male
• Mice
• Naloxone (therapeutic use)
• Pain (drug therapy, physiopathology)
• Pain Measurement (methods)