RU-1205

Last updated

RU-1205
RU-1205.svg
Identifiers
  • 4-[2-[2-(4-fluorophenyl)imidazo[1,2-a]benzimidazol-4-yl]ethyl]morpholine
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
Formula C21H21FN4O
Molar mass 364.424 g·mol−1
3D model (JSmol)
  • C1COCCN1CCN2C3=CC=CC=C3N4C2=NC(=C4)C5=CC=C(C=C5)F
  • InChI=1S/C21H21FN4O/c22-17-7-5-16(6-8-17)18-15-26-20-4-2-1-3-19(20)25(21(26)23-18)10-9-24-11-13-27-14-12-24/h1-8,15H,9-14H2
  • Key:VRTSZUQZRYFXJK-UHFFFAOYSA-N

RU-1205 is a kappa opioid receptor agonist used for pain treatment. It has high bioavailability (44.17 and 56.03% upon peroral and subcutaneous introduction). [1]

Granulated RU-1205 produced maximum analgesic effect within 4-h investigation and retained higher analgesic activity compared to that of parent substance. [2]

RU-1205 does not cause side effects typical of morphine and butorphanol including the development of withdrawal syndrome upon naloxone provocation and tolerance to analgesic activity upon 14-day administration. [3]

See also

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References

  1. Spasov AA, Smirnova LA, Rashchenko AI, Kuznetsov KA, Anisimova VA (2014). "[The absolute bioavailability of benzimidazole derivative RU-1205 in rats]". Eksperimental'naia i Klinicheskaia Farmakologiia. 77 (1): 17–19. PMID   24649597.
  2. Spasov AA, Smirnova LA, Grechko OI, Rashchenko AI, Shtareva DM, Anisimova VA (2014). "[Pharmacokinetic and analgesic properties of tabletized dosage form of RU-1205-new imidazobenzimidazole derivative with kappa agonist activity]". Eksperimental'naia i Klinicheskaia Farmakologiia. 77 (7): 27–30. PMID   25322651.
  3. Grechko OY, Shtareva DM, Spasov AA, Litvinov LA, Rashchenko AI (August 2016). "Studying the Physical Dependence on and Tolerance to the Antinociceptive Effect of Ru-1205 Substance". Eksperimental'naia i Klinicheskaia Farmakologiia. 79 (4): 8–11. PMID   29949697.