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Draft:RU-1205

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RU-1205
Identifiers
PubChem CID
ChemSpider
Chemical and physical data
FormulaC21H21FN4O
Molar mass364.424 g·mol−1
3D model (JSmol)
  • C1COCCN1CCN2C3=CC=CC=C3N4C2=NC(=C4)C5=CC=C(C=C5)F

RU-1205 is a kappa opioid receptor (KOR) agonist with analgesic utility in treatment of pain. It was six times the potency of butorphanol.[1]

RU-1205 substance has high bioavailability (44.17 and 56.03% upon peroral and subcutaneous introduction).[2]

Granulated RU-1205 produced maximum analgesic effect (138.8% relative to control) within 4-h investigation and retained higher analgesic activity compared to that of parent substance (on the average by 58%, p < 0.05) up to 12 h.[3]

It is established that this compound 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.[4]

See also

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References

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  1. ^ Spasov AA, Grechko OIu, Shtareva DM, Anisimova VA. [Analgesic properties of morpholinoethylimidazobenzimidazole derivative RU-1205]. Eksp Klin Farmakol. 2013;76(9):15-8. Russian. PMID: 24432563.
  2. ^ Spasov AA, Smirnova LA, Rashchenko AI, Kuznetsov KA, Anisimova VA. [The absolute bioavailability of benzimidazole derivative RU-1205 in rats]. Eksp Klin Farmakol. 2014;77(1):17-9. Russian. PMID: 24649597.
  3. ^ Spasov AA, Smirnova LA, Grechko OIu, Rashchenko AI, Shtareva DM, Anisimova VA. [Pharmacokinetic and analgesic properties of tabletized dosage form of RU-1205-new imidazobenzimidazole derivative with kappa agonist activity]. Eksp Klin Farmakol. 2014;77(7):27-30. Russian. PMID: 25322651.
  4. ^ Grechko OY, Shtareva DM, Spasov AA, Litvinov LA, Rashchenko AI. STUDYING THE PHYSICAL DEPENDENCE ON AND TOLERANCE TO THE ANTINOCICEPTIVE EFFECT OF RU-1205 SUBSTANCE. Eksp Klin Farmakol. 2016 Aug;79(4):8-11. English, Russian. PMID: 29949697.