Draft:RU-1205
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Identifiers | |
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PubChem CID | |
ChemSpider | |
Chemical and physical data | |
Formula | C21H21FN4O |
Molar mass | 364.424 g·mol−1 |
3D model (JSmol) | |
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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
[edit]References
[edit]- ^ 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.
- ^ 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.
- ^ 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.
- ^ 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.