RU-1205

RU-1205
Identifiers
	IUPAC name 4-[2-[2-(4-fluorophenyl)imidazo[1,2-a]benzimidazol-4-yl]ethyl]morpholine;
PubChem CID	4641302;
ChemSpider	3831213;
Chemical and physical data
Formula	C21H21FN4O
Molar mass	364.424 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1COCCN1CCN2C3=CC=CC=C3N4C2=NC(=C4)C5=CC=C(C=C5)F;
	InChI 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]

References

^ 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): 17–9. PMID 24649597.
^ Spasov, AA; Smirnova, LA; Grechko, OIu; 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.
^ 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.

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[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): 17–9. PMID 24649597.

[2] Spasov, AA; Smirnova, LA; Grechko, OIu; 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.

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See also

References