Study of μ- and δ-Opioid Activities in Agents with Various κ-Receptor Selectivity
- Authors: Grechko O.Y.1, Litvinov R.A.1, Spasov A.A.1,2, Rashchenko A.I.1, Shtareva D.M.1, Anisimova V.A.3, Minkin V.I.3
-
Affiliations:
- Volgograd State Medical University
- Volgograd Medical Research Center
- Research Institute of Physical and Organic Chemistry, Southern Federal University
- Issue: Vol 162, No 5 (2017)
- Pages: 632-635
- Section: Pharmacology and Toxicology
- URL: https://journals.rcsi.science/0007-4888/article/view/238420
- DOI: https://doi.org/10.1007/s10517-017-3674-5
- ID: 238420
Cite item
Abstract
A putative opioid agonist RU-1205 was ineffective within in vitro model of electrically induced contractions of rat ileum assessing the μ- and δ-opioid receptor pathways, while morphine inhibited these contractions in a dose-dependent and naloxone-reversible manners with EC50=2.6×10—7 M. In vivo experiments revealed no significant effects of RU-1205 on respiration and gastrointestinal tract contractile activity. In contrast, butorphanol decreased respiration rate by 25% (25-100 mg/kg) and slowed down the transit of labeled particles along the small intestine by 77.1% (1 mg/kg) and by 45.5% (10 mg/kg). Morphine-induced inhibition of peristalsis was dose-dependent with maximum effect (by 68.6%) observed in the dose of 10 mg/kg. It was concluded that the effects of RU-1205 are not related to activation μ- and δ-opioid receptors known to mediate the effects of non-selective opioid agonist morphine and agonist-antagonist butorphanol.
About the authors
O. Yu. Grechko
Volgograd State Medical University
Email: litvinov.volggmu@mail.ru
Russian Federation, Volgograd
R. A. Litvinov
Volgograd State Medical University
Author for correspondence.
Email: litvinov.volggmu@mail.ru
Russian Federation, Volgograd
A. A. Spasov
Volgograd State Medical University; Volgograd Medical Research Center
Email: litvinov.volggmu@mail.ru
Russian Federation, Volgograd; Volgograd
A. I. Rashchenko
Volgograd State Medical University
Email: litvinov.volggmu@mail.ru
Russian Federation, Volgograd
D. M. Shtareva
Volgograd State Medical University
Email: litvinov.volggmu@mail.ru
Russian Federation, Volgograd
V. A. Anisimova
Research Institute of Physical and Organic Chemistry, Southern Federal University
Email: litvinov.volggmu@mail.ru
Russian Federation, Rostov-on-Don
V. I. Minkin
Research Institute of Physical and Organic Chemistry, Southern Federal University
Email: litvinov.volggmu@mail.ru
Russian Federation, Rostov-on-Don