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Sigma receptor activation does not mediate fentanyl-induced attenuation of muscarinic coronary contraction.
- Source :
-
Anesthesia and analgesia [Anesth Analg] 1996 May; Vol. 82 (5), pp. 982-7. - Publication Year :
- 1996
-
Abstract
- Our overall goal was to investigate the mechanism by which fentanyl attenuates acetylcholine-induced contraction in porcine coronary artery. We tested the hypothesis that fentanyl attenuates muscarinic coronary contraction via sigma receptor activation. Left coronary artery vascular rings were isolated from porcine hearts and were suspended in organ chambers for isometric tension recording. In untreated coronary vascular rings, acetylcholine administration resulted in dose-dependent contraction. Fentanyl attenuated acetylcholine-induced contraction. The sigma ligands--(+)-pentazocine, (+)-cyclazocine, haloperidol, and 1,3-di-o-tolylguanidine--also inhibited acetylcholine-induced contraction. In contrast, the selective sigma ligand, (+)-3-(3-hydroxyphenyl)-N-(1-propyl) piperidine failed to have an inhibitory effect on acetylcholine-induced contraction. Moreover, metaphit (1-[1(3-isothiocyanatophenyl)cyclohexyl]piperidine), which causes irreversible acylation of sigma receptors, only inhibited acetylcholine-induced contraction when it was present in the organ chamber. We also assessed the effects of inhibiting various points in the signal transduction pathway distal to naloxone-sensitive opioid receptor activation on acetylcholine-induced contraction. Selective (glybenclamide) and nonselective (tetraethylammonium) K(+)-channel inhibition, guanosine triphosphate-binding protein inactivation (pertussis toxin), and Type 1 and Type 2 dopamine receptor inhibition all failed to alter the attenuating effect of fentanyl on acetylcholine-induced contraction. Thus, neither sigma or opioid receptor activation is a prerequisite for fentanyl-induced inhibition of muscarinic coronary contraction.
- Subjects :
- Acetylcholine administration & dosage
Acetylcholine pharmacology
Anesthetics, Intravenous administration & dosage
Animals
Cyclazocine pharmacology
Dopamine Agonists pharmacology
Dopamine Antagonists pharmacology
Dose-Response Relationship, Drug
Excitatory Amino Acid Antagonists pharmacology
Fentanyl administration & dosage
Guanidines pharmacology
Haloperidol pharmacology
Muscarine administration & dosage
Muscarinic Agonists administration & dosage
Narcotic Antagonists pharmacology
Narcotics administration & dosage
Pentazocine pharmacology
Phencyclidine analogs & derivatives
Phencyclidine pharmacology
Piperidines pharmacology
Potassium Channel Blockers
Receptors, Dopamine drug effects
Receptors, sigma drug effects
Signal Transduction drug effects
Swine
Vasoconstrictor Agents administration & dosage
Vasodilator Agents pharmacology
Anesthetics, Intravenous pharmacology
Coronary Vessels drug effects
Fentanyl pharmacology
Muscarine pharmacology
Muscarinic Agonists pharmacology
Narcotics pharmacology
Receptors, sigma physiology
Vasoconstriction drug effects
Vasoconstrictor Agents pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0003-2999
- Volume :
- 82
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Anesthesia and analgesia
- Publication Type :
- Academic Journal
- Accession number :
- 8610910
- Full Text :
- https://doi.org/10.1097/00000539-199605000-00016