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Structure-activity relationships of 2-aminotetralins and 2-aminoindanes: inhibitory neuroeffector mechanisms in isolated guinea-pig ilea.
- Source :
-
Archives internationales de pharmacodynamie et de therapie [Arch Int Pharmacodyn Ther] 1982 Jul; Vol. 258 (1), pp. 84-99. - Publication Year :
- 1982
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Abstract
- The ability of 2-aminotetralins (2-ATs), 2-aminoindanes (2-AIs), morphine (M) and clonidine (CLON) to alter neuroeffector transmission was studied on field-stimulated (FS) guinea-pig ilea (GPI). The activity of these compounds to inhibit K+, histamine (H), actylcholine (ACh), nicotine (Nic) and serotonin (5-HT) induced contractions was determined using superfused GPI segments. 2-ATs, 2-AIs, M and CLON dose-dependently inhibited contractions produced by low frequency stimulation through alpha-adrenergic, opioid or unknown receptor mediated mechanisms. 2-ATs inhibited ACh, Nic, 5-HT and FS, but not K+- or H-induced contractions. 2-ATs, 2-Ais and M were more potent than hexamethonium in inhibiting Nic-induced contractures. 2-AT and 2-AI-induced inhibition was not antagonized by naloxone or phentolamine. However, the inhibitory effects of 2-ATs. 2-AIs and M on FS-GPI were antagonized by increasing the concentration of Ca2+ ion in the media. These data are consistent with the supposition that 2-ATs, 2-AIs or M alter neuroeffector transmission through competitive changes in Ca2+ disposition in cholinergic neurons of guinea-pig isolated ilea. A discussion relating other biological actions of 2-ATs or 2-AIs (e.g. alpha-adrenergic mediated antinociception) to the observed inhibitory neuroeffector responses is provided.
- Subjects :
- Acetylcholine antagonists & inhibitors
Animals
Electric Stimulation
Guinea Pigs
Histamine Antagonists pharmacology
Ileum drug effects
In Vitro Techniques
Male
Muscle Contraction drug effects
Nicotine antagonists & inhibitors
Potassium antagonists & inhibitors
Serotonin Antagonists pharmacology
Structure-Activity Relationship
Ileum innervation
Indans pharmacology
Indenes pharmacology
Muscle, Smooth drug effects
Naphthalenes pharmacology
Neuroeffector Junction drug effects
Tetrahydronaphthalenes pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0003-9780
- Volume :
- 258
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Archives internationales de pharmacodynamie et de therapie
- Publication Type :
- Academic Journal
- Accession number :
- 7138147