The effect of coniine on presynaptic nicotinic receptors
-
Ulkem Erkent
,
Rustu Onur
Abstract
Toxicity of coniine, an alkaloid of Conium maculatum (poison hemlock), is manifested by characteristic nicotinic clinical signs including excitement, depression, hypermetria, seizures, opisthotonos via postsynaptic nicotinic receptors. There is limited knowledge about the role of presynaptic nicotinic receptors on the pharmacological and toxicological effects of coniine in the literature. The present study was undertaken to evaluate the possible role of presynaptic nicotinic receptors on the pharmacological and toxicological effects of coniine. For this purpose, the rat anococcygeus muscle and guinea-pig atria were used in vitro. Nicotine (100 μM) elicited a biphasic response composed of a relaxation followed by contraction through the activation of nitrergic and noradrenergic nerve terminals in the phenylephrine-contracted rat anococcygeus muscle. Coniine inhibited both the nitrergic and noradrenergic response in the muscle (–logIC50 = 3.79 ± 0.11 and –logIC50 = 4.57 ± 0.12 M, respectively). The effect of coniine on nicotinic receptor-mediated noradrenergic transmission was also evaluated in the guinea-pig atrium (–logIC50 = 4.47 ± 0.12 M) and did not differ from the –logIC50 value obtained in the rat anococcygeus muscle. This study demonstrated that coniine exerts inhibitory effects on nicotinic receptor-mediated nitrergic and noradrenergic transmitter response.
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©2016 by De Gruyter
Articles in the same Issue
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Articles in the same Issue
- Frontmatter
- Editorial
- ZNC opens a new chapter focussing on the emerging field of natural and natural-like compounds
- Research Articles
- Design, synthesis and evaluation of antitumor activity of new rotundic acid acylhydrazone derivatives
- Synthesis and in vitro anti-HIV-1 activity of a series of N-arylsulfonyl-3-propionylindoles
- Jaspiferin G, a new isomalabaricane-type triterpenoid from the sponge Jaspis stellifera
- The effect of coniine on presynaptic nicotinic receptors
- Nematicidal effect of plumbagin on Caenorhabditis elegans: a model for testing a nematicidal drug
- Synthesis and biological evaluation of novel pyrimidines derived from 6-aryl-5-cyano-2-thiouracil
- Phytochemical investigation of the bioactive extracts of the leaves of Ficus cyathistipula Warb.
- Chemical composition and biological activity of the essential oil from Thymus lanceolatus
- Ascidian bioresources: common and variant chemical compositions and exploitation strategy – examples of Halocynthia roretzi, Styela plicata, Ascidia sp. and Ciona intestinalis
- Structural and evolutionary relationships among RuBisCOs inferred from their large and small subunits
