Topic
Arecoline
About: Arecoline is a research topic. Over the lifetime, 744 publications have been published within this topic receiving 16015 citations. The topic is also known as: methylarecaiden & methylarecaidin.
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TL;DR: The agonist profile of the Ascaris muscle cell ACh receptor clearly indicates that it is Nicotinic, and the potency of ganglionic and neuromuscular nicotinic receptor antagonists in As Caris does not enable a further subclassification of this nicotinics receptor.
Abstract: 1. 1. Acetylcholine (ACh) elicited depolarization and an increase in input conductance of the somatic muscle cells of the parasitic nematode Ascaris suum .
2. 2. The relative potency of nicotinic and muscarinic agents was studied in this preparation. The order of potency of these compounds was metahydroxyphenylpropyltrimethylammonium (HPPT)> 1,1 dimethyl-4-phenylpiperazinium>(DMPP)> ACh> carbachol> nicotine> tetramethylammonium (TMA+)> muscarone> furtrethonium> arecoline. Decamethonium was also a weak agonist. McN-A-343 elicited a very weak depolarization at concentrations above 1 mmoll−1. Bethanechol and methacholine were without effect up to 1 mmoll−1. Pilocarpine and muscarine elicited a slight hyperpolarization of up to 3 mV with a threshold for the response of around 500 μmoll−1. Oxotremorine (1 mmoll−1) was without effect.
3. 3. The nitromethylene insecticide 2(nitromethylene)tetrahydro 1,3-thiazine (NMTHT), an agonist at insect nicotinic receptors, was without effect on Ascaris muscle cells up to 1 mmoll−1.
4. 4. Mecamylamine and benzoquinonium were the most potent antagonists of the acetylcholine response. The order of potency of the other antagonists was tetraphenylphosphonium (TPP) > quinacrine > pancuronium, curare> trimethaphan> atropine chlorisondamine, decamethonium > hexamethonium > dihydro-/3-ery throidine.
5. 5. The agonist profile of the Ascaris muscle cell ACh receptor clearly indicates that it is nicotinic. The potency of ganglionic and neuromuscular nicotinic receptor antagonists in Ascaris does not enable a further subclassification of this nicotinic receptor. The Ascaris nicotinic receptor seems to possess some of the pharmacological properties of each type of vertebrate nicotinic receptor. The pharmacology of the Ascaris nicotinic receptor is discussed in relation to that of nicotinic receptors in other invertebrate preparations and in vertebrate preparations.
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76 citations
TL;DR: Arecoline appears to be a compound suitable to selectively evaluate the responsiveness of the central component of the HPA axis and that this effect is mediated mainly by the release of endogenous CRH.
Abstract: Several lines of experimental evidence suggest that acetylcholine and other cholinergic agonists are excitatory to the hypothalamic-pituitary-adrenal (HPA) axis. To examine the site on the HPA axis that is stimulated by cholinergic agents, we evaluated the in vivo and in vitro effects of the muscarinic cholinergic agonist arecoline in intact and pituitary stalk-transected rats as well as on isolated rat hypothalami, dispersed anterior pituicytes, and adrenocortical cells in culture. Arecoline, injected iv to catheterized, freely moving male Sprague-Dawley rats, stimulated plasma ACTH and corticosterone release in a dose-dependent fashion. The muscarinic cholinergic antagonist atropine significantly blunted the ACTH response to arecoline. Pituitary stalk transection led to diminished plasma ACTH and corticosterone responses to arecoline. Similarly, previous administration of anti-CRH serum significantly blunted these responses. These findings suggest that arecoline stimulates the HPA axis centrally, mainly via secretion of CRH. This hypothesis was confirmed by the dose-dependent ability of arecoline to cause hypothalamic CRH secretion in vitro, an effect antagonized by atropine, and its failure to elicit ACTH and corticosterone secretion by dispersed anterior pituicytes and adrenocortical cells in culture, respectively. These data suggest that the muscarinic cholinergic agonist arecoline stimulates the HPA axis in the rat and that this effect is mediated mainly by the release of endogenous CRH. Arecoline, therefore, appears to be a compound suitable to selectively evaluate the responsiveness of the central component of the HPA axis.
76 citations
TL;DR: It is suggested that muscarinic receptors in the nucleus accumbens can control immobility in the Porsolt swim test.
76 citations
TL;DR: A capillary zone electrophoretic method for the rapid analysis of the major alkaloids (arecoline and guavacoline) in areca nut extract is described and is applicable to the analysis of alkaloid in the nut, commercial preparations and in the saliva of areca Nut chewers.
Abstract: A capillary zone electrophoretic (CZE) method for the rapid analysis of the major alkaloids (arecoline and guavacoline) in areca nut extract is described. Areca nuts were pulverized and then extracted with water by sonication in a water bath. After centrifugation, the supernatant was analysed on a fused-silica capillary with 100 mM ammonium acetate-acetic acid (pH 4.6) as the running buffer at a voltage of 20 kV and temperature of 30 degrees C. The method is applicable to the analysis of alkaloids in the nut, commercial preparations (pan masala) and in the saliva of areca nut chewers.
75 citations
TL;DR: It is concluded that arecoline attacks multiple targets to finally generate systemic toxicity in mice and caused depression of antioxidants, i.e., superoxide dismutase (SOD), catalase, reduced glutathione (GSH) and glutATHione-S-transferase (GST) that are known to neutralize reactive oxygen species.
75 citations