Anticholinergic effects of cis-chlorprothixene characterized in rat parotid acini
| Autor: | Mogens Undén, Steen Dissing, Birgitte Nauntofte |
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| Rok vydání: | 1989 |
| Předmět: |
Agonist
Male medicine.medical_specialty medicine.drug_class Ionophore chemistry.chemical_element Chlorprothixene Stimulation Calcium In Vitro Techniques Inhibitory postsynaptic potential Cytosol Oxygen Consumption Chlorides Internal medicine medicine Animals Parotid Gland Acetylcholine receptor Pharmacology Chemistry Parasympatholytics Rats Inbred Strains Rats Endocrinology Cholinergic Carbachol medicine.drug |
| Zdroj: | European journal of pharmacology. 164(1) |
| ISSN: | 0014-2999 |
| Popis: | The anticholinergic effects of the antipsychotic drug, cis-chlorprothixene, on the secretory events underlying the formation of primary saliva were investigated. The neuroleptic, cis-chlorprothixene, is used extensively as a major tranquillizer but shares side-effects such as xerostomia with most antidepressants. The inhibitory effects of cis-chlorprothixene upon the cholinergic-induced rise in Ca 2+ as well as on O 2 consumption and Cl − loss were investigated in isolated rat parotid acini in order to characterize its anticholinegic effects quantitatively. The cholinergic-induced rise in cytosolic, free Ca 2+ was inhibited by cis-chlorprothixene with half-maximal effect at 1.9 μM and maximal inhibition at 10 μM. When the cytosolic, free Ca 2+ was enhanced in the presence of 10 μM cis-chlorprothixene by means of the Ca 2+ ionophore A23187, a loss of Cl − was observed similar to that observed during cholinergic stimulation in the absence of cis-chlorprothixene. The findings are consistent with the possibility that cis-chlorprothixene exerts its effects on the steps leading from agonist binding to the acetylcholine receptor and to the increase of cytosolic free Ca 2+ . Thus, measurement of the stimulation-induced rise in cytosolic, free Ca 2+ in the presence of neuroleptics such as the thioxanthenes represents a fast and reliable method for detecting inhibitory effects on autonomic receptor activation. |
| Databáze: | OpenAIRE |
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