Noncompetitive inhibition by camphor of nicotinic acetylcholine receptors

The effect of camphor, a monoterpenoid, on catecholamine secretion was investigated in bovine adrenal chromaffin cells. Camphor inhibited [ 3H]norepinephrine ([ 3H]NE) secretion induced by a nicotinic acetylcholine receptor (nAChR) agonist, 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP), with a hal...

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Bibliographic Details
Published in:Biochemical pharmacology 2001-04, Vol.61 (7), p.787-793
Main Authors: Park, Tae-Ju, Seo, Hyuck-Kyo, Kang, Byung-Jo, Kim, Kyong-Tai
Format: Article
Language:English
Subjects:
Animals
Anti-Infective Agents, Local - pharmacology
Binding Sites - drug effects
Biological and medical sciences
Calcium - metabolism
Camphor
Camphor - pharmacology
Catecholamine secretion
Catecholamines - metabolism
Cattle
Cholinergic system
Chromaffin cells
Chromaffin Cells - drug effects
Chromaffin Cells - metabolism
Dimethylphenylpiperazinium Iodide - pharmacology
Drug Interactions
In Vitro Techniques
Medical sciences
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Nicotine - pharmacology
Nicotinic acetylcholine receptors
Nicotinic Agonists - pharmacology
Nicotinic Antagonists - pharmacology
Norepinephrine - metabolism
Pharmacology. Drug treatments
Receptors, Nicotinic - drug effects
Receptors, Nicotinic - metabolism
Sodium - metabolism
Time Factors
Tritium
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Summary:The effect of camphor, a monoterpenoid, on catecholamine secretion was investigated in bovine adrenal chromaffin cells. Camphor inhibited [ 3H]norepinephrine ([ 3H]NE) secretion induced by a nicotinic acetylcholine receptor (nAChR) agonist, 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP), with a half-maximal inhibitory concentration ( ic 50) of 70 ± 12 μM. In addition, camphor inhibited the rise in cytosolic calcium ([Ca 2+] i) and sodium ([Na +] i) induced by DMPP with ic 50 values of 88 ± 32 and 19 ± 2 μM, respectively, suggesting that the activity of nAChRs is also inhibited by camphor. On the other hand, binding of [ 3H]nicotine to nAChRs was not affected by camphor. [Ca 2+] i increases induced by high K +, veratridine, and bradykinin were not affected by camphor. The data suggest that camphor specifically inhibits catecholamine secretion by blocking nAChRs without affecting agonist binding.
ISSN:0006-2952
1873-2968
DOI:10.1016/S0006-2952(01)00547-0