PMID: 7545885Jul 12, 1995Paper

Clonidine and cirazoline inhibit activation of nicotinic channels in PC-12 cells

Annals of the New York Academy of Sciences
I F MusgraveG Schultz

Abstract

Clonidine and cirazoline bind with high affinity to a nonadrenergic site in the brain stem, the so-called imidazoline I1 receptor. Our aim was to determine the mechanism by which these receptors act and their possible linkage to signal-transducing heterotrimeric G-proteins. We examined the effects of clonidine and cirazoline on PC-12 cells, a neuronal cell line that is reported to possess the I1 site and have no alpha 2-adrenoceptors. In undifferentiated PC-12 cells loaded with the Ca2+ indicator dye fura-2, clonidine and cirazoline (10-100 microM) inhibited the increase in [Ca2+]i produced by nicotine (10 microM). This inhibition was not reversed by yohimbine (100 microM), and adrenaline and BHT 920 were ineffective at 100 microM. This effect was not inhibited by pretreatment with pertussis toxin (24 hours, 100 ng/ml) and not modulated by pretreatment with IBMX (100 microM). The nicotine-induced increase in [Ca2+]i is apparently due to Ca2+ entering via the intrinsic ion channel of the nicotinic acetylcholine receptor. Clonidine and cirazoline inhibited the inward current produced by nicotine (10 microM) as measured by the whole cell patch-clamp technique in differentiated PC-12 cells, recorded at a holding potential of -60 mV...Continue Reading

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Citations

Aug 29, 1996·European Journal of Pharmacology·G OlmosJ A García-Sevilla
Dec 16, 1998·Journal of the Autonomic Nervous System·I F Musgrave, R A Hughes
Oct 1, 1996·Clinical and Experimental Pharmacology & Physiology·I F MusgraveG Schultz
Jul 23, 1999·Annals of the New York Academy of Sciences·I F Musgrave, R A Hughes
Feb 11, 1999·Anesthesia and Analgesia·K NishinaY Niwa
Feb 27, 2003·The Journal of Pharmacology and Experimental Therapeutics·Walter RaaschPeter Dominiak
Dec 11, 2019·Pharmacological Reviews·Pascal BousquetJun-Xu Li
Dec 31, 1997·The American Journal of Physiology·D J Reis, J E Piletz

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