Histamine H1 antagonists block M-currents in dissociated rat cortical neurons

We investigated the effects of histamine H1 antagonists on acutely dissociated neurons from the rat cortex using the patch-clamp technique. First-generation antihistamines, such as pyrilamine, d-chlorpheniramine, diphenhydramine, and ketotifen, suppressed M-currents in a concentration-dependent mann...

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Bibliographic Details
Published in:Brain research 2005-09, Vol.1057 (1-2), p.81-87
Main Authors: SATO, Ikuko, MUNAKATA, Mitsutoshi, IINUMA, Kazuie
Format: Article
Language:English
Subjects:
Analysis of Variance
Animals
Animals, Newborn
Biological and medical sciences
Cells, Cultured
Central nervous system
Cerebral Cortex - cytology
Dose-Response Relationship, Drug
Drug Interactions
Electric Stimulation - methods
Electrophysiology
Fundamental and applied biological sciences. Psychology
Histamine H1 Antagonists - pharmacology
Indoles - pharmacology
Ion Channels - drug effects
Ion Channels - physiology
Membrane Potentials - drug effects
Membrane Potentials - physiology
Membrane Potentials - radiation effects
Neural Inhibition - drug effects
Neural Inhibition - physiology
Neurons - drug effects
Neurons - physiology
Patch-Clamp Techniques
Potassium Channel Blockers - pharmacology
Pyridines - pharmacology
Rats
Rats, Wistar
Tetrodotoxin - pharmacology
Vertebrates: nervous system and sense organs
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Summary:We investigated the effects of histamine H1 antagonists on acutely dissociated neurons from the rat cortex using the patch-clamp technique. First-generation antihistamines, such as pyrilamine, d-chlorpheniramine, diphenhydramine, and ketotifen, suppressed M-currents in a concentration-dependent manner with respective half-inhibition concentrations (C50) of 35.9, 48.5, 34.8, and 47.8 microM at a holding potential of -26.5 mV. Astemizole, a second-generation antihistamine, inhibited M-currents with a C50 of 18.1 microM, but cetirizine did not do so, up to a concentration of 300 microM. Neither ranitidine nor cimetidine, both H2 antagonists, suppressed M-currents. The C50 of pyrilamine significantly decreased with membrane hyperpolarization, suggesting that it acts directly on M channel pores. The inhibition of M channels may be involved in the neurotoxic effects of histamine H1 antagonist overdose.
ISSN:0006-8993
1872-6240
DOI:10.1016/j.brainres.2005.07.040