Document Detail

Modulation of nicotinic ACh-, GABAA- and 5-HT3-receptor functions by external H-7, a protein kinase inhibitor, in rat sensory neurones.
MedLine Citation:
PMID:  9401786     Owner:  NLM     Status:  MEDLINE    
1. The effects of external H-7, a potent protein kinase inhibitor, on the responses mediated by gamma-aminobutyric acid A type (GABAA)-, nicotinic acetylcholine (nicotinic ACh)-, ionotropic 5-hydroxytryptamine (5-HT3)-, adenosine 5'-triphosphate (ATP)-, N-methyl-D-aspartate (NMDA)- and kainate (KA)-receptors were studied in freshly dissociated rat dorsal root ganglion neurone by use of whole cell patch-clamp technique. 2. External H-7 (1-1000 microM) produced a reversible, dose-dependent inhibition of whole cell currents activated by GABA, ACh and 5-HT. 3. Whole-cell currents evoked by ATP, 2-methylthio-ATP, NMDA and KA were insensitive to external H-7. 4. External H-7 shifted the dose-response curve of GABA-activated currents downward without changing the EC50 significantly (from 15.0 +/- 4.0 microM to 18.0 +/- 5.0 microM). The maximum response to GABA was depressed by 34.0 +/- 5.3%. This inhibitory action of H-7 was voltage-independent. 5. Intracellular application of H-7 (20 microM), cyclic AMP (1 mM) and BAPTA (10 mM) could not reverse the H-7 inhibition of GABA-activated currents. 6. The results suggest that external H-7 selectively and allosterically modulates the functions of GABAA-, nicotine ACh- and 5-HT3 receptors via a common conserved site in the external domain of these receptors.
H Z Hu; Z W Li
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't    
Journal Detail:
Title:  British journal of pharmacology     Volume:  122     ISSN:  0007-1188     ISO Abbreviation:  Br. J. Pharmacol.     Publication Date:  1997 Nov 
Date Detail:
Created Date:  1998-02-23     Completed Date:  1998-02-23     Revised Date:  2008-11-20    
Medline Journal Info:
Nlm Unique ID:  7502536     Medline TA:  Br J Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  1195-201     Citation Subset:  IM    
Research Center of Experimental Medicine, Tongji Medical University, Wuhan, People's Republic of China.
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MeSH Terms
1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine / pharmacology*
Acetylcholine / pharmacology
Adenosine Triphosphate / pharmacology
Allosteric Regulation
Dose-Response Relationship, Drug
Enzyme Inhibitors / pharmacology
Kainic Acid / pharmacology
Membrane Potentials / drug effects
N-Methylaspartate / pharmacology
Neurons, Afferent / drug effects*,  metabolism
Protein Kinase Inhibitors*
Rats, Sprague-Dawley
Receptors, GABA-A / drug effects*
Receptors, Nicotinic / drug effects*
Receptors, Serotonin / drug effects*
Receptors, Serotonin, 5-HT3
Second Messenger Systems / drug effects
Serotonin / pharmacology
gamma-Aminobutyric Acid / pharmacology
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Protein Kinase Inhibitors; 0/Receptors, GABA-A; 0/Receptors, Nicotinic; 0/Receptors, Serotonin; 0/Receptors, Serotonin, 5-HT3; 487-79-6/Kainic Acid; 50-67-9/Serotonin; 51-84-3/Acetylcholine; 56-12-2/gamma-Aminobutyric Acid; 56-65-5/Adenosine Triphosphate; 6384-92-5/N-Methylaspartate; 84477-87-2/1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine

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