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Effects of WIN55,212-2 on voltage-gated sodium channels in trigeminal ganglion neurons of rats.
- Source :
- Neurological Research; Feb2008, Vol. 30 Issue 1, p85-91, 7p, 4 Graphs
- Publication Year :
- 2008
-
Abstract
- Objectives: This study was carried out to investigate the effects of WIN55,212-2, a potential cannabinoid receptor agonist, on voltage-gated sodium currents I<subscript>Na</subscript> in cultured trigeminal ganglion neurons of rats, and to investigate whether the anti-nociceptive effects of cannabinoid receptor subtype 1 (CB1) were produced through its modulation on I<subscript>Na</subscript>. Methods: Whole cell patch clamp techniques were used to record I<subscript>Na</subscript> before and after WIN55,212-2 was perfused in cultured trigeminal ganglion neurons of rats. Results: WIN55,212-2 (0.01 μmol/l) could enhance I<subscript>Na</subscript> slightly by 11.5 ± 4.7% (n=7, p<0.05), and this effect could not be blocked by AM251, the CB1 receptor antagonist. However, WIN55,212-2 could inhibit I<subscript>Na</subscript> in concentration dependent manner at concentrations from 0.1 to 100 μmol/l. The inhibitory rates were 17.4 ± 6.0, 22.5 ± 7.8, 43.9 ± 9.4 and 73.9 ± 6.7% respectively by 0.1, 1, 10, 100 μmol/l WIN55,212-2, and the EC<subscript>50</subscript> was 17.8 μmol/l (n=7, p<0.05 or p<0.01). This inhibitory effect could be blocked partly by 1 μmol/l AM251 (n=7, p<0.05). WIN55,212-2 (0.01 μmol/l) shifted the active curve of I<subscript>Na</subscript> leftward slightly (n=7, p<0.05), but had no effect on its stable inactive curve (n=7, p>0.05). WIN55,212-2 (10 μmol/l) did not affect the active and stable inactive curves of I<subscript>Na</subscript> (n=7, p>0.05). Conclusion: WIN55,212-2 had bidirectional (two phases) effects on I<subscript>Na</subscript> in trigeminal ganglion neurons. It might act on different receptors, and the CB1 receptor participated in its modulation on I<subscript>Na</subscript>. [ABSTRACT FROM AUTHOR]
Details
- Language :
- English
- ISSN :
- 01616412
- Volume :
- 30
- Issue :
- 1
- Database :
- Complementary Index
- Journal :
- Neurological Research
- Publication Type :
- Academic Journal
- Accession number :
- 31383006
- Full Text :
- https://doi.org/10.1179/016164107X228642