Access the full text.
Sign up today, get DeepDyve free for 14 days.
Willow (1982)
627Mol. Pharmacol., 22
Crevling (1983)
350Mol. Pharmacol., 25
Janis Eells, P. Bandettini, P. Holman, J. Propp (1992)
Pyrethroid insecticide-induced alterations in mammalian synaptic membrane potential.The Journal of pharmacology and experimental therapeutics, 262 3
Gifford (1996)
1431J. Pharmacol. Exp. Therap., 277
R. Nicholson, Chengyong Liao, Jian Zheng, Laurence David, L. Coyne, A. Errington, G. Singh, G. Lees (2003)
Sodium channel inhibition by anandamide and synthetic cannabimimetics in brainBrain Research, 978
M. Rinaldi-Carmona, F. Barth, M. Héaulme, D. Shire, B. Calandra, C. Congy, Serge Martinez, J. Maruani, G. Néliat, D. Caput, P. Ferrara, P. Soubrié, J. Breliere, G. Fur (1994)
SR141716A, a potent and selective antagonist of the brain cannabinoid receptorFEBS Letters, 350
S. Childers, T. Sexton, Mary Roy (1994)
Effects of anandamide on cannabinoid receptors in rat brain membranes.Biochemical pharmacology, 47 4
Catterall (1981)
356Mol. Pharmacol., 20
Kilpatrick (1991)
555, 2
B. Verdon, Jian Zheng, R. Nicholson, C Ganelli, G. Lees (2000)
Stereoselective modulatory actions of oleamide on GABAA receptors and voltage‐gated Na+ channels in vitro: a putative endogenous ligand for depressant drug sites in CNSBritish Journal of Pharmacology, 129
T. Ohno-Shosaku, T. Maejima, M. Kano (2001)
Endogenous Cannabinoids Mediate Retrograde Signals from Depolarized Postsynaptic Neurons to Presynaptic TerminalsNeuron, 29
A. Zhang, P. Towner, R. Nicholson (1996)
Dihydropyrazole Insecticides: Interference with Depolarization-Dependent Phosphorylation of Synapsin I and Evoked Release ofl-Glutamate in Nerve-Terminal Preparations from Mammalian BrainPesticide Biochemistry and Physiology, 54
Crevling Crevling, McNeal McNeal, Daly Daly, Brown Brown (1983)
Batrachotoxin‐induced depolarization and ( 3 H)batrachotoxin‐A 20‐alpha‐benzoate binding in a vesicular preparation from guinea pig cerebral cortex: Inhibition by local anestheticsMol. Pharmacol., 25
R. Lan, Qian Liu, P. Fan, Sonyuan Lin, S. Fernando, D. McCallion, R. Pertwee, A. Makriyannis (1999)
Structure-activity relationships of pyrazole derivatives as cannabinoid receptor antagonists.Journal of medicinal chemistry, 42 4
R. Nicholson, Elena Merletti (1990)
The effect of dihydropyrazoles on release of [3H]GABA from nerve terminals isolated from mammalian cerebral cortexPesticide Biochemistry and Physiology, 37
D. Deecher, G. Payne, D. Soderlund (1991)
Inhibition of [3H]batrachotoxinin A 20-α-benzoate binding to mouse brain sodium channels by the dihydropyrazole insecticide RH 3421Pesticide Biochemistry and Physiology, 41
Anatol Kreitzer, W. Regehr (2001)
Retrograde Inhibition of Presynaptic Calcium Influx by Endogenous Cannabinoids at Excitatory Synapses onto Purkinje CellsNeuron, 29
Nicholson Nicholson, Liao Liao, Zheng Zheng, David David, Coyne Coyne, Errington Errington, Singh Singh, Lees Lees (2003)
Sodium channel inhibition by anandamide and synthetic cannabimimetics in mammalian brainBrain Res., 978
Postma (1984)
19Mol. Pharmacol., 25
Anatol Kreitzer, Adam Carter, W. Regehr (2002)
Inhibition of Interneuron Firing Extends the Spread of Endocannabinoid Signaling in the CerebellumNeuron, 34
C. Creveling, E. McNeal, J. Daly, G. Brown (1983)
Batrachotoxin-induced depolarization and [3H]batrachotoxinin-a 20 alpha-benzoate binding in a vesicular preparation from guinea pig cerebral cortex.Molecular pharmacology, 23 2
A. Gifford, C. Ashby (1996)
Electrically evoked acetylcholine release from hippocampal slices is inhibited by the cannabinoid receptor agonist, WIN 55212-2, and is potentiated by the cannabinoid antagonist, SR 141716A.The Journal of pharmacology and experimental therapeutics, 277 3
W. Catterall (1980)
Neurotoxins that act on voltage-sensitive sodium channels in excitable membranes.Annual review of pharmacology and toxicology, 20
Adams (1995)
1172J. Pharmacol. Exp. Therap., 273
Rachel Wilson, R. Nicoll (2001)
Endogenous cannabinoids mediate retrograde signalling at hippocampal synapsesNature, 410
W. Catterall (1981)
Inhibition of voltage-sensitive sodium channels in neuroblastoma cells by antiarrhythmic drugs.Molecular pharmacology, 20 2
B. Thomas, A. Gilliam, D. Burch, M. Roche, H. Seltzman (1998)
Comparative receptor binding analyses of cannabinoid agonists and antagonists.The Journal of pharmacology and experimental therapeutics, 285 1
Thomas (1998)
285J. Pharmacol. Exp. Therap., 285
S. Postma, W. Catterall (1984)
Inhibition of binding of [3H]batrachotoxinin A 20-alpha-benzoate to sodium channels by local anesthetics.Molecular pharmacology, 25 2
M. Willow, W. Catterall (1982)
Inhibition of binding of [3H]batrachotoxinin A 20-alpha-benzoate to sodium channels by the anticonvulsant drugs diphenylhydantoin and carbamazepine.Molecular pharmacology, 22 3
W. Catterall, C. Morrow, J. Daly, G. Brown (1981)
Binding of batrachotoxinin A 20-alpha-benzoate to a receptor site associated with sodium channels in synaptic nerve ending particles.The Journal of biological chemistry, 256 17
R. Nicholson (1992)
Insecticidal dihydropyrazoles antagonize the depolarizing action of veratridine in mammalian synaptosomes as measured with a voltage-sensitive dyePesticide Biochemistry and Physiology, 42
R. Harris, A. Allan (1985)
Functional coupling of gamma-aminobutyric acid receptors to chloride channels in brain membranes.Science, 228 4703
P. Dunkley, P. Jarvie, J. Heath, G. Kidd, J. Rostas (1986)
A rapid method for isolation of synaptosomes on Percoll gradientsBrain Research, 372
Nicholson Nicholson, Merletti Merletti (1990)
The effect of dihydropyrazoles on release of ( 3 H)GABA from nerve terminals isolated from mammalian cerebral cortexPestic. Physiol. Biochem., 37
Eells (1992)
1173J. Pharmacol. Exp. Therap., 262
I. Adams, W. Ryan, M. Singer, B. Thomas, D. Compton, R. Razdan, B. Martin (1995)
Evaluation of cannabinoid receptor binding and in vivo activities for anandamide analogs.The Journal of pharmacology and experimental therapeutics, 273 3
Abstract: The cannabinoid 1 receptor antagonist AM 251 is known to block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain. We examined the ability of AM 251 to inhibit sodium channel‐dependent functions and the binding of (3H)batrachotoxinin A 20‐α‐benzoate to sodium channels in mouse brain synaptic preparations. Depolarization of synaptoneurosomes by the sodium channel site 2‐specific neurotoxin veratridine, which is abolished by tetrodotoxin, was found to be inhibited in a concentration‐dependent fashion by AM 251 (IC50=8.9 μM). Veratridine‐dependent (tetrodotoxin suppressible) release, of L‐glutamic acid and GABA from synaptosomes was also reduced by AM 251 (IC50s=8.5 μM (L‐glutamic acid), 9.2 μM (GABA)). The binding of the radioligand (3H)batrachotoxinin A 20‐α‐benzoate to site 2 on sodium channels was displaced by AM 251 (IC50=11.2 μM). Scatchard analysis of binding showed that at its IC50, AM 251 increased (by 2.3 times) the KD of radioligand without altering Bmax, suggesting a competitive mechanism of inhibition by AM 251. Kinetic experiments indicated that AM 251 inhibits equilibrium binding by allosterically accelerating the dissociation of the (3H)‐batrachotoxinin A 20‐α‐benzoate:sodium channel complex. Our data suggest that micromolar concentrations of AM 251 are capable of reducing neuronal excitability and inhibiting release of excitatory and inhibitory transmitters through blockade of voltage‐sensitive sodium channels in brain.
Basic and Clinical Pharmacology & Toxicology – Wiley
Published: Feb 1, 2004
Read and print from thousands of top scholarly journals.
Already have an account? Log in
Bookmark this article. You can see your Bookmarks on your DeepDyve Library.
To save an article, log in first, or sign up for a DeepDyve account if you don’t already have one.
Copy and paste the desired citation format or use the link below to download a file formatted for EndNote
Access the full text.
Sign up today, get DeepDyve free for 14 days.
All DeepDyve websites use cookies to improve your online experience. They were placed on your computer when you launched this website. You can change your cookie settings through your browser.