Chemistry:CHEB
CHEB, also known as BRN 0250312 is a convulsant barbiturate. Its mechanism of action is not fully understood.
Pharmacodynamics
CHEB has uncommon action compared to other barbiturates. While other barbiturates such as Barbital are usually anticonvulsants, CHEB is a convulsant.
CHEB's convulsant action is not fully understood. There may be multiple mechanisms involved in its properties;
In rats, CHEB stimulates the release of glutamate, an excitatory neurotransmitter.[1]
In low doses, CHEB can block the action of glycine, thus operating in a strychnine similar way.[2]
Another study has shown that CHEB could increase the release of acetylcholine. This result was not observed with some other convulsants (S(+)-MPPB, pentylenetetrazol and Ro-5-3663), suggesting that this property is unique.[3]
Paradoxically, CHEB is able to enhance the binding of GABA, this is a strange property, as compounds that enhance GABA binding usually have anticonvulsant action, such as diazepam.[4]
See also
- Diberal (DMBB)
- McN-481
References
- ↑ Wei, L.; Schlame, M.; Downes, H.; Hemmings, H. C. (June 1996). "CHEB, a convulsant barbiturate, evokes calcium-dependent spontaneous glutamate release from rat cerebrocortical synaptosomes". Neuropharmacology 35 (6): 695–701. doi:10.1016/0028-3908(96)84641-7. ISSN 0028-3908. PMID 8887978.
- ↑ Nicholson, G. M.; Spence, I.; Johnston, G. A. (June 1985). "Strychnine-like action of the convulsant barbiturate, CHEB". Neuropharmacology 24 (6): 465–471. doi:10.1016/0028-3908(85)90050-4. ISSN 0028-3908. PMID 2862600.
- ↑ Holtman, J. R.; Richter, J. A. (September 1983). "Increased release of [3H]acetylcholine in vitro from the mouse hippocampus by a convulsant barbiturate". Neuropharmacology 22 (9): 1101–1108. doi:10.1016/0028-3908(83)90031-x. ISSN 0028-3908. PMID 6138729.
- ↑ Willow, M; Johnston, GA (1981-04-01). "Enhancement by anesthetic and convulsant barbiturates of GABA binding to rat brain synaptosomal membranes". The Journal of Neuroscience 1 (4): 364–367. doi:10.1523/JNEUROSCI.01-04-00364.1981. ISSN 0270-6474. PMID 6267224.
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