To install click the Add extension button. That's it.

The source code for the WIKI 2 extension is being checked by specialists of the Mozilla Foundation, Google, and Apple. You could also do it yourself at any point in time.

4,5
Kelly Slayton
Congratulations on this excellent venture… what a great idea!
Alexander Grigorievskiy
I use WIKI 2 every day and almost forgot how the original Wikipedia looks like.
Live Statistics
English Articles
Improved in 24 Hours
Added in 24 Hours
What we do. Every page goes through several hundred of perfecting techniques; in live mode. Quite the same Wikipedia. Just better.
.
Leo
Newton
Brights
Milds

From Wikipedia, the free encyclopedia

Loreclezole
Loreclezole.svg
Clinical data
ATC code
  • none
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
Chemical and physical data
Formula C10H6Cl3N3
Molar mass 274.534 g/mol
  (verify)

Loreclezole is a sedative and an anticonvulsant which acts as a GABAA receptor positive allosteric modulator.[1] The binding site of loreclezole has been shown experimentally to be shared by valerenic acid, an extract of the root of the valerian plant.[2] Structurally, loreclezole is a triazole derivative. In animal seizure models, loreclezole is protective against pentylenetetrazol seizures but is less active in the maximal electroshock test.[3] In addition, at low, nontoxic doses, the drug has anti-absence activity in a genetic model of generalized absence epilepsy. Consequently, loreclezole has a profile of activity similar to that of benzodiazepines. A potential benzodiazepine-like interaction with GABA receptors is suggested by the observation that the anticonvulsant effects of loreclezole can be reversed by benzodiazepine receptor inverse agonists. The benzodiazepine antagonist flumazenil, however, fails to alter the anticonvulsant activity of loreclezole, indicating that loreclezole is not a benzodiazepine receptor agonist. Using native rat and cloned human GABA-A receptors, loreclezole strongly potentiated GABA-activated chloride current. However, activity of the drug did not require the presence of the γ-subunit and was not blocked by flumazenil, confirming that loreclezole does not interact with the benzodiazepine recognition site.

References

  1. ^ Wingrove, P. B.; Wafford, K. A.; Bain, C.; Whiting, P. J. (1994). "The modulatory action of loreclezole at the gamma-aminobutyric acid type a receptor is determined by a single amino acid in the beta 2 and beta 3 subunit". Proceedings of the National Academy of Sciences of the United States of America. 91 (10): 4569–4573. doi:10.1073/pnas.91.10.4569. PMC 43827Freely accessible. PMID 8183949. 
  2. ^ Khom, S.; Baburin, I.; Timin, E.; Hohaus, A.; Trauner, G.; Kopp, B.; Hering, S. (2007). "Valerenic acid potentiates and inhibits GABAA receptors: Molecular mechanism and subunit specificity". Neuropharmacology. 53 (1): 178–187. doi:10.1016/j.neuropharm.2007.04.018. PMID 17585957. 
  3. ^ Rogawski, M (1996). "Epilepsy". In Pullan, L; Patel, J. Neurotherapeutics: Emerging Strategies. Humana Press. pp. 193–273. 


This page was last edited on 8 July 2016, at 04:19
Basis of this page is in Wikipedia. Text is available under the CC BY-SA 3.0 Unported License. Non-text media are available under their specified licenses. Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc. WIKI 2 is an independent company and has no affiliation with Wikimedia Foundation.