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Its impossible homotaurine be antagonist if it mimick gaba! Error and unsourced. Evicence says that is a gaba ionotropic agonist and gaba metrabotropic low efficacy agonist (antagonist) <small class="autosigned">— Preceding ] comment added by ] (]) 12:08, 10 March 2016 (UTC)</small><!-- Template:Unsigned IP --> <!--Autosigned by SineBot--> | Its impossible homotaurine be antagonist if it mimick gaba! Error and unsourced. Evicence says that is a gaba ionotropic agonist and gaba metrabotropic low efficacy agonist (antagonist) <small class="autosigned">— Preceding ] comment added by ] (]) 12:08, 10 March 2016 (UTC)</small><!-- Template:Unsigned IP --> <!--Autosigned by SineBot--> | ||
:No. it is a common drug discovery strategy. There are discussing this. The idea is that a small molecule drug candidate is similar enough to the endogenous ligand to bind the receptor and block it, but not have the same effect (activating or inactivating) as the the endogenous ligand. You have just made it clear that you lack comepetence in the science here, as well lack competence in Misplaced Pages's policies and guidelines. Again, I would be happy to work with you but you need to work within Misplaced Pages's system. ] (]) 15:59, 10 March 2016 (UTC) | |||
== Alzheimers == | == Alzheimers == |
Revision as of 15:59, 10 March 2016
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The Jytdog version has a few sources and No source for say homotaurine is a gaba antagonist mimicking gaba. Current evicence shows that homotaurine is an agonist at GABA a ionotropic and a partial low efficacy agonist of gabab receptors, who compite with gaba and baclofen , more potents agonists OK, let's discuss this:
It is a GABAb receptor antagonist and reversed the catatonia induced by baclofen in rats. Moreover, Homotaurine suppress ethanol-stimulated dopamine release, ethanol intake and preference in rats similar to acamprosate (Acetylated homotaurine analogue) .
References
- Giotti A, Luzzi S, Spagnesi S, Zilletti L. "Homotaurine: a GABAB antagonist in guinea-pig ileum". PMID 6652358.
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(help)CS1 maint: multiple names: authors list (link) - Mehta AK1, Ticku MK. "Baclofen induces catatonia in rats". PMID 2823166.
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(help)CS1 maint: numeric names: authors list (link) - Olive MF, Nannini MA, Ou CJ, Koenig HN, Hodge CW. "Effects of acute acamprosate and homotaurine on ethanol intake and ethanol-stimulated mesolimbic dopamine release". PMID 11864639.
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The sources here are both old and primary. This is not how we should be sourcing WP content. These kinds of papers often turn out to be incorrect. If they are correct and valuable, they are discussed in reviews. Where are the secondary sources supporting this content? Jytdog (talk) 21:18, 9 March 2016 (UTC)
Response:
The entire document is accesible, and "it has GABAergic effects and may be useful as an anticonvulsant." has a old source too. Another source: http://naturaldatabase.therapeuticresearch.com/nd/PrintVersion.aspx?id=1251&AspxAutoDetectCookieSupport=1
is 2002 an old source? OK, lets go to erase all of "old" sources. — Preceding unsigned comment added by Fonsy74 (talk • contribs) 21:36, 9 March 2016 (UTC)
- this is not a response. where are the reviews discussing this? Jytdog (talk) 21:48, 9 March 2016 (UTC)
- OK, I finally had time to go look for reveiws myself - here is the search. I added three reviews from that seach:
- Caltagirone C et al. The potential protective effect of tramiprosate (homotaurine) against Alzheimer's disease: a review. Aging Clin Exp Res. 2012 Dec;24(6):580-7. PMID 22961121
- Herrmann N et al. Current and emerging drug treatment options for Alzheimer's disease: a systematic review. Drugs. 2011 Oct 22;71(15):2031-65. Review. PMID 21985169
- Aisen PS Alzhemed: a potential treatment for Alzheimer's disease. Curr Alzheimer Res. 2007 Sep;4(4):473-8. PMID 17908052
- None of these recent reviews mentions that GABA binding data. This appears to be not something that the field finds true or relevant - we cannot know which. This is why we rely on reviews, and not the primary literature. I have again removed this content, as MEDRS-compliant sources do not support it. Jytdog (talk) 01:16, 10 March 2016 (UTC)
- OK, I finally had time to go look for reveiws myself - here is the search. I added three reviews from that seach:
Its impossible homotaurine be antagonist if it mimick gaba! Error and unsourced. Evicence says that is a gaba ionotropic agonist and gaba metrabotropic low efficacy agonist (antagonist) — Preceding unsigned comment added by 81.60.45.17 (talk) 12:08, 10 March 2016 (UTC)
- No. it is a common drug discovery strategy. There are many reviews discussing this. The idea is that a small molecule drug candidate is similar enough to the endogenous ligand to bind the receptor and block it, but not have the same effect (activating or inactivating) as the the endogenous ligand. You have just made it clear that you lack comepetence in the science here, as well lack competence in Misplaced Pages's policies and guidelines. Again, I would be happy to work with you but you need to work within Misplaced Pages's system. Jytdog (talk) 15:59, 10 March 2016 (UTC)
Alzheimers
This content too is not appropriately sourced. moving here for now...
Homotaurine has also been investigated as a potential treatment for Alzheimer's disease. It binds to soluble amyloid beta and inhibits the formation of neurotoxic aggregates that lead to amyloid plaque deposition in the brain. However, clinical trials failed to show improvement compared to placebo.
References
- Gauthier, S; Aisen, P. S.; Ferris, S. H.; Saumier, D; Duong, A; Haine, D; Garceau, D; Suhy, J; Oh, J; Lau, W; Sampalis, J (2009). "Effect of tramiprosate in patients with mild-to-moderate Alzheimer's disease: Exploratory analyses of the MRI sub-group of the Alphase study". The journal of nutrition, health & aging. 13 (6): 550–7. PMID 19536424.
- Aisen PS, Gauthier S, Vellas B (2007). "Alzhemed: a potential treatment for Alzheimer's disease". Curr Alzheimer Res. 4 (4): 473–8. doi:10.2174/156720507781788882. PMID 17908052.
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suggested) (help)CS1 maint: multiple names: authors list (link) - "Tramiprosate Falls Short in Phase III Alzheimer's Trial". Clinical Psychiatry News. November 1, 2007.
- "Drugs In Clinical Trials : Alzhemed". Alzheimer Research Forum. Retrieved 1 October 2011.
- "Analysts Skeptical Of Neurochem's Efforts To Salvage Value From Alzhemed". Canada National Post. November 13, 2007. Retrieved 1 October 2011.
- Jytdog (talk) 21:19, 9 March 2016 (UTC)
- You have also restored this without discussing or fixing the sources. This is not reliable content because the source are not MEDRS. Jytdog (talk) 22:18, 9 March 2016 (UTC)
- I have fixed this now. Jytdog (talk) 01:16, 10 March 2016 (UTC)