Talk:Homotaurine/Archive 1

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Archive 1

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.[1] It binds to soluble amyloid beta and inhibits the formation of neurotoxic aggregates that lead to amyloid plaque deposition in the brain.[2] However, clinical trials failed to show improvement compared to placebo.[3][4][5]

References

  1. ^ 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.
  2. ^ 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. {{cite journal}}: Unknown parameter |displayauthors= ignored (|display-authors= suggested) (help)CS1 maint: multiple names: authors list (link)
  3. ^ "Tramiprosate Falls Short in Phase III Alzheimer's Trial". Clinical Psychiatry News. November 1, 2007.
  4. ^ "Drugs In Clinical Trials : Alzhemed". Alzheimer Research Forum. Retrieved 1 October 2011.
  5. ^ "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)

activities

OK, let's discuss this:

It is a GABAb receptor antagonist [1] and reversed the catatonia induced by baclofen in rats. [2] Moreover, Homotaurine suppress ethanol-stimulated dopamine release, ethanol intake and preference in rats similar to acamprosate (Acetylated homotaurine analogue) [3].

References

  1. ^ Giotti A, Luzzi S, Spagnesi S, Zilletti L. "Homotaurine: a GABAB antagonist in guinea-pig ileum". PMID 6652358. {{cite journal}}: Cite journal requires |journal= (help)CS1 maint: multiple names: authors list (link)
  2. ^ Mehta AK1, Ticku MK. "Baclofen induces catatonia in rats". PMID 2823166. {{cite journal}}: Cite journal requires |journal= (help)CS1 maint: numeric names: authors list (link)
  3. ^ 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. {{cite journal}}: Cite journal requires |journal= (help)CS1 maint: multiple names: authors list (link)

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.[2]" has a old source too. Another source: http://naturaldatabase.therapeuticresearch.com/nd/PrintVersion.aspx?id=1251&AspxAutoDetectCookieSupport=1

https://books.google.es/books?id=4oXFr_aHRAwC&pg=PA169&lpg=PA169&dq=homotaurine+gabab&source=bl&ots=cvlQ4Y07ea&sig=QfMyPpg-40d1hCNINjqlHMhK7n0&hl=es&sa=X&ved=0ahUKEwjgzcyPx7TLAhXThhoKHT2jCGw4ChDoAQhLMAY#v=onepage&q=homotaurine%20gabab&f=false

http://tauruspet.med.yale.edu/staff/edm42/IUPUI-website/emorris.tar/emorris/emorris/PETjournalCLub/ideas%20for%20ntPET%20studies/Effects%20of%20acamporsate%20-%20delay%20of%20DA%20Olve%20EJPharm%202001.pdf

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)


  • 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 competence in the science here, as well lacking competence in Wikipedia's policies and guidelines. Please see WP:CIR. Again, I would be happy to work with you but you need to work within Wikipedia's system. Jytdog (talk) 15:59, 10 March 2016 (UTC)
  • 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 — Preceding unsigned comment added by 81.60.45.17 (talk • contribs) 12:22, 10 March 2016 (UTC)
The source at the end of the paragraph, was for the whole two-sentence paragraph. I added it after the 1st sentence to deal with your objection. everything is sourced. The source is Daniel Lednicer, The Organic Chemistry of Drug Synthesis. John Wiley & Sons, 2007 ISBN 9780470180662. Page 15 If you have a more recent secondary source on this, that would be great. Jytdog (talk) 16:16, 10 March 2016 (UTC)
  • Fonsy74 there are dispute resolution processes here in Wikipedia, but we cannot use them if you will not actually talk, and base the discussion on Wikipedia's policies and guidelines. Will you please agree to use one of the dispute resolution procedures? There is a whole community here we can tap, and well established ways to work out content disputes. I can walk you through them. Jytdog (talk) 18:48, 10 March 2016 (UTC)

Nicely formatted content, originally added by SOCKING blocked editor

Moving this here for now, this was added by obvious sock.

  • from the 1st paragraph)

Because of its similarity in structure to the neurotransmitter gamma-aminobutyric acid (GABA), it has GABAergic effects and may be useful as an anticonvulsant.[1]

Animal studies

Homotaurine reversed the catatonia induced by baclofen in rats.[2] Homotaurine also suppress ethanol-stimulated dopamine release, ethanol intake and preference in rats similar to acamprosate (an acetylated homotaurine analogue).[3][4] Acamprosate, enhance NMDA currents and inhibited GABAB receptor too.[5]

Homotaurine has shown activity in animal models of alcoholism, and a GABAB receptor partial agonist with low efficacy, becoming an antagonist and displacing full agonist as GABA or baclofen.[6] Homotaurine produces analgesia via GABAB receptor, effect that is abolished when applied CGP 35348, a GABAB receptor antagonist.[7][8]

References

  1. ^ Fariello RG, Golden GT, Pisa M (Mar 1982). "Homotaurine (3 aminopropanesulfonic acid; 3APS) protects from the convulsant and cytotoxic effect of systemically administered kainic acid". Neurology. 32 (3): 241–5. doi:10.1212/wnl.32.3.241. PMID 7199633.
  2. ^ Mehta AK, Ticku MK (Sep 1987). "Baclofen induces catatonia in rats". Neuropharmacology. 26 (9): 1419–23. PMID 2823166.
  3. ^ Olive MF, Nannini MA, Ou CJ, Koenig HN, Hodge CW (Feb 2002). "Effects of acute acamprosate and homotaurine on ethanol intake and ethanol-stimulated mesolimbic dopamine release". European Journal of Pharmacology. 437 (1–2): 55–61. PMID 11864639.
  4. ^ Lee MR, Hinton DJ, Wu J, Mishra PK, Port JD, Macura SI, Choi DS (Feb 2011). "Acamprosate reduces ethanol drinking behaviors and alters the metabolite profile in mice lacking ENT1". Neuroscience Letters. 490 (2): 90–5. doi:10.1016/j.neulet.2010.12.033. PMID 21172405.
  5. ^ Berton F, Francesconi WG, Madamba SG, Zieglgänsberger W, Siggins GR (Feb 1998). "Acamprosate enhances N-methyl-D-apartate receptor-mediated neurotransmission but inhibits presynaptic GABA(B) receptors in nucleus accumbens neurons". Alcoholism, Clinical and Experimental Research. 22 (1): 183–91. PMID 9514305.
  6. ^ Giotti A, Luzzi S, Spagnesi S, Zilletti L (Aug 1983). "Homotaurine: a GABAB antagonist in guinea-pig ileum". British Journal of Pharmacology. 79 (4): 855–62. PMID 6652358.
  7. ^ Serrano MI, Serrano JS, Fernández A, Asadi I, Serrano-Martino MC (Mar 1998). "GABA(B) receptors and opioid mechanisms involved in homotaurine-induced analgesia". General Pharmacology. 30 (3): 411–5. PMID 9510095.
  8. ^ Serrano MI, Serrano JS, Asadi I, Fernández A, Serrano-Martino MC (Jun 2001). "Role of K+ -channels in homotaurine-induced analgesia". Fundamental & Clinical Pharmacology. 15 (3): 167–73. PMID 11468027.

- Jytdog (talk) 21:30, 10 March 2016 (UTC)

It is the active molecule in ALZ-801

[1] Could mention ? or just say it is known as ALZ-801 for Alzheimers trials ? - Rod57 (talk) 17:21, 17 April 2017 (UTC)

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