| 词条 | Homotaurine |
| 释义 |
| Watchedfields = changed | verifiedrevid = 415530375 | Reference =[1] | ImageFile_Ref = {{chemboximage|correct|??}} | ImageFile = Homotaurine.svg | ImageSize = | ImageAlt = Skeletal formula | ImageFile1 = Homotaurine-3D-balls.png | ImageAlt1 = Ball-and-stick model | IUPACName =3-Aminopropane-1-sulfonic acid | OtherNames =Tramiprosate; Alzhemed; 3-APS |Section1={{Chembox Identifiers | ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}} | ChemSpiderID = 1584 | KEGG_Ref = {{keggcite|correct|kegg}} | KEGG = D06202 | InChI = 1/C3H9NO3S/c4-2-1-3-8(5,6)7/h1-4H2,(H,5,6,7) | InChIKey = SNKZJIOFVMKAOJ-UHFFFAOYAT | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 149082 | StdInChI_Ref = {{stdinchicite|correct|chemspider}} | StdInChI = 1S/C3H9NO3S/c4-2-1-3-8(5,6)7/h1-4H2,(H,5,6,7) | StdInChIKey_Ref = {{stdinchicite|correct|chemspider}} | StdInChIKey = SNKZJIOFVMKAOJ-UHFFFAOYSA-N | CASNo_Ref = {{cascite|correct|??}} | CASNo =3687-18-1 | PubChem =1646 | SMILES = O=S(=O)(O)CCCN }} |Section2={{Chembox Properties | C=3 | H=9 | N=1 | O=3 | S=1 | Appearance = | Density = | MeltingPtC = 293 | MeltingPt_notes = (decomposition) | BoilingPt = | Solubility = |Section3={{Chembox Hazards | MainHazards = | FlashPt = | AutoignitionPt = | RPhrases ={{R36/37/38}} | SPhrases ={{S26}} {{S36}} }}Homotaurine (also known as tramiprosate (INN), 3-amino-1-propanesulfonic acid, or 3-APS) is a natural amino acid found in seaweed. [2] It is analogous to taurine, but with an extra carbon in its chain. It has GABAergic activity, apparently by mimicking GABA, which it resembles.[3] Homotaurine was investigated in a Phase III clinical trial as a potential treatment for Alzheimer's disease that did not show efficacy.[3] A study in cognitive impairment done in 2018 did show positive benefits. [4] Biochemical propertiesIn preclinical studies it had been found to bind to soluble amyloid beta and inhibit the formation of neurotoxic aggregates.[3][5] Homotaurine has also shown anticonvulsant activities, reduction in skeletal muscle tonus, and hypothermic activity.[8] Homotaurine has been reported as a GABA antagonist,[3] as well as a GABA agonist.[6][7] In vitro studies have found that homotaurine is a GABAA partial agonist[8] as well as a GABAB receptor partial agonist with low efficacy, becoming an antagonist and a displacing full agonist of GABA or baclofen at this receptor.[9] In a study in rats, homotaurine reversed the catatonia induced by baclofen (the prototypical GABAB agonist),[10] and was able to produce analgesia via the GABAB receptor, an effect that was abolished when CGP-35348, a GABAB receptor antagonist was applied.[11][12] One study in rats showed that homotaurine suppressed ethanol-stimulated dopamine release, as well as ethanol intake and preference in rats in a way similar to the N-acetyl derivative of homotaurine, acamprosate.[13] Acamprosate was approved by the FDA in 2004 to treat alcohol dependence.[14] References1. ^{{cite web | url = http://www.sigmaaldrich.com/catalog/search/ProductDetail/ALDRICH/A76109 | title = Homotaurine | publisher = Sigma-Aldrich}} {{Anticonvulsants}}{{GABAergics}}2. ^{{cite journal | pmc = 4172065| year = 2014| last1 = Martorana| first1 = A.| title = Homotaurine Induces Measurable Changes of Short Latency Afferent Inhibition in a Group of Mild Cognitive Impairment Individuals| journal = Frontiers in Aging Neuroscience| volume = 6| pages = 254| last2 = Di Lorenzo| first2 = F.| last3 = Manenti| first3 = G.| last4 = Semprini| first4 = R.| last5 = Koch| first5 = G.| pmid = 25295005| doi = 10.3389/fnagi.2014.00254}} 3. ^1 {{cite journal | doi = 10.3275/8585 | pmid = 22961121 | year = 2012 | last1 = Caltagirone | first1 = C. | title = The potential protective effect of tramiprosate (homotaurine) against Alzheimer's disease: A review | journal = Aging Clinical and Experimental Research | volume = 24 | issue = 6 | pages = 580–7 | last2 = Ferrannini | first2 = L. | last3 = Marchionni | first3 = N. | last4 = Nappi | first4 = G. | last5 = Scapagnini | first5 = G. | last6 = Trabucchi | first6 = M. }} 4. ^http://www.jgerontology-geriatrics.com/wp-content/uploads/2018/03/03_Martorana-1.pdf 5. ^{{cite journal | doi = 10.2174/156720507781788882 | title = Alzhemed: A Potential Treatment for Alzheimers Disease | journal = Current Alzheimer Research | volume = 4 | issue = 4 | pages = 473–478 | year = 2007 | last1 = Aisen | first1 = Paul | last2 = Gauthier | first2 = Serge | last3 = Vellas | first3 = Bruno | last4 = Briand | first4 = Richard | last5 = Saumier | first5 = Daniel | last6 = Laurin | first6 = Julie | last7 = Garceau | first7 = Denis }} 6. ^1 {{cite book | author = Oja SS and Kontro P. | title = Chapter 18: Taurine | work = Metabolism in the Nervous System | editor = Lajtha ANS | publisher = Springer Science & Business Media| date = 2013 | url = https://books.google.es/books?id=du_TBwAAQBAJ&pg=PA520 | page = 520 | isbn = 9781468443677}} 7. ^Armen H. Tashjian and Ehrin J. Armstrong. Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy. Edited by David E. Golan. Lippincott Williams & Wilkins, 2011 {{ISBN|9781451118056}}. [https://books.google.com/books?id=kjCCMZHInigC&pg=PA308 Page 308] 8. ^{{cite journal | doi =10.1007/s00726-014-1813-0 | pmid =25119985 | title =Modulation of GABA-A receptors of astrocytes and STC-1 cells by taurine structural analogs | journal =Amino Acids | volume =46 | issue =11 | pages =2587–2593 | year =2014 | last1 =Reyes-Haro | first1 =Daniel | last2 =Cabrera-Ruíz | first2 =Elizabeth | last3 =Estrada-Mondragón | first3 =Argel | last4 =Miledi | first4 =Ricardo | last5 =Martínez-Torres | first5 =Ataúlfo }} 9. ^{{cite journal | doi = 10.1111/j.1476-5381.1983.tb10529.x | title = Homotaurine: A GABAB antagonist in guinea-pig ileum | journal = British Journal of Pharmacology | volume = 79 | issue = 4 | pages = 855–862 | year = 1983 | last1 = Giotti | first1 = A. | last2 = Luzzi | first2 = S. | last3 = Spagnesi | first3 = S. | last4 = Zilletti | first4 = Lucilla }} 10. ^{{cite journal | doi = 10.1016/0028-3908(87)90108-0| title = Baclofen induces catatonia in rats| journal = Neuropharmacology| volume = 26| issue = 9| pages = 1419–1423| year = 1987| last1 = Mehta| first1 = A.| last2 = Ticku| first2 = M.}} 11. ^{{cite journal | doi =10.1016/s0306-3623(97)00279-6| title =GABAB Receptors and Opioid Mechanisms Involved in Homotaurine-Induced Analgesia| journal =General Pharmacology: The Vascular System| volume =30| issue =3| pages =411–415| year =1998| last1 =Serrano| first1 =M.Isabel| last2 =Serrano| first2 =Jose S.| last3 =Fernández| first3 =Ana| last4 =Asadi| first4 =Ihklas| last5 =Serrano-Martino| first5 =M.Carmen}} 12. ^{{cite journal | doi = 10.1046/j.1472-8206.2001.00026.x| title = Role of K+-channels in homotaurine-induced analgesia| journal = Fundamental and Clinical Pharmacology| volume = 15| issue = 3| pages = 167–173| year = 2001| last1 = Serrano| first1 = Maria Isabel| last2 = Serrano| first2 = Jose S.| last3 = Asadi| first3 = Ikhlas| last4 = Fernandez| first4 = Ana| last5 = Serrano-Martino| first5 = Maria Carmen}} 13. ^{{cite journal | doi = 10.1016/s0014-2999(02)01272-4| pmid = 11864639| title = Effects of acute acamprosate and homotaurine on ethanol intake and ethanol-stimulated mesolimbic dopamine release| journal = European Journal of Pharmacology| volume = 437| issue = 1–2| pages = 55–61| year = 2002| last1 = Olive| first1 = M.Foster| last2 = Nannini| first2 = Michelle A.| last3 = Ou| first3 = Christine J.| last4 = Koenig| first4 = Heather N.| last5 = Hodge| first5 = Clyde W.}} 14. ^1 2 {{cite book | last1 = Lednicer | first1 = Daniel | name-list-format = vanc | title = The Organic Chemistry of Drug Synthesis | date = 2008 | publisher = John Wiley & Sons | location = Hoboken | isbn = 978-0-470-18066-2 | edition = 7th | url = https://books.google.com/books?id=N6OAhuiHqiIC&pg=PA15 | page = 15 }} 6 : Anticonvulsants|Sulfonic acids|Amines|Neuroprotective agents|GABAA receptor agonists|GABAB receptor antagonists |
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