词条 | S-17092 |
释义 |
| Verifiedfields = changed | Watchedfields = changed | verifiedrevid = 415304348 | IUPAC_name = [(2S,3aS,7aS)-1([(R,R)-2-phenylcyclopropyl]- carbonyl)-2-([thiazolidin-3-yl]carbonyl)octahydro-1H-indole | image = S-17092.svg | width = 250 | CAS_number_Ref = {{cascite|correct|??}} | CAS_number = | ATC_prefix = | ATC_suffix = | PubChem = 9977327 | DrugBank_Ref = {{drugbankcite|correct|drugbank}} | DrugBank = | ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}} | ChemSpiderID = 8152919 | smiles = O=C(N1CCCC1)[C@H]4N(C(=O)[C@H]3[C@H](c2ccc(F)cc2)C3)[C@H]5CCCC[C@H]5C4 | StdInChI_Ref = {{stdinchicite|changed|chemspider}} | StdInChI = 1S/C23H29FN2O2/c24-17-9-7-15(8-10-17)18-14-19(18)22(27)26-20-6-2-1-5-16(20)13-21(26)23(28)25-11-3-4-12-25/h7-10,16,18-21H,1-6,11-14H2/t16-,18-,19+,20-,21-/m0/s1 | StdInChIKey_Ref = {{stdinchicite|changed|chemspider}} | StdInChIKey = JNUXCIMICQKTPX-RQUKQETFSA-N | C=23 | H=29 | F=1 | N=2 | O=2 | molecular_weight = 384.486 g/mol | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = Investigational New Drug | legal_status = | routes_of_administration = }}S-17092 is a drug which acts as a selective inhibitor of the enzyme prolyl endopeptidase.[1] This enzyme is involved in the metabolic breakdown of a number of neuropeptide neurotransmitters in the brain,[2][3] and so inhibiting the action of the enzyme increases the activity of these neuropeptides. This produces nootropic effects which make S-17092 a promising and novel treatment for neurodegenerative conditions such as Alzheimer's disease and Parkinson's disease.[4][5] See also
References1. ^Barelli H, Petit A, Hirsch E, Wilk S, De Nanteuil G, Morain P, Checler F. S 17092-1, a highly potent, specific and cell permeant inhibitor of human proline endopeptidase. Biochemical and Biophysical Research and Communications. 1999 Apr 21;257(3):657-61. {{PMID|10208839}} {{Nootropics}}{{nervous-system-drug-stub}}2. ^Bellemère G, Morain P, Vaudry H, Jégou S. Effect of S 17092, a novel prolyl endopeptidase inhibitor, on substance P and alpha-melanocyte-stimulating hormone breakdown in the rat brain. Journal of Neurochemistry. 2003 Mar;84(5):919-29. {{DOI|10.1046/j.1471-4159.2003.01536.x}} {{PMID|12603817}} 3. ^Bellemère G, Vaudry H, Morain P, Jégou S. Effect of prolyl endopeptidase inhibition on arginine-vasopressin and thyrotrophin-releasing hormone catabolism in the rat brain. Journal of Neuroendocrinology. 2005 May;17(5):306-13. {{PMID|15869566}} 4. ^Morain P, Lestage P, De Nanteuil G, Jochemsen R, Robin JL, Guez D, Boyer PA. S 17092: a prolyl endopeptidase inhibitor as a potential therapeutic drug for memory impairment. Preclinical and clinical studies. CNS Drug Reviews. 2002 Spring;8(1):31-52. {{PMID|12070525}} 5. ^Morain P, Boeijinga PH, Demazières A, De Nanteuil G, Luthringer R. Psychotropic profile of S 17092, a prolyl endopeptidase inhibitor, using quantitative EEG in young healthy volunteers. Neuropsychobiology. 2007;55(3-4):176-83. {{PMID|17700042}} 6 : Hydrolase inhibitors|Nootropics|Carboxamides|Indoles|Thiazolidines|Cyclopropanes |
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