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词条 S-17092
释义

  1. See also

  2. References

{{drugbox
| 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

  • C16 (PKR inhibitor)
  • UK-414,495

References

1. ^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}}
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}}
{{Nootropics}}{{nervous-system-drug-stub}}

6 : Hydrolase inhibitors|Nootropics|Carboxamides|Indoles|Thiazolidines|Cyclopropanes

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