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词条 Lecozotan
释义

  1. Method of action

  2. References

{{Drugbox
| verifiedrevid = 444728200
| IUPAC_name = 4-Cyano-N-[(2R)-2-[4-(2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl]propyl]-N-2-pyridinylbenzamide hydrochloride
| image = Lecozotan_structure.svg
| tradename =
| pregnancy_category =
| legal_status =
| routes_of_administration =
| bioavailability =
| metabolism =
| elimination_half-life =
| excretion =
| PubChem = 10116877
| DrugBank =
| ChemSpiderID = 8292400
| ChEMBL = 372205
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 48854OTZ5E
| KEGG_Ref = {{keggcite|correct|kegg}}
| KEGG = D04683
| C=28 | H=30 | Cl=1 | N=5 | O=3
| molecular_weight = 520.021 g/mol
| CAS_number = 434283-16-6
| ATC_prefix =
| ATC_suffix =
| smiles = C[C@H](CN(C1=CC=CC=N1)C(=O)C2=CC=C(C=C2)C#N)N3CCN(CC3)C4=C5C(=CC=C4)OCCO5
| StdInChI = 1S/C28H29N5O3/c1-21(31-13-15-32(16-14-31)24-5-4-6-25-27(24)36-18-17-35-25)20-33(26-7-2-3-12-30-26)28(34)23-10-8-22(19-29)9-11-23/h2-12,21H,13-18,20H2,1H3/t21-/m1/s1
| StdInChIKey = NRPQELCNMADTOZ-OAQYLSRUSA-N
}}Lecozotan is an investigational drug by Wyeth tested for improvement of cognitive functions of Alzheimer's disease patients.[1]{{As of|June 2008}}, the first Phase III clinical trial has been completed.[2]

Method of action

Lecozotan is a competitive, selective 5-HT1A receptor antagonist[3]

which enhances the potassium-stimulated release of acetylcholine and glutamate.[4]

References

1. ^{{cite journal | author = H. Spreitzer | date = August 13, 2008 | title = Neue Wirkstoffe - Lecozotan | journal = Österreichische Apothekerzeitung | issue = 17/2007 | pages = 805 | language = German }}
2. ^ClinicalTrials
3. ^{{cite journal|last=Schlechter|first=LE|date=June 10, 2005|title=Lecotozan (SRA-333): A selective serotonin1A receptor antagonist that enhances the stimulated release of glutamate and acetylcholine in the hippocampus and promotes procognitive effects|journal=Journal of Pharmacology and Experimental Therapeutics|url=http://jpet.aspetjournals.org/cgi/content/short/jpet.105.086363v1|pmid=15951399|doi=10.1124/jpet.105.086363|volume=314|pages=1274–89|last2=Smith|first2=DL|last3=Rosenzweig-Lipson|first3=S|last4=Sukoff|first4=SJ|last5=Dawson|first5=LA|last6=Marquis|first6=K|last7=Jones|first7=D|last8=Piesla|first8=M|last9=Andree|first9=T|last10=Nawoschik|first10=S|last11=Harder|first11=J. A.|last12=Womack|first12=M. D.|last13=Buccafusco|first13=J|last14=Terry|first14=A. V.|last15=Hoebel|first15=B|last16=Rada|first16=P|last17=Kelly|first17=M|last18=Abou-Gharbia|first18=M|last19=Barrett|first19=J. E.|last20=Childers|first20=W|issue=3|display-authors=8}}
4. ^{{cite journal | author = Childers, WE Jr, Harrison, BL, Abou-Gharbia, MA, Raje, S, Parks, V, Pangalos, MN, Schechter, LE | title = Lecozotan Hydrochloride | journal = Drugs of the Future | year = 2007 | volume = 32 | issue = 5 | pages = 399–407 | url = http://journals.prous.com/journals/servlet/xmlxsl/pk_journals.xml_summary_pr?p_JournalId=2&p_RefId=1092901&p_IsPs=N | doi = 10.1358/dof.2007.032.05.1092901 }}
{{Antidementia}}{{Nootropics}}{{Serotonergics}}{{nervous-system-drug-stub}}

7 : 5-HT1A antagonists|Antidementia agents|Piperazines|Pyridines|Nitriles|Benzodioxans|Benzamides

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