Mibampator

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Mibampator
Systematic (IUPAC) name
N-[(2R)-2-[4-[4-[2-(methanesulfonamido)ethyl]phenyl]phenyl]propyl]propane-2-sulfonamide
Identifiers
CAS Number 375345-95-2
PubChem CID: 9889366
ChemSpider 8065037
UNII A9V5BW73UU
KEGG D09931
ChEMBL CHEMBL1277001
Synonyms LY-451395
Chemical data
Formula C21H30N2O4S2
Molecular mass 438.601 g/mol
  • C[C@@H](CNS(=O)(=O)C(C)C)C1=CC=C(C=C1)C2=CC=C(C=C2)CCNS(=O)(=O)C
  • InChI=1S/C21H30N2O4S2/c1-16(2)29(26,27)23-15-17(3)19-9-11-21(12-10-19)20-7-5-18(6-8-20)13-14-22-28(4,24)25/h5-12,16-17,22-23H,13-15H2,1-4H3/t17-/m0/s1
  • Key:ULRDYYKSPCRXAJ-KRWDZBQOSA-N

Mibampator (developmental code name LY-451395) is a positive allosteric modulator of the AMPA receptor (AMPAR), an ionotropic glutamate receptor, which was under development by Eli Lilly for the treatment of agitation/aggression in Alzheimer's disease but was never marketed.[1][2] It is a "high-impact" AMPAR potentiator, unlike "low-impact" AMPAR potentiators like CX-516 and its congener farampator (CX-691), and is able to elicit more robust increases in AMPAR signaling.[2] In animals, high-impact AMPAR potentiators enhance cognition and memory at low doses, but produce motor coordination disruptions, convulsions, and neurotoxicity at higher doses.[3] Mibampator failed to produce cognitive improvement in patients with Alzheimer's disease, though it did show improvements in neuropsychiatric measures.[4] A caveat of the study was that the maximally tolerated dosage of the drug could not be used due to toxicity, and dosages in the same range in rodents notably failed to improve memory-related behavior.[5] Mibampator reached phase II clinical trials prior to the discontinuation of its development.[1]

See also

References

  1. 1.0 1.1 http://adisinsight.springer.com/drugs/800024387
  2. 2.0 2.1 Lua error in package.lua at line 80: module 'strict' not found.
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External links



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