Movatterモバイル変換


[0]ホーム

URL:


Jump to content
WikipediaThe Free Encyclopedia
Search

Mibampator

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Mibampator
Clinical data
Other namesLY-451395
Identifiers
  • N-[(2R)-2-[4-[4-[2-(methanesulfonamido)ethyl]phenyl]phenyl]propyl]propane-2-sulfonamide
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC21H30N2O4S2
Molar mass438.60 g·mol−1
3D model (JSmol)
  • 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 nameLY-451395) is apositive allosteric modulator (PAM) of theAMPA receptor (AMPAR), anionotropic glutamate receptor, which was under development byEli Lilly for the treatment ofagitation/aggression inAlzheimer's disease but was never marketed.[1][2] It reachedphase IIclinical trials prior to the discontinuation of its development.[1]

Mibampator belongs to thebiarylpropylsulfonamide group of AMPAR PAMs, which also includesLY-404187,LY-503430, andPF-04958242 among others.[3] It is a "high-impact" AMPAR potentiator, unlike "low-impact" AMPAR potentiators from other classes likeCX-516 and itscongenerfarampator (CX-691, ORG-24448), and is able to elicit comparatively more robust increases in AMPAR signaling.[2] In animals, high-impact AMPAR potentiators enhancecognition andmemory at low doses, but producemotor coordinationdisruptions,convulsions, andneurotoxicity at higher doses.[4]

Mibampator failed to produce cognitive improvement in patients with Alzheimer's disease, though it did show improvements in neuropsychiatric measures.[5] A caveat of the study was that the maximally tolerated dosage of the drug could not be used due totoxicity, and dosages in the same range in rodents notably failed to improve memory-related behavior.[6]

See also

[edit]

References

[edit]
  1. ^ab"Mibampator - AdisInsight".
  2. ^abRoberts BM, Holden DE, Shaffer CL, Seymour PA, Menniti FS, Schmidt CJ, Williams GV, Castner SA (2010). "Prevention of ketamine-induced working memory impairments by AMPA potentiators in a nonhuman primate model of cognitive dysfunction".Behav. Brain Res.212 (1):41–8.doi:10.1016/j.bbr.2010.03.039.PMID 20347881.S2CID 9432930.
  3. ^Froestl W, Muhs A, Pfeifer A (2012). "Cognitive enhancers (nootropics). Part 1: drugs interacting with receptors".J. Alzheimers Dis.32 (4):793–887.doi:10.3233/JAD-2012-121186.PMID 22886028.
  4. ^Ranganathan M, DeMartinis N, Huguenel B, Gaudreault F, Bednar MM, Shaffer CL, Gupta S, Cahill J, Sherif MA, Mancuso J, Zumpano L, D'Souza DC (2017). "Attenuation of ketamine-induced impairment in verbal learning and memory in healthy volunteers by the AMPA receptor potentiator PF-04958242".Mol. Psychiatry.22 (11):1633–1640.doi:10.1038/mp.2017.6.PMID 28242871.S2CID 3691566.
  5. ^Zarate CA, Manji HK (2008)."The role of AMPA receptor modulation in the treatment of neuropsychiatric diseases".Exp. Neurol.211 (1):7–10.doi:10.1016/j.expneurol.2008.01.011.PMC 2441819.PMID 18291371.
  6. ^Buccafusco JJ (2009). "Emerging cognitive enhancing drugs".Expert Opin Emerg Drugs.14 (4):577–89.doi:10.1517/14728210903257796.PMID 19772371.S2CID 20980837.

External links

[edit]
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor
KARTooltip Kainate receptor
NMDARTooltip N-Methyl-D-aspartate receptor


Stub icon

Thisdrug article relating to thenervous system is astub. You can help Wikipedia byexpanding it.

Retrieved from "https://en.wikipedia.org/w/index.php?title=Mibampator&oldid=1277347509"
Categories:
Hidden categories:

[8]ページ先頭

©2009-2025 Movatter.jp