From Wikipedia, the free encyclopedia
Chemical compound
Licostinel (
INN) (code name ACEA-1021) is a
competitive,
silent antagonist of the
glycine site of the
NMDA receptor (Kb = 5 nM).
[1]
[2]
[3] It was under investigation by Acea Pharmaceuticals as a
neuroprotective agent for the treatment of
cerebral ischemia associated with
stroke and
head injuries but was ultimately never marketed.
[1]
[2]
[4] In
clinical trials, licostinel did not produce
phencyclidine-like
psychotomimetic effects at the doses tested, though transient
sedation,
dizziness, and
nausea were observed.
[4]
[5] In addition to its actions at the NMDA receptor, licostinel also acts as an antagonist of the
AMPA and
kainate receptors at high concentrations (Kb = 0.9 μM and 2.5 μM, respectively).
[3]
See also
References
- ^
a
b Small DL, Tauskela JS (31 January 2007).
"Glutamate Receptor Pharmacology: Lessons Learned from the Last Decade of Stroke Trials". In Gill S, Pulido O (eds.). Glutamate Receptors in Peripheral Tissue: Excitatory Transmission Outside the CNS. Springer Science & Business Media. pp. 36–.
ISBN
978-0-306-48644-9.
- ^
a
b Gusev EI, Skvortsova VI (30 April 2003).
"Primary Neuroprotection". Brain Ischemia. Springer Science & Business Media. pp. 249–.
ISBN
978-0-306-47694-5.
- ^
a
b Wilding TJ, Huettner JE (March 1996).
"Antagonist pharmacology of kainate- and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-preferring receptors". Molecular Pharmacology. 49 (3): 540–546.
PMID
8643094.
- ^
a
b Boyce SG, Rupniak N (1 January 2002).
"Behavioural studies on the potential of NMDA receptor antagonists as analgesics". In Sirinathsinghji DJ, Hill RG (eds.). NMDA Antagonists As Potential Analgesic Drugs. Springer Science & Business Media. pp. 151–.
ISBN
978-3-7643-6011-5.
-
^ Chizh BA, Headly PM (28 May 2013).
"N-Methyl-D-Aspartate (NMDA) Receptors as Target for Pain Therapy". In Bountra C, Munglani R, Schmidt WK (eds.). Pain: Current Understanding, Emerging Therapies, and Novel Approaches to Drug Discovery. CRC Press. pp. 567–.
ISBN
978-0-203-91125-9.
|
---|
AMPARTooltip α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor | |
---|
KARTooltip Kainate receptor | |
---|
NMDARTooltip N-Methyl-D-aspartate receptor | |
---|
|