neuropharm flash card lec 5
neuropharm lecture 5
regions of brain where NR1 can be found
everywhere there is an AMPA receptor
neuropharm lecture 5
NR2a and NR2b can be found
in the forebrain and hippocampus
neuropharm lecture 5
NR2c can be found
almost exclusively in cerebellum and olfactory bulb
neuropharm lecture 5
NR2d can be found
cerebellum, midbrain, brainstem and olfactory bulb
neuropharm lecture 5
unique structure of NRs
2NR1+2NR2 ( dual heterodimer= tetramer
neuropharm lecture 5
NR2 bind
Glutamate
neuropharm lecture 5
NR1 bind
Serine
neuropharm lecture 5
Therapeutic uses of NMDARs
dissociative anesthesia, cough suppression, helping with learning and memory (ex: Alzhaimer), Ischemia neuroprotection, stroke and drowning
neuropharm lecture 5
Non- therapeutic uses of NMDARs
Dissociative hallucinogen
neuropharm lecture 5
NR1 antagonist that bind to PCP
PCP, angeldustin, MK801, Ketamine, memantine, dextromethorphan, nitrous oxide
neuropharm lecture 5
effects of NR1 antagonist that bind to PCP
Dissociative anesthesia
neuropharm lecture 5
Mg2+
NR1 antagonist that blocks open channels
neuropharm lecture 5
PO4-
endogenous positive modulator(phosporylation) for NR1. it prolongs open channel
neuropharm lecture 5
Ethanol
antagonist for NR1 that binds to ethanol and prevents channel openning
neuropharm lecture 5
Ifenprodil
exogenous antagonist that bind to polyamine site of NR2 and decrease glutamate binding
neuropharm lecture 5
two endogenous antagonist that bind to polyamine site of NR2
Cadaverine, putrescine
neuropharm lecture 5
heavy metals
Decrease glutamate binding affinity
neuropharm lecture 5
MK801
blocks excitotoxic apoptosis
neuropharm lecture 5
competative agonist for NR2
NMDA, Glutamate(endogenous)
neuropharm lecture 5
competative antagonist for NR2
APV (AP5), CPP
neuropharm lecture 5
what can NR non-competitive antagonist cause in high doses?
impair learning
neuropharm lecture 5
NR1 agonists
serine and glycine
neuropharm lecture 5
NR1 partial agonist
DCS ( D- cycloserine)
neuropharm lecture 5
NR1 competative antagonist
Kynurenate (Kyn)- endogenous, 5,7-Cl-Ky,
neuropharm lecture 5
Glutamate EPSPs
heterogenous (mediated by multiple receptor type)
neuropharm lecture 5
NMDA gene family
NR1, NR2a, NR2b, NR2c, NR2d, NR3a, NR3b
neuropharm lecture 5
Gene families of AMPA
GLuR1, GLuR2, GLuR3
neuropharm lecture 5
Hiil coefficient for glutmate binding of NR2
two
neuropharm lecture 5
Hill coefficient for serine binding of NR1
two
neuropharm lecture 5
Polyamine site
Where other types of receptors can bind
neuropharm lecture 5
the only type of NT receptor system that requires 2 distinct sets of signals for activation
NMDA receptors
neuropharm lecture 5
one of the most important functions of NMDA receptors
They are sites for Ca2+ influx