PMID- 10608276
OWN - NLM
STAT- MEDLINE
DCOM- 20000118
LR  - 20190726
IS  - 0028-3908 (Print)
IS  - 0028-3908 (Linking)
VI  - 38
IP  - 12
DP  - 1999 Dec
TI  - [3H]ATPA: a high affinity ligand for GluR5 kainate receptors.
PG  - 1811-7
AB  - The pharmacological properties of [3H]ATPA 
      ((RS)-2-amino-3(3-hydroxy-5-tert-butylisoxazol-4-yl)propanoic acid) are 
      described. ATPA is a tert-butyl analogue of AMPA 
      (alpha-amino-3-hydroxy-5-methyl-4-isoxazoleproprionic acid) that has been shown 
      to possess high affinity for the GluR5 subunit of kainate receptors. [3H]ATPA 
      exhibits saturable, high affinity binding to membranes expressing human GluR5 
      (GluR5) kainate receptors (Kd approximately 13 nM). No specific binding was 
      observed in membranes expressing GluR2 and GluR6 receptors. Several compounds 
      known to interact with the GluR5 kainate receptor inhibited [3H]ATPA binding with 
      potencies similar to those obtained for competition of [3H]kainate binding to 
      GluR5. Saturable, high affinity [3H]ATPA binding (Kd approximately 4 nM) was also 
      observed in DRG neuron (DRG) membranes isolated from neonatal rats. The rank 
      order potency of compounds to inhibit [3H]ATPA binding in rat DRG and GluR5 
      membranes were in agreement. These finding demonstrate that [3H]ATPA can be used 
      as a radioligand to examine the pharmacological properties of GluR5 containing 
      kainate receptors.
FAU - Hoo, K
AU  - Hoo K
AD  - Allelix Biopharmaceuticals, Mississauga, Ont., Canada.
FAU - Legutko, B
AU  - Legutko B
FAU - Rizkalla, G
AU  - Rizkalla G
FAU - Deverill, M
AU  - Deverill M
FAU - Hawes, C R
AU  - Hawes CR
FAU - Ellis, G J
AU  - Ellis GJ
FAU - Stensbol, T B
AU  - Stensbol TB
FAU - Krogsgaard-Larsen, P
AU  - Krogsgaard-Larsen P
FAU - Skolnick, P
AU  - Skolnick P
FAU - Bleakman, D
AU  - Bleakman D
LA  - eng
PT  - Journal Article
PL  - England
TA  - Neuropharmacology
JT  - Neuropharmacology
JID - 0236217
RN  - 0 (Excitatory Amino Acid Agonists)
RN  - 0 (Gluk1 kainate receptor)
RN  - 0 (Isoxazoles)
RN  - 0 (Propionates)
RN  - 0 (Receptors, Kainic Acid)
RN  - 140158-50-5 (alpha-amino-3-hydroxy-5-tert-butyl-4-isoxazolepropionate)
RN  - SIV03811UC (Kainic Acid)
SB  - IM
MH  - Animals
MH  - Animals, Newborn
MH  - Cell Line
MH  - Excitatory Amino Acid Agonists/*pharmacokinetics
MH  - Ganglia, Spinal/*metabolism
MH  - Humans
MH  - Isoxazoles/*pharmacokinetics
MH  - Kainic Acid/*metabolism
MH  - Neurons/*metabolism
MH  - Propionates/*pharmacokinetics
MH  - Rats
MH  - Receptors, Kainic Acid/genetics/*metabolism
EDAT- 1999/12/23 00:00
MHDA- 1999/12/23 00:01
CRDT- 1999/12/23 00:00
PHST- 1999/12/23 00:00 [pubmed]
PHST- 1999/12/23 00:01 [medline]
PHST- 1999/12/23 00:00 [entrez]
AID - S0028390899001331 [pii]
AID - 10.1016/s0028-3908(99)00133-1 [doi]
PST - ppublish
SO  - Neuropharmacology. 1999 Dec;38(12):1811-7. doi: 10.1016/s0028-3908(99)00133-1.