Abstract
Desglycinyl remacemide (DGR), a biologically active metabolite of remacemide, was radiolabeled in an attempt to develop a ligand binding assay to identify its site of action. Incubation of the radioligand with membranes obtained from P2 fractions of whole rat brain revealed a single population of specific [3H]-DGR binding sites having a K(d) of 290 nM and a B(max) of 1.3 pmole/mg protein. The specific binding of [3H]-DGR is most enriched in the P2 subcellular fraction and is heterogeneously distributed throughout the brain. The binding of [3H]-DGR to rat brain membranes was inhibited most potently by MK-801 and SKF-10,047. In contrast, haloperidol, and other sigma receptor-active agents, were relatively inactive at this site. These data suggest that DGR interacts with a channel blocking site on the NMDA receptor.
| Original language | English |
|---|---|
| Pages (from-to) | 46-50 |
| Number of pages | 5 |
| Journal | Brain Research |
| Volume | 827 |
| Issue number | 1-2 |
| DOIs | |
| State | Published - May 8 1999 |
| Externally published | Yes |
Fingerprint
Keywords
- Anticonvulsant
- Desglycinyl remacemide
- MK- 801
- Phencyclidine
- Remacemide
- SKF-10,047
ASJC Scopus subject areas
- Neuroscience(all)
- Clinical Neurology
- Developmental Biology
- Molecular Biology
Cite this
Binding of [3H]desglycinyl remacemide to rat brain membranes : Association with the benzomorphan attachment site of the N-methyl-D-aspartic acid receptor channel. / Ahmed, Mahmoud; Mather, A.; Enna, S. J.
In: Brain Research, Vol. 827, No. 1-2, 08.05.1999, p. 46-50.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Binding of [3H]desglycinyl remacemide to rat brain membranes
T2 - Association with the benzomorphan attachment site of the N-methyl-D-aspartic acid receptor channel
AU - Ahmed, Mahmoud
AU - Mather, A.
AU - Enna, S. J.
PY - 1999/5/8
Y1 - 1999/5/8
N2 - Desglycinyl remacemide (DGR), a biologically active metabolite of remacemide, was radiolabeled in an attempt to develop a ligand binding assay to identify its site of action. Incubation of the radioligand with membranes obtained from P2 fractions of whole rat brain revealed a single population of specific [3H]-DGR binding sites having a K(d) of 290 nM and a B(max) of 1.3 pmole/mg protein. The specific binding of [3H]-DGR is most enriched in the P2 subcellular fraction and is heterogeneously distributed throughout the brain. The binding of [3H]-DGR to rat brain membranes was inhibited most potently by MK-801 and SKF-10,047. In contrast, haloperidol, and other sigma receptor-active agents, were relatively inactive at this site. These data suggest that DGR interacts with a channel blocking site on the NMDA receptor.
AB - Desglycinyl remacemide (DGR), a biologically active metabolite of remacemide, was radiolabeled in an attempt to develop a ligand binding assay to identify its site of action. Incubation of the radioligand with membranes obtained from P2 fractions of whole rat brain revealed a single population of specific [3H]-DGR binding sites having a K(d) of 290 nM and a B(max) of 1.3 pmole/mg protein. The specific binding of [3H]-DGR is most enriched in the P2 subcellular fraction and is heterogeneously distributed throughout the brain. The binding of [3H]-DGR to rat brain membranes was inhibited most potently by MK-801 and SKF-10,047. In contrast, haloperidol, and other sigma receptor-active agents, were relatively inactive at this site. These data suggest that DGR interacts with a channel blocking site on the NMDA receptor.
KW - Anticonvulsant
KW - Desglycinyl remacemide
KW - MK- 801
KW - Phencyclidine
KW - Remacemide
KW - SKF-10,047
UR - http://www.scopus.com/inward/record.url?scp=0033535631&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0033535631&partnerID=8YFLogxK
U2 - 10.1016/S0006-8993(99)01263-9
DO - 10.1016/S0006-8993(99)01263-9
M3 - Article
VL - 827
SP - 46
EP - 50
JO - Brain Research
JF - Brain Research
SN - 0006-8993
IS - 1-2
ER -