Determination of δ-opioid receptors in NG108-15 cells
The δ-opioid receptors in mouse neuroblastoma X rat glioma hybridoma NG108-15 cells were characterized by receptor binding and cAMP assays. Saturation binding assays using [ 3H]naltrindole, [ 3H][ d-Pen 2, d-Pen 5]enkephalin (DPDPE) or [ 3H][ d-Ser 2,Leu 5,Thr 6]enkephalin (DSLET) gave similar bindi...
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| Published in | European journal of pharmacology Vol. 319; no. 1; pp. 109 - 114 |
|---|---|
| Main Authors | , , , |
| Format | Journal Article |
| Language | English |
| Published |
Amsterdam
Elsevier B.V
01.01.1997
Elsevier |
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| Abstract | The δ-opioid receptors in mouse neuroblastoma X rat glioma hybridoma NG108-15 cells were characterized by receptor binding and cAMP assays. Saturation binding assays using [
3H]naltrindole, [
3H][
d-Pen
2,
d-Pen
5]enkephalin (DPDPE) or [
3H][
d-Ser
2,Leu
5,Thr
6]enkephalin (DSLET) gave similar binding capacities (
B
max). Competition binding assays showed that DPDPE and DSLET have similar affinity for the [
3H]DPDPE or [
3H]DSLET binding sites. The rank order of potency of competition with [
3H]DPDPE and [
3H]DSLET was similar: naltriben ∼ DSLET ≥ DPDPE > 7-benzylidenenaltrexone (BNTX). Both DPDPE and DSLET were found to decrease cAMP formation. The action of DSLET was antagonized by naltriben but not BNTX, while the action of DPDPE was reversed by both antagonists. Therefore, the δ-opioid receptor in NG108-15 cells has similar affinity for the agonists DPDPE and DSLET, and a higher affinity for the antagonist naltriben than BNTX. |
|---|---|
| AbstractList | The δ-opioid receptors in mouse neuroblastoma X rat glioma hybridoma NG108-15 cells were characterized by receptor binding and cAMP assays. Saturation binding assays using [
3H]naltrindole, [
3H][
d-Pen
2,
d-Pen
5]enkephalin (DPDPE) or [
3H][
d-Ser
2,Leu
5,Thr
6]enkephalin (DSLET) gave similar binding capacities (
B
max). Competition binding assays showed that DPDPE and DSLET have similar affinity for the [
3H]DPDPE or [
3H]DSLET binding sites. The rank order of potency of competition with [
3H]DPDPE and [
3H]DSLET was similar: naltriben ∼ DSLET ≥ DPDPE > 7-benzylidenenaltrexone (BNTX). Both DPDPE and DSLET were found to decrease cAMP formation. The action of DSLET was antagonized by naltriben but not BNTX, while the action of DPDPE was reversed by both antagonists. Therefore, the δ-opioid receptor in NG108-15 cells has similar affinity for the agonists DPDPE and DSLET, and a higher affinity for the antagonist naltriben than BNTX. The delta -opioid receptors in mouse neuroblastoma X rat glioma hybridoma NG108-15 cells were characterized by receptor binding and cAMP assays. Saturation binding assays using [ super(3)H]naltrindole, [ super(3)H][D-Pen super(2),D-Pen super(5)]enkephalin (DPDPE) or [ super(3)H][D-Ser super(2),Leu super(5),Thr super(6)]enkephalin (DSLET) gave similar binding capacities (B sub(max)). Competition binding assays showed that DPDPE and DSLET have similar affinity for the [ super(3)H]DPDPE or [ super(3)H]DSLET binding sites. The rank order of potency of competition with [ super(3)H]DPDPE and [ super(3)H]DSLET was similar: naltriben similar to DSLET greater than or equal to DPDPE > 7-benzylidenenaltrexone (BNTX). Both DPDPE and DSLET were found to decrease cAMP formation. The action of DSLET was antagonized by naltriben but not BNTX, while the action of DPDPE was reversed by both antagonists. Therefore, the delta -opioid receptor in NG108-15 cells has similar affinity for the agonists DPDPE and DSLET, and a higher affinity for the antagonist naltriben than BNTX. |
| Author | Holmes, Blythe B. Ho, Begonia Y. Fujimoto, James Zhao, Jinchuan |
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| Cites_doi | 10.1016/0024-3205(92)90138-F 10.1016/0024-3205(93)90240-4 10.1016/0024-3205(90)90462-Z 10.1016/0165-6147(88)90239-8 10.1016/0024-3205(91)90397-T 10.1523/JNEUROSCI.14-04-01920.1994 10.1016/0024-3205(94)00738-1 10.1016/0014-5793(77)80186-5 10.1016/0014-2999(92)90167-3 10.1126/science.1335167 10.1016/0003-2697(76)90527-3 10.1146/annurev.pa.30.040190.001011 10.1016/0165-6147(92)90062-B |
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| Keywords | BNTX (7-benzylidenenaltrexone) δ-Opioid receptor NG108-15 cell DPDPE ([ d-Pen 2, d-Pen 5]enkephalin) DSLET ([ d-Ser 2,Leu 5,Thr 6]enkephalin) Naltriben Molecular structure Opiate receptor δ Rodentia Cyclic AMP Functional analysis Identification In vitro Vertebrata Biological fixation Mammalia Structure activity relation Mouse Animal Established cell line Affinity |
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| SubjectTerms | Biological and medical sciences BNTX (7-benzylidenenaltrexone) Cell receptors Cell structures and functions DPDPE ([ d-Pen 2, d-Pen 5]enkephalin) DSLET ([ d-Ser 2,Leu 5,Thr 6]enkephalin) Fundamental and applied biological sciences. Psychology Molecular and cellular biology Naltriben Neuropeptide receptors NG108-15 cell δ-Opioid receptor |
| Title | Determination of δ-opioid receptors in NG108-15 cells |
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