L-772405
L-772405 is a selective 5-HT1D receptor agonist with the Ki values of 318, 29 and > 1000 nM aganist guinea pig 5-HT1B receptor, guinea pig 5-HT1D receptor and rat 5-HT rransporter, respectively. L-772405 decreases the potassium-induced outflow of 5-HT with an IC50 value of 240 nM.
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- CAS No.: 177947-03-4
- Formule: C26H31FN6O
- Masse moléculaire:462.56
-
Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
|
5-HT1B Receptor |
5-HT1D Receptor |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.8 nM
Compound: 80
|
Agonist-induced [35S]- GTPgammaS binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor
Agonist-induced [35S]- GTPgammaS binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor
|
[PMID: 10585208] |
| CHO | IC50 |
>10000 nM
Compound: 80
|
Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1F receptor stably expressed in CHO cells
Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1F receptor stably expressed in CHO cells
|
[PMID: 10585208] |
| CHO | IC50 |
>10000 nM
Compound: 80
|
Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 5A receptor stably expressed in CHO cells
Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 5A receptor stably expressed in CHO cells
|
[PMID: 10585208] |
| CHO | IC50 |
>10000 nM
Compound: 80
|
Compound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 6 receptor stably expressed in CHO cells
Compound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 6 receptor stably expressed in CHO cells
|
[PMID: 10585208] |
| CHO | IC50 |
0.9 nM
Compound: 80
|
Displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells
Displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1D receptor stably expressed in CHO cells
|
[PMID: 10585208] |
| CHO | IC50 |
1100 nM
Compound: 80
|
Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 2A receptor stably expressed in CHO cells
Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 2A receptor stably expressed in CHO cells
|
[PMID: 10585208] |
| CHO | IC50 |
150 nM
Compound: 80
|
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
Displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1B receptor stably expressed in CHO cells
|
[PMID: 10585208] |
| CHO | IC50 |
540 nM
Compound: 80
|
Compound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 7 receptor stably expressed in CHO cells
Compound was tested for the displacement of [3H]5-HT binding to cloned rat 5-hydroxytryptamine 7 receptor stably expressed in CHO cells
|
[PMID: 10585208] |
| CHO | IC50 |
66 nM
Compound: 80
|
Compound was tested for the displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1A receptor stably expressed in CHO cells
Compound was tested for the displacement of [3H]5-HT binding to cloned 5-hydroxytryptamine 1A receptor stably expressed in CHO cells
|
[PMID: 10585208] |
| CHO | IC50 |
>10000 nM
Compound: 80
|
Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1E receptor stably expressed in CHO cells
Compound was tested for the displacement of [3H]5-HT binding to cloned human 5-hydroxytryptamine 1E receptor stably expressed in CHO cells
|
[PMID: 10585208] |
| CHO | EC50 |
1.1 nM
Compound: 6h
|
Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor.
Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor.
|
[PMID: 9357514] |
| CHO | IC50 |
0.9 nM
Compound: 6h
|
Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
|
[PMID: 9357514] |
| CHO | IC50 |
185 nM
Compound: 6h
|
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
|
[PMID: 9357514] |
| CHO | EC50 |
1.1 nM
Compound: 1
|
Agonist induced [35S]GTP-gamma-S, binding in CHO cells expressing 5-HT 1d receptor
Agonist induced [35S]GTP-gamma-S, binding in CHO cells expressing 5-HT 1d receptor
|
[PMID: 9667955] |
| CHO | IC50 |
0.9 nM
Compound: 1
|
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells
Displacement of [3H]5-HT from human 5-hydroxytryptamine 1D receptor expressed in CHO cells
|
[PMID: 9667955] |
Chemical Information
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CAS No. 177947-03-4
-
Masse moléculaire 462.56
-
Formule C26H31FN6O
-
SMILES
OC[C@@H](C1=CC=C(C=C1)F)NC(CC2)CCN2CCCC3=CNC4=CC=C(N5C=NN=C5)C=C34
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Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)