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. Nr.: 177947-03-4
- Formel: C26H31FN6O
- Molecular Weight:462.56
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
IC50 & Target
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5-HT1B Receptor |
5-HT1D Receptor |
Cellular Effect
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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. Nr. 177947-03-4
-
Molecular Weight 462.56
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)