AVN-101
AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
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- CAS. Nr.: 1025725-91-0
- Formel: C21H24N2
- Molecular Weight:304.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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5-HT2A Receptor |
5-HT2C Receptor |
5-HT6 Receptor |
5-HT7 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.158 μM
Compound: 4(2)
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Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
Antagonist activity at human recombinant 5HT6 receptor expressed in HEK293 cells assessed as inhibition of serotonin-induced increase in intracellular cAMP level by cAMP-LANCE method
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[PMID: 19945877] |
| SK-N-SH | IC50 |
0.04 μM
Compound: 4(2)
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Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as histamine-induced maximum intracellular calcium spike at phase 1 treated 10 to 15 seconds before histamine challenge
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[PMID: 19945877] |
| SK-N-SH | IC50 |
0.146 μM
Compound: 4(2)
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Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
Antagonist activity at histamine H1 receptor in human SK-N-SH cells assessed as reduction of histamine-induced intracellular calcium spike at phase 2 treated 20 to 30 seconds after histamine challenge
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[PMID: 19945877] |
AVN-101 shows some ability to compete with radio-labeled ligands for both the histamine H1 (Ki = 0.58 nM) and H2 receptors (Ki = 89 nM) while being totally inactive on H3 receptor[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
AVN-101 (0.02-5 mg/kg; i.p.; once) prevents Scopolamine (HY-N0296)-induced amnesia in a passive avoidance test in mice when administered at a dose of 0.05 mg/kg[1].
AVN-101 (0.2, 1, and 5 mg/kg) increases the time spent in the open arms of the elevated plus maze in mice[1].
AVN-101 is poorly stable in murine plasma: by the end of 30-min incubation at room temperature, the residual amount of the original compound is reduced to 16%. At the same time, AVN-101 shows better stability in plasma samples taken from monkey and human: by the end of the 30-min incubation at room temperature, the residual amount of the original compound is reduced to only 45% and 68%, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/C mice bearing porsolt forced swim and the tail suspension tests[1].
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Dosage:0.05 mg/kg
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Administration:i.p.; once daily; for 4 days
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Result:Reduced immobility in the forced swim test in mice.
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Animal Model:Male BALB/c mice were used with amnesiac models based on either Scopolamine-induced memory impairment[1].
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Dosage:0.02 mg/kg, 0.05 mg/kg, 0.2 mg/kg, 0.5 mg/kg, 1 mg/kg, and 5 mg/kg
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Administration:i.p.; once
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Result:Prevented scopolamine-induced amnesia in a passive avoidance test in mice
Chemical Information
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CAS. Nr. 1025725-91-0
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Molecular Weight 304.43
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Formel C21H24N2
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SMILES
CC1=CC2=C(N(CCC3=CC=CC=C3)C4=C2CN(C)CC4)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AVN-101 Related Classifications
HY-117046 Related Classifications
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