2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. 5-HT Receptor Histamine Receptor Adrenergic Receptor
  4. 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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AVN-101 Chemical Structure

AVN-101 Chemical Structure

CAS No. : 1025725-91-0

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Description

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[1].

IC50 & Target

5-HT2A Receptor

 

5-HT2C Receptor

 

5-HT6 Receptor

 

5-HT7 Receptor

 

In Vitro

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 Related Antibodies
In Vivo

AVN-101 (0.05 mg/kg; i.p.; once daily; for 4 days) reduces immobility in the forced swim test in mice[1].
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.

Animal Model: Balb/C mice bearing porsolt forced swim and the tail suspension tests[1].
Dosage: 0.05 mg/kg
Administration: i.p.; once daily; for 4 days
Result: Reduced immobility in the forced swim test in mice.
Animal Model: Male BALB/c mice were used with amnesiac models based on either Scopolamine-induced memory impairment[1].
Dosage: 0.02 mg/kg, 0.05 mg/kg, 0.2 mg/kg, 0.5 mg/kg, 1 mg/kg, and 5 mg/kg
Administration: i.p.; once
Result: Prevented scopolamine-induced amnesia in a passive avoidance test in mice
Molecular Weight

304.43

Formula

C21H24N2
CAS No.
SMILES

CC1=CC2=C(N(CCC3=CC=CC=C3)C4=C2CN(C)CC4)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AVN-101 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AVN-1011025725-91-0AVN101AVN 1015-HT ReceptorHistamine ReceptorAdrenergic ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorBeta Receptorbrain-penetrantorally active5-HT7 receptoranxiety disordersdepressionschizophreniaAlzheimer’s diseaseand multiple sclerosisInhibitorinhibitorinhibit

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