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AVN-101

Chemical Structure : AVN-101

CAS No.: 1025725-91-0

AVN-101 (AVN101)

Catalog No.: PC-61504Not For Human Use, Lab Use Only.

A higly potent, orally bioavailable, BBB permeable 5-HT7 receptor antagonist with Ki of 153 pM, with slightly lesser potency toward 5-HT6, 5-HT2A and 5HT-2C (Ki = 1.2-2.0  nM).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A higly potent, orally bioavailable, BBB permeable 5-HT7 receptor antagonist with Ki of 153 pM, with slightly lesser potency toward 5-HT6, 5-HT2A and 5HT-2C (Ki = 1.2-2.0  nM); also exhibits a rather high affinity toward histamine H1 (Ki = 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki = 0.41-3.6 nM) receptors; demonstrates reasonable anxiolytic and anti-depressive activities in animal models of CNS diseases with low safety concerns.

Anxiety

Phase 2 Clinical

Physicochemical Properties

M.Wt 304.437
Formula C21H24N2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2,8-dimethyl-5-phenethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole

References

1. Ivachtchenko AV, et al. J Alzheimers Dis. 2016 May 25;53(2):583-620.

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