1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Azapetine

Azapetine is an α-adrenergic receptor antagonist, with a IC50 of 0.205 μM against rat α1-adrenergic receptors and a IC50 of 1.3 μM against rat α2-adrenergic receptors. Azapetine blocks α1/α2-adrenergic receptor-mediated contraction of blood vessels and vascular smooth muscles. Azapetine can be used for the research of peripheral vascular diseases.

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Azapetine

Azapetine Chemical Structure

CAS No. : 146-36-1

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Description

Azapetine is an α-adrenergic receptor antagonist, with a IC50 of 0.205 μM against rat α1-adrenergic receptors and a IC50 of 1.3 μM against rat α2-adrenergic receptors. Azapetine blocks α1/α2-adrenergic receptor-mediated contraction of blood vessels and vascular smooth muscles. Azapetine can be used for the research of peripheral vascular diseases[1].

IC50 & Target[1]

rat α1-adrenergic receptor

0.205 μM (IC50)

rat α2-adrenergic receptor

1.3 μM (IC50)

In Vitro

Azapetine (45-60 min) exhibits higher binding affinity for α1-adrenergic receptors than for α2-adrenergic receptors in isolated rat brain cell membranes, with an IC50 of 0.205 μM for α1-adrenergic receptors and 1.3 μM for α2-adrenergic receptors[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Azapetine (intravenous administration) exhibits in vivo functional blockade selectivity for α1-adrenergic receptors over α2-adrenergic receptors in normotensive decerebrate-spinal Wistar rats, with a logarithmic selectivity ratio of 1.21[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

235.32

Formula

C17H17N

CAS No.
SMILES

C=CCN1CC2=C(C3=C(C1)C=CC=C3)C=CC=C2

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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    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.

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Azapetine
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HY-181635
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