146-36-1
146-36-1
Chemical Structure
Azapetine
- CAS No.: 146-36-1
- Formula:C17H17N
- Molecular Weight:235.32
InChIKey: NYGHGTMKALXFIA-UHFFFAOYSA-N
SMILES: C=CCN1CC2=C(C3=C(C1)C=CC=C3)C=CC=C2
Biological Activity: Azapetine is an antagonist of α1-adrenoceptor, with an IC50 of 0.205 μM at rat α1-adrenoceptor and an IC50 of 1.3 μM at rat α2-adrenoceptor, and exhibits higher selectivity for α1-adrenoceptor than for α2-adrenoceptor. Azapetine functionally blocks postsynaptic α1-adrenoceptors, and at higher concentrations, it blocks presynaptic α2-adrenoceptors, central α-adrenoceptors, and H2 histamine receptors. Azapetine is used in related research on hypotension[1][2][3][4].
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Azapetine | Azapetine is an antagonist of α1-adrenoceptor, with an IC50 of 0.205 μM at rat α1-adrenoceptor and an IC50 of 1.3 μM at rat α2-adrenoceptor, and exhibits higher selectivity for α1-adrenoceptor than for α2-adrenoceptor. Azapetine functionally blocks postsynaptic α1-adrenoceptors, and at higher concentrations, it blocks presynaptic α2-adrenoceptors, central α-adrenoceptors, and H2 histamine receptors. Azapetine is used in related research on hypotension. | |||||||||||||||||||||
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References
- [1]. Ishida Y, et al. Alpha-adrenolytic properties of apogalanthamine and azapetine analogs. Journal of pharmacobio-dynamics. 1985 Nov;8(11):917-23. [Content Brief]
- [2]. MacLeod KM, et al. The effect of several α‑adrenoceptor antagonists on the response to histamine in various tissues. Canadian Journal of Physiology and Pharmacology. 1980 Jan;58(1):1‑8.
- [3]. Tsoucaris-Kupfer D, et al. Furter investigations on the interaction between alpha-adrenoceptor antagonists and the central hypotensive effect of clonidine in rats, rabbits and dogs. Clinical and experimental pharmacology & physiology. 1980 Jul;7(4):355-66.
- [4]. Timmermans PB, et al. Quantitative relationships between alpha-adrenergic activity and binding affinity of alpha-adrenoceptor agonists and antagonists. Journal of medicinal chemistry. 1984 Apr;27(4):495-503. [Content Brief]
