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5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, with weak α1 adrenoceptor blocking activity.

5-HT2 antagonist 1 shows 45%, 88%, 93% inhibition of 10 μM erotonin-induced contraction at 10 nM, 100 nM, 1000 nM, respectively, in guinea pig mesentcric artery. 5-HT2 antagonist 1 causes 1% and 10% inhibition of 10 μM norepinephrine-induced contraction at 10 and 100 nM, respectively, in guinea pig aorta[1].

[1]. Mizuno A, et al. Synthesis and serotonin 2 (5-HT2) receptor antagonist activity of 5-aminoalkyl-substituted pyrrolo[3,2-c]azepines and related compounds. Chem Pharm Bull (Tokyo). 2000 May;48(5):623-35.

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