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Jpn J Pharmacol. 1999 Nov;81(3):313-5.

Antagonistic effect of N-methyltyramine on alpha2-adrenoceptor in mice.

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Products Safety & Alcohol Science Laboratory, Suntory Limited, Mishima-gun, Osaka, Japan.


We examined the effect of N-methyltyramine (NMT) on alpha2-adrenoceptor. NMT (10(-8)-10(-3) M) inhibited the binding of [3H]p-aminoclonidine to alpha2-adrenoceptor dose-dependently. However, the IC50 value for NMT (5.53 x 10(-6) M) was higher than that for RX821002, an alpha2-adrenoceptor antagonist (1.07 x 10(-8) M). RX821002 (5 mg/kg, i.p.) inhibited hypermotility induced by scopolamine (8 mg/kg, s.c.) in male ddY mice. NMT (20 or 100 mg/kg, i.p.) was found to have a dose-dependent inhibitory effect similar to that of RX821002. These findings indicate that NMT has the properties of an alpha2-adrenoceptor antagonist. However, the affinity of NMT for alpha2-adrenoceptor is weaker than that of RX821002.

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