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1-(o-Methoxyphenyl)piperazine is a metabolite of drugs bearing a methoxyphenylpiperazine side-chain.

Drugs bearing an o-methoxyphenylpiperazine (oOCH3PP) moiety in the side-chain of their molecule may form oOCH3PP during biotransformation in-vivo in the rat. This has been verified by combined gas chromatography-mass spectrometry of urine from rats given orally a series of relatively new o-methoxyphenylpiperazine-substituted derivatives. The metabolite is reported to be biochemically and pharmacologically active and therefore its formation may have pharmacological significance, at least for derivatives undergoing extensive cleavage of the arylpiperazine side-chain.

Animals↗

An alpha-adrenoceptor-blocking action of SGB-483, a new piperazine antihypertensive agent in isolated vascular smooth muscles.

SGB (10(-7)-10(-5) M), a new piperazinyl antihypertensive agent, like prazosin (10(-8)-10(-6) M), a potent preferential alpha 1-adrenoceptor antagonist, inhibited the contractile response of rabbit aorta to norepinephrine and methoxamine in a competitive manner whereas in the cat coronary and rabbit basilar artery, the inhibition by SGB was not a competitive one. The potency of the inhibitory action of SGB was less than that of prazosin in all preparations used. Neither SGB nor prazosin had any inhibitory effect on the response to potassium, 5-hydroxytryptamine, prostaglandin F2 alpha, and excess Ca2+ in all preparations. In the rabbit aortic membrane preparation, the specific binding of [3H]-prazosin was inhibited, concentration-dependently, by SGB with IC50 value of 1.4 +/- 0.09 microM. These studies indicated that SGB has an alpha 1-adrenoceptor-blocking action though its potency is weaker than prazosin.

Adrenergic alpha-Antagonists↗