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3-Methoxytyramine, an extraneuronal dopamine metabolite plays a physiological role in the brain as an inhibitory regulator of catecholaminergic activity.

Abstract：

:3-Methoxytyramine (3-MT), an extraneuronal metabolite of dopamine, present in the synaptic cleft at a very low amount (low nanomolar range), comparable to dopamine concentration, is generally regarded as a biologically inactive compound. We have shown in this study that 3-MT binds to the rat noradrenergic cortical alpha(1) and striatal dopamine D(1) and D(2) receptors in nanomolar concentration range, and to cortical alpha(2) adrenoceptor at low micromolar concentration. Bilateral intrastriatal injections of 3-MT (0.25 micromol in 0.5 microl) did not affect significantly locomotor activity in naive rats but strongly antagonized amphetamine-induced (1 mg/kg s.c.) hypermotility. Biochemical studies in rat brain structures showed that 3-MT behaved as an antagonist of the noradrenergic system, i.e. accelerated noradrenaline metabolism and counteracted the inhibitory effect of amphetamine on the rate of noradrenaline metabolism. In contrast to a general view about the lack of physiological role of monoamine metabolites, these results for the first time strongly suggest that an extraneuronal metabolite of dopamine, 3-MT plays an important physiological role as an inhibitory regulator counteracting excessive stimulation of catecholaminergic neurons in the striatum.

journal_name

Eur J Pharmacol

journal_title

European journal of pharmacology

authors

Antkiewicz-Michaluk L,Ossowska K,Romańska I,Michaluk J,Vetulani J

doi

10.1016/j.ejphar.2008.09.033

subject

Has Abstract

pub_date

2008-12-03 00:00:00

pages

32-5

issue

1-3

eissn

0014-2999

issn

1879-0712

pii

S0014-2999(08)00974-6

journal_volume

599

pub_type

杂志文章

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