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Literature DB >> 8491246

The effects of the COMT inhibitor nitecapone for one week on exercise haemodynamics and catecholamine disposition.

S Sundberg¹, M Scheinin, P Ojala-Karlsson, J Akkila, A Gordin.

Abstract

We have studied resting and exercise haemodynamics and catecholamine disposition after catechol-O-methyl-transferase (COMT) inhibition with nitecapone 100 mg t.d.s. for 7 days in 15 healthy men (aged 21 to 28 y) in a placebo-controlled, cross-over study. Nitecapone did not alter resting or exercise heart rates, blood pressure, or plasma catecholamine concentrations, but it altered the metabolic profile of endogenous catecholamines, as shown by: (1) a fall in the concentrations of the COMT-dependent metabolite 3-methoxy-4-hydroxy-phenylglycol (MHPG) by 22% (P < 0.01), (2) increases in plasma concentrations of the monoamine oxidase-dependent metabolites 3,4-dihydroxyphenylglycol (DHPG) by up to 90% (P < 0.001) and 3,4-dihydroxyphenylacetic acid (DOPAC) by 67% (P < 0.05), (3) a three-fold increase in the concentration of circulating conjugated adrenaline (P < 0.001).

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Year: 1993 PMID： 8491246 DOI： 10.1007/BF00271374

Source DB: PubMed Journal: Eur J Clin Pharmacol ISSN： 0031-6970 Impact factor: 2.953

16 in total

1. Hypokalaemia and other non-bronchial effects of inhaled fenoterol and salbutamol: a placebo-controlled dose-response study in healthy volunteers.

Authors: M Scheinin; M Koulu; E Laurikainen; H Allonen
Journal: Br J Clin Pharmacol Date: 1987-11 Impact factor: 4.335

2. Plasma 3,4-dihydroxyphenylglycol (DHPG) and 3-methoxy-4-hydroxyphenylglycol (MHPG) are insensitive indicators of alpha 2-adrenoceptor mediated regulation of norepinephrine release in healthy human volunteers.

Authors: M Scheinin; S Karhuvaara; P Ojala-Karlsson; A Kallio; M Koulu
Journal: Life Sci Date: 1991 Impact factor: 5.037

The effects of the COMT inhibitor nitecapone for one week on exercise haemodynamics and catecholamine disposition.

1. Hypokalaemia and other non-bronchial effects of inhaled fenoterol and salbutamol: a placebo-controlled dose-response study in healthy volunteers.

2. Plasma 3,4-dihydroxyphenylglycol (DHPG) and 3-methoxy-4-hydroxyphenylglycol (MHPG) are insensitive indicators of alpha 2-adrenoceptor mediated regulation of norepinephrine release in healthy human volunteers.

3. Favorable effect of catechol-O-methyltransferase inhibition by OR-462 in experimental models of Parkinson's disease.

4. The use of non-parametric methods in the statistical analysis of the two-period change-over design.

Review 5. Catecholamine metabolism: basic aspects and clinical significance.

6. Persistence of arrhythmia exercise response in healthy young men.

7. Exercise hemodynamics and catecholamine metabolism after catechol-O-methyltransferase inhibition with nitecapone.

8. COMT inhibition with nitecapone does not affect the tyramine pressor response.

9. Inhibition of human erythrocyte and gastroduodenal catechol-O-methyltransferase activity by nitecapone.

10. Inhibition of catechol-O-methyltransferase activity by two novel disubstituted catechols in the rat.

1. Clinical Potential of Catechol-OMethyltransferase (COMT) Inhibitors as Adjuvants in Parkinson's Disease.