The cardiovascular and central nervous system effects in the human of U-62066E. A selective opioid receptor agonist.

Abstract:

:The cardiovascular and central nervous system effects of the kappa opioid receptor agonist U-62066E were investigated in ten normal male subjects who received U-62066E or placebo with low or high dose naloxone in a randomized, double blind study. Blood pressure and heart rate in the supine and standing position, plasma adrenaline and noradrenaline, regional Doppler blood velocity indices and psychometric assessments were recorded for 1.25 h before and 6 h following injection. U-62066E caused sedation and dysphoria but no euphoria. Plasma noradrenaline was increased by U62066E when compared with basal levels. This action of U62066E was prevented by high but not low dose naloxone. U-62066E had no significant effect on blood pressure, heart rate or regional blood flow indices in the vessels studied and no effect on plasma adrenaline levels. Since U62066E at a dose known to have marked kappa effects was not found to influence cardiovascular indices our results do not support a major role for kappa opioids in the control of the circulation. However, U62066E may influence noradrenaline release or clearance and cause sedation and psychotomimetic effects.

journal_name

Eur J Clin Pharmacol

authors

Rimoy GH,Wright DM,Bhaskar NK,Rubin PC

doi

10.1007/BF00192549

subject

Has Abstract

pub_date

1994-01-01 00:00:00

pages

203-7

issue

3

eissn

0031-6970

issn

1432-1041

journal_volume

46

pub_type

临床试验,杂志文章,随机对照试验
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