Effects of d- and l-pentazocine on the release and uptake of norepinephrine in rat brain cortex.
Effects of d- and l-pentazocine on the release and uptake of norepinephrine and other neurotransmitters were examined in rat cerebral cortex. D- and l-pentazocine (10(-6)-10(-4) M) evoked the release of tritium from rat cortex slices preloaded with [3H]norepinephrine. Both isomers of pentazocine (3 x 10(-5) M) also evoked the release of tritium from slices preloaded with [3H]dopamine and [3H]5-hydroxytryptamine ([3H]5-HT) but did not from those preloaded with [3H] gamma-aminobutyric acid ([3H]GABA) and [3H]choline. The releasing effect of pentazocine was neither dependent on the extracellular calcium nor antagonized by naloxone. Both isomers inhibited the uptake of [3H]norepinephrine, [3H]dopamine and [3H]5-HT but not that of [3H]GABA and [3H]choline into synaptosomes prepared from the cortex. These results suggest that the effects of d- and l-pentazocine on release and uptake are relatively specific to monoamines and might explain some aspects of pharmacological actions of pentazocine.
Kinouchi
K
K
Department of Anesthesiology, Osaka University Medical School, Japan.
Maeda
S
S
Saito
K
K
Inoki
R
R
Fukumitsu
K
K
Yoshiya
I
I
D000818:Animals; D001679:Biogenic Amines / Q000378:metabolism; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D066298:In Vitro Techniques; D008297:Male; D018377:Neurotransmitter Agents / Q000378:metabolism; D009638:Norepinephrine / Q000378:metabolism*; D010423:Pentazocine / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism
D001679:Biogenic Amines; D018377:Neurotransmitter Agents; D010423:Pentazocine; D009638:Norepinephrine