The effects of some slow channel blocking drugs on high affinity serotonin uptake by rat brain synaptosomes.

Article Details

Citation

Copy to clipboard

Brown NL, Sirugue O, Worcel M

The effects of some slow channel blocking drugs on high affinity serotonin uptake by rat brain synaptosomes.

Eur J Pharmacol. 1986 Apr 9;123(1):161-5.

PubMed ID

2940099 [ View in PubMed

]

Abstract

The effects of some slow channel blocking drugs were investigated on high affinity serotonin uptake into crude rat brain synaptosomes. Serotonin uptake was sodium-dependent and competitively inhibited by imipramine (IC50 0.6 microM, Ki 0.26 microM). Bepridil, verapamil and diltiazem produced an apparent competitive inhibition of serotonin uptake with respective IC50 of 4.8, 5.2 and 308 microM. Nitrendipine and the sodium channel blocker, lidocaine, were without effect, even at 100 microM. The mechanism of the inhibitory effect is unknown but may involve an allosteric interaction with the sodium-dependent transporter.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Verapamil	Sodium-dependent serotonin transporter	Protein	Humans	Unknown	Unknown	Details