S. Ross, A. L. Renyi
Jan 31, 1977
Citations
1
Influential Citations
174
Citations
Quality indicators
Journal
Neuropharmacology
Abstract
(Z)-3-(4-Bromophenyl)-N,N-dimethyl-3-(3-pyridyl)allylamine (H ) and the secondary amine analogue (A 24356) were about 10 times more potent in inhibiting the uptake of [14C]-hydroxytryptamine than the uptake of [3H]-(−)noradrenaline in homogenate and slices of the rat hypothalamus in vitro, whereas the corresponding tertiary (E)-isomer (A 23140) had the same activity on both uptake mechanisms and the secondary (E)-derivative (A 23889) was much more potent in inhibiting the noradrenaline uptake. All four amines had rather low activity on the dopamine uptake in homogenate of rat striatum. After oral administration in vivo, H and A 24356 were about equally potent in inhibiting the 5-hydroxytryptamine uptake in slices of rat hypothalamus and were much less active on the noradrenaline uptake. On the other hand, A 23889 and A 23140 were very active inhibitors of the noradrenaline uptake but poor inhibitors of the 5-hydroxytryptamine uptake after administration in vivo. It was found that H was rapidly transformed to A 24356 in vivo and that the main effect in vivo was caused by the secondary amine derivative.