The effect of different calcium channel blockers was studied on basal and cocaine-inhibited [3H]dopamine uptake in rat striatal synaptosomes. Isradipine (dihydropyridine calcium antagonist) and diltiazem (L-type calaium antagonist) were devoid of effect on [3H]dopamine uptake, while flunarizine (T-type calcium antagonist) inhibited [3H]dopamine uptake. Flunarizine inhibition was competitive and the inhibitory curve was biphasic with a Hill coefficient of 2.1. The high Hill number suggested a mechanism of positive cooperativity between two sites. Flunarizine inhibition showed a complex interaction with cocaine inhibition. While flunarizine at low concentrations interacts with a distinct site, at higher concentrations it interacts with the same site as cocaine. The relevance of this finding for the potentiation by flunarizine of cocaine-induced dopamine release in vivo is discussed. © 1991.

Inhibition of [3H]dopamine uptake by flunarizine / Devoto, P.; Pani, L.; Kuzmin, A.; Montis, G. D.. - In: EUROPEAN JOURNAL OF PHARMACOLOGY. - ISSN 0014-2999. - 203:1(1991), pp. 67-69. [10.1016/0014-2999(91)90791-N]

Inhibition of [3H]dopamine uptake by flunarizine

Pani L.;
1991

Abstract

The effect of different calcium channel blockers was studied on basal and cocaine-inhibited [3H]dopamine uptake in rat striatal synaptosomes. Isradipine (dihydropyridine calcium antagonist) and diltiazem (L-type calaium antagonist) were devoid of effect on [3H]dopamine uptake, while flunarizine (T-type calcium antagonist) inhibited [3H]dopamine uptake. Flunarizine inhibition was competitive and the inhibitory curve was biphasic with a Hill coefficient of 2.1. The high Hill number suggested a mechanism of positive cooperativity between two sites. Flunarizine inhibition showed a complex interaction with cocaine inhibition. While flunarizine at low concentrations interacts with a distinct site, at higher concentrations it interacts with the same site as cocaine. The relevance of this finding for the potentiation by flunarizine of cocaine-induced dopamine release in vivo is discussed. © 1991.
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Inhibition of [3H]dopamine uptake by flunarizine / Devoto, P.; Pani, L.; Kuzmin, A.; Montis, G. D.. - In: EUROPEAN JOURNAL OF PHARMACOLOGY. - ISSN 0014-2999. - 203:1(1991), pp. 67-69. [10.1016/0014-2999(91)90791-N]
Devoto, P.; Pani, L.; Kuzmin, A.; Montis, G. D.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11380/1211948
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