溴法罗明对大鼠脑单胺氧化酶-A和单胺氧化酶-B的区域作用。

Regional action of brofaromine on rat brain MAO-A and MAO-B.

Gerardy J, Dresse A

Department of Pharmacology, University of Liège, Sart-Tilman, Belgium.

Prog Neuropsychopharmacol Biol Psychiatry. 1998 Oct;22(7):1141-55. doi: 10.1016/s0278-5846(98)00067-0.

Abstract

Brofaromine (CGP 11,305 A) belongs to a new generation of monoamine oxidase (MAO) inhibitors. These compounds induce short, reversible and selective inhibition of brain MAO of type A. 2. The aim of this work is to study monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B) activities of several rat brain regions after increasing doses of brofaromine. 3. Brofaromine inhibits MAO-A activities in a dose dependent manner in all brain regions examined. 4. The largest reduction was found in hippocampal formation, striatum and prefrontal cortex respectively. ID50 is 2 times lower in hippocampus than in remaining brain. 5. Brofaromine does not inhibit MAO-B activities in the different regions examined. 6. Brofaromine is a very selective inhibitor of rat brain MAO-A with a preferential action on telencephalic monoaminergic nerve terminals.

摘要

溴法罗明（CGP 11,305 A）属于新一代单胺氧化酶（MAO）抑制剂。这些化合物可引起对A型脑MAO的短暂、可逆且选择性抑制。2. 本研究的目的是在递增剂量的溴法罗明作用后，研究大鼠几个脑区的单胺氧化酶A（MAO - A）和单胺氧化酶B（MAO - B）活性。3. 溴法罗明在所检测的所有脑区中均以剂量依赖性方式抑制MAO - A活性。4. 分别在海马结构、纹状体和前额叶皮质中发现最大程度的降低。海马中的半数抑制剂量（ID₅₀）比其余脑区低2倍。5. 溴法罗明在所检测的不同脑区中不抑制MAO - B活性。6. 溴法罗明是大鼠脑MAO - A的一种非常有选择性的抑制剂，对端脑单胺能神经末梢有优先作用。