Audi E A, de-Oliveira C E, Graeff F G
Departamento de Farmácia e Farmacologia, Fundação Universidade Estadual de Maringá, PR, Brasil.
Braz J Med Biol Res. 1989;22(6):699-701.
The effect of intracerebrally injected propranolol was measured in the elevated plus-maze, an animal model of anxiety. Microinjection of 10 nmol of propranolol into the dorsal midbrain central gray of the rat increased the percentage of open arm entries, without affecting the total number of arm entries. This selective anxiolytic effect of propranolol was antagonized by 10 nmol of ritanserin, also injected into the dorsal midbrain. The same dose of ritanserin, given alone, did not affect the percentage of open arm entries, though it tended to decrease the total number of entries, an indication of unspecific behavioral depression. Since propranolol is a stereospecific antagonist of presynaptic serotonin (5-HT) autoreceptors and ritanserin is a selective blocker of type 2 5-HT receptors, the present results suggest that the anxiolytic action of propranolol in the midbrain central gray is due to release of endogenous 5-HT acting upon 5-HT2 receptors.
在高架十字迷宫(一种焦虑动物模型)中测量了脑内注射普萘洛尔的效果。向大鼠背侧中脑中央灰质微量注射10纳摩尔普萘洛尔可增加进入开放臂的百分比,而不影响进入臂的总数。普萘洛尔的这种选择性抗焦虑作用被同样注射到背侧中脑的10纳摩尔利坦色林所拮抗。单独给予相同剂量的利坦色林并不影响进入开放臂的百分比,尽管它倾向于减少进入总数,这表明存在非特异性行为抑制。由于普萘洛尔是突触前5-羟色胺(5-HT)自身受体的立体特异性拮抗剂,而利坦色林是2型5-HT受体的选择性阻滞剂,目前的结果表明普萘洛尔在中脑中央灰质的抗焦虑作用是由于内源性5-HT释放作用于5-HT2受体所致。