Przegaliński E, Rawłów A
J Neural Transm. 1982;55(1):9-17. doi: 10.1007/BF01243337.
We studied the action of the following phosphodiesterase inhibitors (PDEIs): rolipram (4-[3-cyclopentoxy-5-methoxyphenyl]-2-pyrrolidione), Ro 20-1724 (4-[3-butoxy-4-methoxybenzyl]-2-imidazolidione), 1-methyl-3-isobutylxanthine (IMBX) and theophylline on flexor reflex activity of the hind limb in the spinal rat. Potentiation of this reflex is thought to be due to enhancement of either 5-hydroxytryptaminergic or alpha-adrenergic transmission in the spinal cord. All the inhibitors potentiated flexor reflex activity in a dose-dependent manner in the following order of potency: rolipram greater than Ro 20-1724 greater than IBMX greater than theophylline. Their stimulatory action in this model paralleled their known potency in inhibiting phosphodiesterase (PDE). Neither the 5-hydroxytryptamine (5-HT) antagonist cyproheptadine nor the alpha-adrenoceptor blocker phenoxybenzamine prevented potentiation of flexor reflex activity by PDEIs. It is suggested that (1) the PDEIs potentiate flexor reflex activity through a novel spinal mechanism which does not involve alpha-adrenoceptors of 5-HT receptors in the spinal cord but rather is related to the inhibition of PDE localized postsynaptically; (2) flexor reflex activity in the spinal rat can be a useful experimental preparation to estimate the in vivo effects of known PDEIs.
我们研究了以下磷酸二酯酶抑制剂（PDEIs）：咯利普兰（4-[3-环戊氧基-5-甲氧基苯基]-2-吡咯烷酮）、Ro 20-1724（4-[3-丁氧基-4-甲氧基苄基]-2-咪唑烷二酮）、1-甲基-3-异丁基黄嘌呤（IMBX）和茶碱对脊髓损伤大鼠后肢屈肌反射活动的作用。这种反射的增强被认为是由于脊髓中5-羟色胺能或α-肾上腺素能传递的增强。所有抑制剂均以剂量依赖性方式增强屈肌反射活动，其效力顺序如下：咯利普兰＞Ro 20-1724＞IMBX＞茶碱。它们在该模型中的刺激作用与其已知的抑制磷酸二酯酶（PDE）的效力平行。5-羟色胺（5-HT）拮抗剂赛庚啶和α-肾上腺素能受体阻滞剂酚苄明均不能阻止PDEIs对屈肌反射活动的增强作用。提示：（1）PDEIs通过一种新的脊髓机制增强屈肌反射活动，该机制不涉及脊髓中的α-肾上腺素能受体或5-HT受体，而是与突触后局部PDE的抑制有关；（2）脊髓损伤大鼠的屈肌反射活动可能是评估已知PDEIs体内效应的有用实验制剂。
