Pawłowski L, Sidorowicz L
Pol J Pharmacol Pharm. 1978 Sep-Oct;30(5):665-73.
The effect of atropine on the spiperone- or reserpine-induced catalepsy was compared with the effect pure antihistamines (chlorcyclizine, diphenhydramine, mepyramine) and antiserotonin -- antihistamine drugs (cyproheptadine, danitracen). All the drugs were used in equipotent doses in respect of their central cholinolytic action, assassed previously on the basis of the tremorine test. The potency of the antiserotonin action of chlorcyclizine, diphenhydramine and mepyramine was estimated by assessing the ID50 values of these compounds in the test based on antagonism to L-5-hydroxytryptophan action in the mouse. The spiperone-induced catelepsy, was most effectively inhibited by classical histaminolytics and less by drugs of a combined antiserotonin and antihistamine action. For the reserpine-induced catalepsy, differences in action of the two groups of drugs were less distinct. In both cases atropine produced the weakest anticataleptic effect. Amodiaquine, an inhibitor of histamine degradation, enhanced the catalepsy induced by either neuroleptic (the reserpine-induced catalepsy in a statistically significant menner). A possibility that the anticataleptic action of chlorcyclizine, cyproheptadine, diphenhydramine, mepyrymine and danitracen depends on the blockade of the histamine receptors in the brain is discussed.
将阿托品对舒必利或利血平诱导的僵住症的作用,与纯抗组胺药(氯环嗪、苯海拉明、美吡拉敏)以及抗血清素 - 抗组胺药(赛庚啶、达尼曲生)的作用进行了比较。所有药物均以等效力剂量使用,其依据先前通过震颤素试验测定的中枢抗胆碱作用。通过评估这些化合物在基于对小鼠体内L - 5 - 羟色氨酸作用的拮抗作用试验中的ID50值,来估计氯环嗪、苯海拉明和美吡拉敏的抗血清素作用效力。舒必利诱导的僵住症,最有效地被经典抗组胺药抑制,而具有抗血清素和抗组胺联合作用的药物抑制作用较弱。对于利血平诱导的僵住症,两组药物的作用差异不太明显。在这两种情况下,阿托品产生的抗僵住症作用最弱。阿莫地喹,一种组胺降解抑制剂,增强了由任何一种抗精神病药物诱导的僵住症(利血平诱导的僵住症具有统计学意义)。讨论了氯环嗪、赛庚啶、苯海拉明、美吡拉明和达尼曲生的抗僵住症作用可能取决于对脑内组胺受体的阻断。