MAFFII G, SONCIN E
Br J Pharmacol Chemother. 1958 Dec;13(4):357-63. doi: 10.1111/j.1476-5381.1958.tb00221.x.
The pharmacological actions of 5-phenyl-1:3:4-thiadiazole (L 1538), 2-amino-5-phenyl-1:3:4-thiadiazole (L 1460) and 2-amino-5-(2'-thienyl)-1:3:4-thiadiazole (L 1458) have been studied and compared with those of other muscular relaxant drugs. The three compounds have paralysing effects in mice, rats, cats, and dogs. They block the tonic component of maximal electroshock seizures and protect against strychnine, though not against leptazol-induced convulsions in mice. Like other centrally acting paralysing drugs, they depress spinal polysynaptic transmission in doses which leave monosynaptic transmission relatively unaffected. The rigidity of the decerebrate cat is reduced but not always abolished. The compounds do not induce synchronization in epidural electroencephalogram recordings. In doses not greatly affecting muscular tone and spontaneous activity, they prolong the hypnotic effects of pentobarbitone and other barbiturates in mice. Autonomic functions are only slightly affected. The similar actions of substituted thiadiazoles and 2-amino-benzothiazoles confirm a previous hypothesis that pharmacological equivalence may result either from condensing heterocyclic nuclei with aromatic nuclei or from introducing aryl substituents into them.
已对5-苯基-1:3:4-噻二唑（L 1538）、2-氨基-5-苯基-1:3:4-噻二唑（L 1460）和2-氨基-5-（2'-噻吩基）-1:3:4-噻二唑（L 1458）的药理作用进行了研究，并与其他肌肉松弛药物的药理作用进行了比较。这三种化合物对小鼠、大鼠、猫和狗均有麻痹作用。它们能阻断最大电休克惊厥的强直成分，对士的宁有保护作用，但对小鼠戊四氮诱发的惊厥无保护作用。与其他中枢性麻痹药物一样，它们在剂量上能抑制脊髓多突触传递，而使单突触传递相对不受影响。去大脑猫的强直状态有所减轻，但并非总是消除。这些化合物不会在硬膜外脑电图记录中诱发同步化。在剂量对肌肉张力和自发活动影响不大的情况下，它们能延长戊巴比妥和其他巴比妥类药物对小鼠的催眠作用。自主功能仅受到轻微影响。取代噻二唑和2-氨基苯并噻唑的类似作用证实了先前的一个假设，即药理等效性可能源于杂环核与芳核的缩合，或者源于向其中引入芳基取代基。
