Kleinrok Z, Kolasa K, Mastalerz P, Kafarski P
Pol J Pharmacol Pharm. 1986 Sep-Dec;38(5-6):435-42.
Ten newly synthesized derivatives of phosphonoamino acids were subjected to preliminary pharmacological evaluation in mice and rats. We investigated their effect on acute toxicity, body temperature, spontaneous and exploratory activity, electrogenic and pentetrazole convulsions, and motor coordination and gamma-amino-butyric acid concentration in various brain regions. The most active derivatives were alpha-amino-alpha-p-hydroxyphenyl-methylphosphonic acid 40, beta-(alpha-aminoethyl)-carbamoyl-ethylphosphonic acid 43, alpha-amino-beta-phenylethylphosphonic acid 46, and alpha-amino-beta-(p-nitrophenyl)-ethylphosphonic acid 47. Those compounds depressed the spontaneous locomotor activity and displayed protective action in electrogenic and pentetrazole convulsions.
十种新合成的膦酰基氨基酸衍生物在小鼠和大鼠身上进行了初步药理学评估。我们研究了它们对急性毒性、体温、自发和探索活动、电惊厥和戊四氮惊厥以及不同脑区运动协调性和γ-氨基丁酸浓度的影响。活性最高的衍生物是α-氨基-α-对羟基苯基甲基膦酸40、β-(α-氨基乙基)-氨基甲酰基乙基膦酸43、α-氨基-β-苯乙基膦酸46和α-氨基-β-(对硝基苯基)乙基膦酸47。这些化合物抑制自发运动活性，并在电惊厥和戊四氮惊厥中表现出保护作用。
