Munt P L, Bruzzese T, Algate D R
Department of Pharmacology, Huntingdon Research Centre, UK.
Arzneimittelforschung. 1995 Jul;45(7):805-9.
N-(N-L-Threonyl-L-alpha-aspartyl)-L-tyrosine (CAS 115053-54-8, SPA-S-646) was originally derived from lysozyme. It has previously been found to have analgesic properties following oral and intravenous administration to laboratory rodents. In the rhesus monkey, intramuscular administration of SPA-S-646 caused a dose-related analgesia. This effect was not seen following oral administration, but when given via the rectum, analgesia was again observed. In the dog, a single dose of 50 mg/kg was active by the intramuscular route but not the oral route. It is thought that unlike the rat, the digestive systems of the rhesus monkey and the dog degrade the tripeptide into inactive constituents.
N-(N-L-苏氨酰-L-α-天冬氨酰)-L-酪氨酸(CAS 115053-54-8,SPA-S-646)最初源自溶菌酶。先前已发现,给实验啮齿动物口服和静脉注射该物质后具有镇痛特性。在恒河猴中,肌肉注射SPA-S-646会产生剂量相关的镇痛效果。口服给药未观察到这种效果,但经直肠给药时,再次观察到了镇痛作用。在犬类中,单次剂量为50 mg/kg时,肌肉注射途径有活性,但口服途径无活性。据认为,与大鼠不同,恒河猴和犬类的消化系统会将三肽降解为无活性成分。