Kuramoto S, Oda M, Terazawa K, Terabayashi M, Otani K, Shimamura K, Ouchida A
Research Laboratories, Torii & Co., Ltd., Chiba, Japan.
J Toxicol Sci. 1992 Dec;17 Suppl 4:287-301. doi: 10.2131/jts.17.supplementiv_287.
Antigenicity study of 6-amidino-2-naphthyl 4(-)[(4,5-dihydro-1H-imidazol-2-yl)amino] benzoate dimethanesulfonate (FUT-187), a new protease inhibitor, was investigated in guinea pigs and mice and the following results were obtained. 1. In guinea pigs immunized with FUT-187 plus adjuvant by intramuscular/subcutaneous routes, ASA, ACA and PCA reactions challenged intravenously or intradermally were positive. 2. In guinea pigs immunized with FUT-187 plus adjuvant by intramuscular/subcutaneous routes, ASA and PCA reactions challenged orally were negative. 3. In guinea pigs immunized with FUT-187 by the oral route, ASA, ACA and PCA reactions were negative. 4. In guinea pigs immunized with IABA and AN plus adjuvant by intramuscular/subcutaneous routes, ASA and PCA reactions were negative. 5. 48-hr PCA reactions were elicited with sera obtained from BALB/c and C3H/He mice immunized with FUT-187 plus adjuvant by the intraperitoneal route, responses were negative. 6. From the results of hapten inhibition tests using anti-FUT-187 guinea pig serum, it is suggested that the antigenicity of FUT-187 is attributable to the its benzoic acid.
对新型蛋白酶抑制剂6-脒基-2-萘基4-[(4,5-二氢-1H-咪唑-2-基)氨基]苯甲酸二甲磺酸盐（FUT-187）进行了豚鼠和小鼠抗原性研究，获得以下结果。1. 用FUT-187加佐剂经肌肉/皮下途径免疫的豚鼠，静脉内或皮内激发的ASA、ACA和PCA反应呈阳性。2. 用FUT-187加佐剂经肌肉/皮下途径免疫的豚鼠，口服激发的ASA和PCA反应呈阴性。3. 经口服途径用FUT-187免疫的豚鼠，ASA、ACA和PCA反应呈阴性。4. 用IABA和AN加佐剂经肌肉/皮下途径免疫的豚鼠，ASA和PCA反应呈阴性。5. 用FUT-187加佐剂经腹腔途径免疫的BALB/c和C3H/He小鼠的血清引发48小时PCA反应，结果为阴性。6. 根据使用抗FUT-187豚鼠血清进行的半抗原抑制试验结果，提示FUT-187的抗原性归因于其苯甲酸。
