Berenbaum M C
Clin Exp Immunol. 1971 Jan;8(1):1-8.
The toxicities and immunosuppressive potencies of single doses of 6-mercaptopurine and azathioprine have been compared in mice, using the 30-day mortality as a measure of toxicity, and reduction in spleen plaque-forming cells in response to sheep erythrocytes as a measure of immunosuppression. When compared on the basis of equivalent toxicity, 6-mercaptopurine was consistently the more effective agent by the intraperitoneal route. By the subcutaneous route, 6-mercaptopurine was more effective at doses above the LD-30; at lower doses, azathioprine was marginally better, but the difference was probably not significant. For the same cost in toxicity, azathioprine was six to seven times more effective as an immunosuppressive by the subcutaneous as by the intraperitoneal route.
已在小鼠中比较了单剂量6-巯基嘌呤和硫唑嘌呤的毒性及免疫抑制效力,采用30天死亡率作为毒性指标,以对绵羊红细胞反应时脾空斑形成细胞的减少作为免疫抑制指标。在等效毒性的基础上进行比较时,腹腔注射途径下6-巯基嘌呤始终是更有效的药物。皮下注射途径下,6-巯基嘌呤在高于LD-30的剂量时更有效;在较低剂量时,硫唑嘌呤略好一些,但差异可能不显著。在毒性相同的情况下,皮下注射途径时硫唑嘌呤作为免疫抑制剂的效力是腹腔注射途径的6至7倍。