Schaeffer J M, Bergstrom A R, Turner M J
Merck Sharp & Dohme Research Laboratories, Department of Biochemical Parasitology, Rahway, NJ 07065.
Biochem J. 1989 Jun 15;260(3):923-6. doi: 10.1042/bj2600923.
MK-801, an N-methyl-D-aspartate antagonist in mammalian brain tissue, is a potent nematocidal agent. Specific MK-801 binding sites have been identified and characterized in a membrane fraction prepared from the free-living nematode Caenorhabditis elegans. The high-affinity MK-801 binding site has an apparent dissociation constant, Kd, of 225 nM. Unlike the MK-801 binding site in mammalian tissues, the C. elegans binding site is not effected by glutamate or glycine, and polyamines are potent inhibitors of specific MK-801 binding.
MK-801是一种存在于哺乳动物脑组织中的N-甲基-D-天冬氨酸拮抗剂，是一种强效杀线虫剂。在从自由生活的线虫秀丽隐杆线虫制备的膜组分中已鉴定并表征了特异性MK-801结合位点。高亲和力MK-801结合位点的表观解离常数Kd为225 nM。与哺乳动物组织中的MK-801结合位点不同，秀丽隐杆线虫的结合位点不受谷氨酸或甘氨酸的影响，而多胺是特异性MK-801结合的有效抑制剂。
