title: Intravenously injected FK506 failed to inhibit hippocampal calcineurin.
abstract: FK506 (tacrolimus) is known as an inhibitor for calcineurin and is used in numerous research fields. It is not clear whether intravenously injected FK506 inhibits neuronal calcineurin. We measured the calcineurin activities of normal and postischemic rat hippocampi after intravenous injection of FK506 (3 mg/kg). Intravenously injected FK506 had no inhibitory effect on calcineurin activity in the hippocampi of normal and postischemic rats, whereas FK506 inhibited the calcineurin in vitro (purified enzyme, hippocampal homogenate, and hippocampal slice culture homogenate). Thus, it is considered that intravenously injected FK506 does not act on intraneuronal calcineurin and that several effects of FK506 are not due to the inhibition of neuronal calcineurin.
authors.affiliation: Department of Neurosurgery, Kumamoto University School of Medicine, Kumamoto, Japan. morioka@kaiju.medic.kumamoto-u.ac.jp
authors.forename: M
authors.initials: M
authors.lastname: Morioka
authors.forename: K
authors.initials: K
authors.lastname: Fukunaga
authors.forename: Y
authors.initials: Y
authors.lastname: Kai
authors.forename: T
authors.initials: T
authors.lastname: Todaka
authors.forename: S
authors.initials: S
authors.lastname: Yano
authors.forename: J
authors.initials: J
authors.lastname: Hamada
authors.forename: E
authors.initials: E
authors.lastname: Miyamoto
authors.forename: Y
authors.initials: Y
authors.lastname: Ushio
mesh_terms: D000818:Animals; D002545:Brain Ischemia / Q000378:metabolism; D065095:Calcineurin Inhibitors; D046508:Culture Techniques; D006624:Hippocampus / Q000187:drug effects / Q000378:metabolism*; D007275:Injections, Intravenous; D007700:Kinetics; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D016559:Tacrolimus / Q000008:administration & dosage / Q000494:pharmacology*; D014020:Tissue Extracts / Q000032:analysis
chemical_list: D065095:Calcineurin Inhibitors; D014020:Tissue Extracts; D016559:Tacrolimus