| Title : Tritium labeling of a powerful methylphosphonate inhibitor of cholinesterase: synthesis and biological applications - Balan_1988_Anal.Biochem_169_95 |
| Author(s) : Balan A , Barness I , Simon G , Levy D , Ashani Y |
| Ref : Analytical Biochemistry , 169 :95 , 1988 |
|
Abstract :
7-(Methylethoxy phosphinyloxy)-1-methyl-quinolinium iodide (MEPQ), a powerful anti-cholinesterase methylphosphonate ester, was labeled with tritium (9 Ci/mmol) at the methylphosphonyl moiety (TCH2P(O)(OR)X) by an iodine-tritium replacement reaction. Kinetic measurements of the rate of inhibition of acetylcholinesterase (AChE) by [3H]MEPQ and its rate of hydrolysis in alkaline solution confirmed the identity of [3H]MEPQ with authentic MEPQ, which was prepared by the same reaction sequences. Gel-filtration experiments verified the radiospecificity of [3H]MEPQ. In vitro radiolabeling of both AChE and butyrylcholinesterase along with the whole-body autoradiography of [3H]MEPQ-treated mice suggests that [3H]MEPQ is a convenient marker for studying biological systems containing these esterases. |
| PubMedSearch : Balan_1988_Anal.Biochem_169_95 |
| PubMedID: 88220750 |
| Inhibitor | MEPQ |
Balan A, Barness I, Simon G, Levy D, Ashani Y (1988)
Tritium labeling of a powerful methylphosphonate inhibitor of cholinesterase: synthesis and biological applications
Analytical Biochemistry
169 :95
Balan A, Barness I, Simon G, Levy D, Ashani Y (1988)
Analytical Biochemistry
169 :95