Disease relevance of TETRAISOPROPYLPYROPHOSPHAMIDE

• Daily pretreatment with the CarbE inhibitors CBDP (2-[o-cresyl]-4H-1,2,3-benzodioxa- phosphorin-2-oxide) (7.22 micromol/kg, s.c.) or iso-OMPA (tetraisopropylpyrophosphoramide) (8.76 micromol/kg, i.p.), followed by paraoxon (0.33 micromol/kg, s.c.) 30 min later, prevented the development of tolerance to paraoxon and potentiated its toxicity [1].

High impact information on TETRAISOPROPYLPYROPHOSPHAMIDE

• Staining was blocked by diisopropyl-fluorophosphate, which inhibits both pseudocholinesterase and acetylcholinesterase, but was not blocked by tetraisopropylpyrophosphoramide, a specific pseudocholinesterase inhibitor [2].
• Administration of tetraisopropylpyrophosphoramide a specific pseudocholinesterase inhibitor, inhibited serum and adipose tissue pseudocholinesterase activity by greater than 80% and liver greater than 50% [3].
• In vitro, bath-applied bambuterol (1-100 microm) and tetraisopropylpyrophosphoramide (10-100 microm) decreased BChE activity in the brainstem but did not perturb central respiratory activity recorded from spinal nerve rootlets [4].
• Addition of 1 microM tetraisopropylpyrophosphoramide (iso-OMPA) led to a 98% inhibition of BuChE activity with little or no effect on AChE activity [5].
• True AChE activity (measured in the presence of a maximally effective concentration of tetraisopropylpyrophosphoramide) had a Vmax of 13.4 +/- 0.17 nmoles X min-1 X mg protein)-1 and an apparent Km value of 1 X 10(-4)M acetylthiocholine [6].

Biological context of TETRAISOPROPYLPYROPHOSPHAMIDE

• 4. Both hydrolysis steps by erythrocyte AChE were totally blocked by the selective AChE inhibitor BW284c51 but were not blocked by the BuChE-specific inhibitor, iso-OMPA (tetraisopropylpyrophosphoramide) [7].

Associations of TETRAISOPROPYLPYROPHOSPHAMIDE with other chemical compounds

• Triton X-100 partially protected BuChE against this tetraisopropylpyrophosphoramide inactivation [8].
• Neostigmine, a non-selective ChE inhibitor, caused concentration-dependent contractions in rat urinary bladder strips, whereas tetraisopropylpyrophosphoramide (iso-OMPA; a BuChE inhibitor) failed to affect the resting tone of the preparations [9].

References