Tirilazad

Molecular formula C38H52N6O2 Molecular weight 624.86 CAS Registry No 110101-66-1 Merck Index 13, 9540 

Sample preparation Condition a 1 mL 100 mg Bond Elut CIS SPE cartridge with 2 mTi MeOH and 2 mL water. Vortex 500 iL plasma with 500 iL 5 rg/mL IS in MeCN for 1 min, centrifuge at 1500 g at 4°, add 800 iL of the supernatant to the SPE cartridge, wash with two 1 ml. portions of MeCNiwater 50 50, elute with two 1 mL portions of MeOH. Evaporate the eluate to dryness under a stream of nitrogen at 40, reconstitute the residue with 350 iL MeCN, vortex for 1 min, dilute with 150 aL water, inject an aliquot. 

Mobile phase MeCNibuffer 75 25 (The buffer was 22 mM triethylamine adjusted to pH 5.0 with glacial acetic acid.) 

Internal standard 21-[4-(2,6-di-l-pyrrolidinyl-4-pyrimidinyl)-l-piperazinyl]-3a-hy-droxy-16a-methyl-5a-pregna-20-one (16) 

Pullen, R.H. High-performance liquid chromatographic determination of a 21-aminosteroid antioxidant in plasma, J.Chromatogr., 1988, 424, 293-302. 

---

ChH, N20 1659-31-0) see Paclitaxel l-(2 (i-dipyrrolidino-4-pyrimidinyl)pipera7jne (C f,H2(iN(5 111641-17-9) see Tirilazad mesilate S)-l, 4-dithia-7-azaspiro[4.4)nonane-S carboxylic acid hydrobromide... 

QH11IO2 53064-79-2) see Cefditoien pivoxil 21-iodo-16a-methylpregna-l,4,9(ll)-triene-3,20-dione (C22H27IO2 111668-07-6) see Tirilazad mesilate... 

CH4O3S 75-75-2) see Alatrofloxacin mesilate Alendronate sodium Dolasetron mesilate Glaziovine Nelfinavir mesylate Tirilazad mesilate Trovafloxacin mesilate... 

C4HCI3N2 3764-01-0) see Minoxidil Tirilazad mesilate l-tricyclo[3.3.1.1 ]dec-l-ylethanone oxime... 

The RANTTAS Investigators. A randomized trial of tirilazad mesylate in patients with acute stroke (RANTTAS). Stroke 1996 27 447-453. 

Sato, P.H. and Hall, E.D. (1992). Tirilazad mesylate protects vitamins C and E in brain ischemia-reperfasion injury. J. Neurochem. 58, 2263-2268. 

Many amino- and hydroxy-substituted heterocycles have reasonably low oxidation potentials and, as such, can act as lipid-peroxidation inhibitors. We have already discussed triaminopyrimidine examples (tirilazad and U78517) and several ascorbic-acid analogues. This section discusses a few more examples. 

Kassell, N.F., Haley, E.C., Halves, W.M., Hunsen, C.A. and Weir, B. (1993). Phase two trial of tirilazad in aneurysmal subarachnoid hemorrhage. Vth International Symposium on Cerebral Vasospasm, Edmonton and Jasper, Alberta, Canada, May 18-21. Can. J. Neurol. Sci. 20, S29. 

Table 3. Hospital costs of tirilazad mesylate for subarachnoid hemorrhage in men...

Ghck H, Wihke R, Polsky D, Liana T, Alves WM, Kasseh N, Schulman KA. Economic analysis of tirilazad mesylate for aneurysmal subarachnoid hemorrhage economic evaluation of a phase IB clinical trial in Eu-... 

Fig. 9.6 Chemical structures of antioxidants in phase III clinical trials. Tirilazad mesylate (a) ...

Haley E. C., Jr. (1998). High-dose tirilazad for acute stroke (RANTTAS II). RANTTAS II Investigators. Stroke 29 1256-1257. 

The STIPAS Investigators (1994). Safety study of tirilazad mesylate in patients with acute ischemic stroke (STIPAS). Stroke 25 418 423. 

Free radical scavengers, antioxidants - ebselen, tirilazad... 

Fleishaker JC, Pearson PG, Wienkers LC, et al. Biotransformation of tirilazad in humans 2. Effect of ketoconazole on tirilazad clearance and oral bioavailability. J Pharmacol Exp Ther 1996 277 991-998. 

Fleishaker JC, Pearson LK, Peters GR. Induction of tirilazad clearance by phenytoin. Biopharm Drug Dispos 1998 19 91 96. 

C6II I()2 53064-79-2) see Cefditoren pivoxil 21 -iodo-16(x-methy Ipregna-1,4,9( 11 )-trienc-3,20-dionc (C22H27I02 111668-07-6) sec Tirilazad mesilate... 

---