Thalidomides

100-fold greater than that required in humans. However, hamsters, mice, and some species of rat are largely resistant. 

Recently, thalidomide has gained approval for use in the United States as an immunomodulatory agent in the treatment of HIV-associated diseases, arthritis, myeloma, and diabetic retinopathy. The FDA has instituted the System of Thalidomide Education and Prescribing Safety (STEPS) to prevent accidental exposures during pregnancy. 

10 Reproductive and Endocrine Toxicology, Elsevier Science, New York, 1997. 

Collins, T. F. History and evolution of reproductive and developmental toxicology guidelines. Curr. Pharm. Des. 12, 1449-1465, 2006. 

De Salvia, M. A., Petruzzi, S., and Alieva, E. Appropriate end points for the characterization of behavioral changes in developmental toxicology. Environ. Health Perspect. 104 (Suppl. 2), 307-315,1996. 

Molecular formula C13H10N2O4 Molecular weight 258.23 CAS Registry No 50-35-1 Merck Index 13,9326 

Sample preparation Condition a 1 mL 100 mg CIS SPE cartridge (Varian) with 1 column vol of MeOH and one column volume of water. Vortex 1 mL 25 mM pH 2.5 phosphate buffer with 1 mL plasma, add 100 p,L 100 rg/mL labetalol in MeOH, vortex, add to the SPE cartridge, wash with 2 column vol of water, dry under vacuum, elute with 1 mL anhydrous diethyl ether, evaporate the eluate to dryness under a stream of nitrogen, reconstitute the residue with 130 p,L mobile phase, inject a 50 p.L aliquot. 

Guard column Bioptic AV-1 (Meta Chem Technologies, Torrance CA) 

Mobile phase Isopropanol 100 mM pH 4 phosphate buffer 2 98 Flow rate 0.6 Injection volume 50 Detector UV 300 

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A much more serious drawback to using chiral drugs as racemic mixtures is illustrated by thalidomide briefly employed as a sedative and antinausea drug in Europe during the period 1959-1962 The desired properties are those of (/ ) thalidomide (S) Thalido mide however has a very different spectrum of bio logical activity and was shown to be responsible for over 2000 cases of serious birth defects in children born to women who took it while pregnant... 

Bromocresol green (3.8...5.4) aliphatic carboxylic acids[103,187 — 204] triiodobenzoic acid [205], derivatives of barbituric acid [206] amphetamine derivatives [207, 208] phenazones, morazone [209] alkaloids [91, 209] nephopam [210] phenyramidol metabolites [211] diethylalkylacetamide derivatives [212] zipeprol (Mirsol) [213] thalidomide and hydrolysis products [214] cyclohexylamine derivatives [215] herbicide residues [216]... 

Development of novel response modifiers derived from thalidomide (3-phthaIimidopyridine-2,6-dione) and other phthalimide derivatives 99 YGK94. 

The glutarimide best known to the lay public, thalidomide (40), owes its reputation not to efficacy, but to the wholly unanticipated and tragic teratogenic effects elicited by this compound. It might be noted that the very efficacy and lack of the usual barbiturate side effects shown by this drug led to its prescription as a hypnotic for expectant mothers. Condensation of the phthalimide of glutamic acid (39) with ammonia at elevated... 

One enantiomer of penicillamine (D-) exhibits antiarthritic properties but foe other is highly toxic (Figure 8.3). The teratogenic effects of thalidomide were induced by one enantiomer, foe other exhibited foe beneficial effects against morning sickness. 

Thalidomide Polycyclic teratogen, antiangiogenic mechanism unknown... 

Cj H403 85-44-9) sec Anisindione Chlortalidone Cilazapril Deptropine Fluorescein Hydralazine Indobufen Indoprofen Melphalan Phenolphthalein Phthalylsulfathiazole Pizotifen Pramipexole hydrochloride Saquinavir Sulfaloxic acid Thalidomide Tilisolol hydrochloride phthalide... 

CH4N2O 57-13-6) see Alfuzosin Allantoin Amobarbital Barbital Bromisoval Butalbital Carbasalate calcium Carbromal Cyclopentobarbital Dimethadione Dipyridamole Enoximone Ethotoin Heptabarb Metaxalone Methyclothiazide Orotic acid Paramethadione Pentobarbital Phenacemide Phenetuiide Phenobarbital Phenytoin Proquazone Secbutabarbital Secobarbital Sulfadimethoxine Thalidomide Trimethadione... 

Tetrahydrocannabinol (= THC)-11-carboxylic acid 290 Tetrahydrocortiso 221 Tetrahydrocortisone 221 Tetrahydrosteroids 222 Tetrazolium salts, reduction 61 Thalidomide 45 -, hydrolysis products 45 Thiabendazole 307, 308 Thiamine 235, 236, 397 Thickening agents 179 Thin-layer chromatography, advantage 5 -, numbers of publications per year 6 Thiobarbiturates 45,66 Thiocarbamide derivatives 322 Thiocarbamides, N -ary I-N -benzenesulfo-nyl- 248,249 Thiochrome 395... 

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