D-Pam

Another approach based on peptides is used by the Italian company Xeptagen (www.xeptagen.com). The D-PAM ligand optimized from a peptide library of 5832 randomized tripeptides is a tetramer of tripeptides linked together by a tetradentate lysine core [structure formula ([NH2-[l ]Arg-(Ji,S)Thr-[JJ]Tyr)4—(S)Lys2-(S)Lys-Gly]. All amino acids are in their artificial D-form giving the selector a higher proteolytic stability (Fassina et al, 2001). 

The subsequent acylation step is generally performed with trifluoroacehc anhydride (TFAA), PFPA, or heptafluorobutync anhydnde (HFBA), all of which yield excellent derivatives for GC-MS. The most popular derivatives include (a) TAB (TFA/n-BuOH)- Summons et al., 1974 Schulman and Abramson, 1975 Petty et al., 1976 Kingston and Duffield, 1978 Finlayson et al., 1980 (b) PAB (PFPA/n-BuOH). Sjoquist, 1979 Lapidot and Nissim, 1980 (c) TAM (TFA/MeOH) Zaylak et al., 1977, Coutts et al., 1979 (d) PAM (PFPA/MeOH) FauU et al., 1978 Ferkany et al., 1978 Corradetti et al, 1983 (e) HAM (HFBA/MeOH) Faull and Barchas, 1983 and (f) HAB (HFPB/ -BuOH) Lapidot and Nissim, 1980 Bengtsson et al, 1981. 

Polyacrylamide gel Polyacrylamide gels Polyacrylamide grout Polyacrylamide pAM) P o ly acryl arm d es... 

Hayama et al.132 discussed the catalytic effects of silver ion-polyacrylic add systems toward the hydrolyses of 2,4-dinitrophenylvinylacetate 84 (DNPVA) by using the weak nudeophilicity of carboxylic groups and the change-transfer interactions between olefinie esters and silver ions133Metal complexes of basic polyelectrolytes are also stimulating as esterase models. Hatano etal. 34, 13S) reported that some copper(II)-poly-L-lysine complexes were active for the hydrolyses of amino acid esters, such as D- and L-phenylalanine methyl ester 85 (PAM). They... 

In a further treatment we shall deal with Eqs. (14) and (14a) under such conditions only, which make the terms with (d2P/dt2)m and d,PJ dQp max negligible as compared with the other terms. Using Eq. (13) we can eliminate from Eq. (14) the unknown value of the surface coverage 0 and thus arrive, for a given pumping speed S and heating rate dT/dt, at a relation between the measured data (i.e. the maximum pressure Pm or the maximum partial pressure Pam, and the corresponding temperature Tm) and the parameters fed, K, Ed, — AH, and x, characteristic of the surface... 

Fig. 15.15 Response of the AchE TEo mode of the MCLW sensor to 1 pM paraoxon, regeneration by 2 PAM and the calibration curve. (A) Tris buffer, (B) AchCl before paraoxon inhibition, (C) AchCl after paraoxon inhibition and (D) regeneration by 2 PAM. Reprinted from Ref. 52 with permission. 2008 Elsevier...

Havron, M.D., Diet drugs and pulmonary hypertension, /. Pam. Tract., 43, 434-435,1996 Cleare, A.J., Phentermine, psychosis, and family history, /. Clin. PsychopharmacoL, 16,470 71, 1996. 

Fig. 6.19 Relaxation rates from single exponential fits to the NSE data from PAM AM den-drimers of generation g=5-8 (5%) in d-methanol. The solid lines are derived from NSE data from the FRJ2-NSE (Jiilich) and MESS (Saclay) spectrometers and show the prediction for simple Stokes-Einstein diffusion of hard spheres at finite concentration. (Reprinted with permission from [306]. Copyright 2002 American Institute of Physics)...

For the graduate or second course the material in Parts 2 to 5 should be suitable. Finally, I d like to acknowledge Professors Keith Levien, Julio Ottino, and Richard Turton, and Dr. Amos Avidan, who have made useful and helpful comments. Also, my grateful thanks go to Pam Wegner and Peggy Blair, who typed and retyped—probably what seemed like ad infinitum—to get this manuscript ready for the publisher. 

Verma, R.P., Hansch, C. and Selassie, C.D. (2007) Comparative QSAR studies on PAM PA/modified PAM PA for high throughput profiling of drug absorption potential with respect to Caco-2 cells and human intestinal absorption. Journal of... 

Repeated oral administration of 2-PAM or TMB-4 In dogs may lead to areas of acute necrosis and to deposition of fibrous tissue In the stomach. Whether those effects are due to a specific action of the oxime or to chronic irritation related to repeated administration is not known. Nor are the long-term effects of such chronic administration and consequent fibrosis known. However, single doses, even orally, have not been reported to produce tissue changes. No change was found in the gastrointestinal tracts of rats given P2S (200 mg/kg) orally each day for 50 d.23... 

A second subject (6849) experienced a grand mal seizure 3 h after receiving 300 mg of 2-PAM (chloride form) intramuscularly. He regained consciousness within 5 min he had bitten his tongue. He was initially lethargic, but felt well 10 h later. He was transferred to Walter Reed Hospital, but followup records are not available. He had received 300 mg of 2-PAM intramuscularly 5 and 8 d before the episode. The only symptom on those occasions was local pain at the injection site. 

Lindsey, D., Pfautz, J.H., Dill, D.B., and Ward, D.M. Oral toxicity of EA 2071 (2-PAM lactate). CWLTM 20-17. U.S. Army Chemical Warfare Laboratories, Army Chemical Center, Md., 1959. 

Edery96 studied the effects of V on neuromuscular blockade Induced by ethyl pyrophosphate or neostigmine methylsulfate in the cat, finding only an Insignificant effect. The skeletal muscle responses to both direct and Indirect excitation were altered by V In the absence of any other active chemical. The effect of V on the response of indirectly stimulated muscle to d-tubocurarlne was an Increase In the blockade of neuromuscular transmission similar to that of the salts of 2-PAM and of III. 

Blockade of neuromuscular transmission produced by an intravenous dose of d-tubocurarine chloride at 0.3 mg/kg, but not that due to 0.5 mg/kg, was antagonized by intravenous 2-PAM 1 at 5 mg/kg. Edrophonium bromide (intravenously at 0.2 mg/kg) was a more potent antagonist of d-tubocurarlne than this dose of 2-PAM 1. Partial blockades of neuromuscular transmission Induced by intravenous injections of decamethonium bromide at 20 Vg/kg, neostigmine bromide at 1 mg/kg, or succinylcholine chloride at 50 Mg/kg were intensified by Intravenous Injection of 2-PAM 1 at 5 mg/kg, in about the same way in which they were enhanced by intravenous doses of edrophonium bromide at 0.2 mg/kg. Intravenous doses of 2-PAM I at up to 150 mg/kg had no effect on the muscle response to direct stimulation in anesthetized cats. 

Way et al. found N-methylpyridlnium-2-nitrile in human urine as a metabolite of 2-PAM. Kramer reported that five men given 2-PAM 1 at 2 g/day by mouth on 2 consecutive days while they were on a closely supervised regimen of dietary and other intakes excreted in their urine not only unaltered 2-PAM, but also a material that had a bright blue fluorescence when exposed to UV light (366 nm). This material was shown not to result from simple exposure to urine by incubation of 2-PAM 1 in normal human urine under several different conditions for up to 7 d. It was thought possibly to be a derivative of N-methylpi olinic acid. 

Longo, V.G., Nachmansohn, D., Bovet, D. 1960. Aspects electroencephalographiques de l antagonlsme entre le iodomethy-late de 2-pyrldlne aidoxime (PAM) et le methylfluororophosphate d lsopropyle (sarin). Arch. Intemat. Pharmacodyn. 123 282-290. 

D-l 2170 2-PAM pralidoxime chloride (or Iodide) protopam chloride (or iodide) 2-f ormyl-N-me thylpyridinium chloride Tor iodide) oxime pyrld ine-2-aldoxime methochloride (or methlodlde) 51-15-0 607... 

D-2 P2S methyl methanesulfonate derivative of 2-PAM pralidoxime methanesulfonate Protopam methanesulfonate 154-92-2 95... 

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