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Simulation-based cheminformatic analysis of organelle-targeted molecules: lysosomotropic monobasic amines [PDF]

Xinyuan Zhang, Nan Zheng, Gus R. Rosania, AM Kaufmann, M Duvvuri, C Duve de, MJ Reasor, H Fujimura, G Cramb, B Styrt, JP Ploemen, PO Seglen, S Ohkuma, UE Honegger, UE Honegger, G Morissette, G Morissette, SJ Hurwitz, J Ishizaki, B Lemieux, WC Yang, A Bulychev, M Duvvuri, ZI Cabantchik, RW Horobin, RJ Gonzalez-Rothi, X Zhang, S Trapp, LM Loew, SL Rybak, CC Cain, RA Preston, RW Dyke Van, SM Felber, S Simon, M Duvvuri, W Li, P Schneider, BP Schmid, WA Daniel, J Ishizaki, D Drenckhahn, CM McCloud, M Hetman, D Pessayre, K Balon, WN Charman, GR Rosania, VY Chen, K Shedden, VY Chen, VY Chen, M Duvvuri, Y Gong, PV Balimane, JD Irvine, M Matsumoto, T Kawai, S Fletcher, P Cristofaro, JP Falgueyret, PR Ginkel van, E Jacotot, VR Fantin, GG D’Souza, V Weissig, GG D’Souza, JP Overington, GR Rosania   +68 more
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Pharmacokinetics of Procainamide and N-Acetylprocainamide in Rats

Journal of Pharmaceutical Sciences, 1981
The pharmacokinetics of distribution and elimination of procainamide and its major metabolite, N-actylprocainamide, were studied in rats. Eight rats were selected randomly, and each received intravenously 14C-labeled procainamide hydrochloride (75 mg/kg) or 14C-labeled N-acetylprocainamide hydrochloride (86 mg/kg) according to a two-way crossover ...
B L, Kamath, C M, Lai, S D, Gupta, M J, Durrani, A, Yacobi   +4 more
exaly   +3 more sources

Age-Related Pharmacokinetics of N-Acetylprocainamide in Rats

Journal of Pharmaceutical Sciences, 1983
The pharmacokinetics of N-acetylprocainamide, administered orally or intravenously, were studied in 3-, 6-, and 12-month-old rats using a two-way crossover study design. At 3, 6, and 12 months of age, the half-life values of N-acetylprocainamide were 1.66, 1.82, and 2.29 hr, respectively; the apparent volumes of distribution were 4.75, 3.35, and 1.98 ...
A, Yacobi, B L, Kamath, H F, Stampfli, Z M, Look, C M, Lai   +4 more
exaly   +3 more sources

Antiarrhythmic potency of procainamide and N-acetylprocainamide in rabbits

European Journal of Pharmacology, 1978
The antiarrhythmic potency of procainamide (PA) and N-acetylprocainamide (NAPA) has been investigated in rabbits using isolated atrial preparations and ouabain-induced ventricular fibrillation in vivo. At concentrations in the range 3 x 10(-5) to 1 x 10(-3) M, both PA and NAPA decreased the maximum following frequency (MFF) of isolated atria. The dose--
Rodney F Minchin
exaly   +4 more sources

N-acetylprocainamide and ischemia-induced ventricular fibrillation in the dog

European Journal of Pharmacology, 1979
Open-chest dogs anesthetized with pentobarbital were treated with saline or N-acetylprocainamide (20 mg/kg, i.v.) 10 min prior to simultaneous ligation of the left anterior descending and septal coronary arteries. Ventricular fibrillation occurred in 20 of 26 control dogs but in only 6 of 15 dogs treated with N-acetylprocainamide (P less than 0.05 ...
R D, Reynolds, B L, Kamath
exaly   +3 more sources

Effects of N-acetylprocainamide as compared with procainamide in isolated rat atria

European Journal of Pharmacology, 1975
The actions of procainamide and its major metabolite N-acetylprocainamide were tested and compared on isolated rat atria. While procainamide exerted a negative chronotropic and iontropic effect, N-acetylprocainamide had the opposite effect. It is suggested that a N-acetylprocainamide-induced increase in myocardial work can counteract the negative ...
H, Refsum, K, Frislid, P K, Lunde, K H, Landmark   +3 more
exaly   +3 more sources

Pharmacokinetics of N-Acetylprocainamide

Angiology, 1986
Shortly after Dreyfus and his colleagues demonstrated that procainamide was metabolized by acetylation to N-acetylprocainamide (NAPA), Drayer, Reidenberg and Sevy reported that NAPA had antiarrhythmic activity in an animal model. We confirmed these findings and found that plasma levels of NAPA were high enough to warrant consideration in managing ...
A J, Atkinson, T I, Ruo
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Kinetics of N-acetylprocainamide deacetylation

Clinical Pharmacology and Therapeutics, 1980
The kinetics of N-acetylprocainamide (NAPA) deacetylation to procainamide (PA) were determined in a normal subject using NAPA-13C, labeled in the acetyl group. The deacetylation clearance of NAPA (ClD) was found to be 6.5 ml/min whereas total NAPA elimination clearance was 231 ml/min, so that 2.8% of the administered NAPA-13C was metabolized by ...
G P, Stec, T I, Ruo, J P, Thenot, A J, Atkinson, Y, Morita, J J, Lertora   +5 more
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Clinical Pharmacokinetics of N-acetylprocainamide

Clinical Pharmacokinetics, 1982
Since N-acetylprocainamide was identified in the urine of patients receiving procainamide, this compound has been studied both as a metabolite of procainamide and as a separate antiarrhythmic agent. N-acetylprocainamide absorption following oral administration is more than 8-% complete.
S J, Connolly, R E, Kates
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Antiarrhythmic potency of N‐acetylprocainamide

Clinical Pharmacology & Therapeutics, 1975
Compared to procainamide in an animal arrhythmia model, the antiarrhythmic potency of the N‐acetylated metabolite of procainamide (NAPA) was 92% with respect to dose and 70% with respect to plasma level. The antiarrhythmic effects of combinations of the drugs were additive.
J, Elson, J M, Strong, W K, Lee, A J, Atkinson   +3 more
openaire   +2 more sources