Drugs online research references
Ther Drug Monit. 1989;11(3):349-53.
Evaluation of the EMIT amitriptyline and nortriptyline assays for the determination of serum clomipramine and desmethylclomipramine.
Fraser AD, Bryan W, Isner AF.
Toxicology Laboratory, Victoria General Hospital, Halifax, Nova Scotia, Canada.
Homogeneous enzyme immunoassay reagents (EMIT) developed for the measurement of amitriptyline and nortriptyline in serum were modified to allow quantitation of clomipramine and desmethylclomipramine. The method was compared to a high-performance liquid chromatographic method. Between-run precision [coefficient of variation (CV)] for clomipramine in the EMIT assay for amitriptyline ranged from 2.6 to 3.2%. For desmethylclomipramine in the nortriptyline assay, the between-run CV ranged from 1.4 to 1.9%. Serum specimens from 43 patients (desmethylclomipramine) and 59 patients (clomipramine) were analyzed by both methods, with good correlation between methods. For clomipramine, recovery ranged from 100 to 102% (0-600 ng/ml range) and was 95-103% for desmethylclomipramine (0-600 ng/ml). The modified EMIT assays offered sufficient reproducibility, accuracy, and correlation with an established method for routine analysis of clomipramine and desmethylclomipramine.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2658213&dopt=Abstract
Pharmacol Biochem Behav. 1982 Oct;17(4):645-9.
A sensitive and selective monkey conflict test.
Patel JB, Migler B.
A conflict model is described in which clinically effective antianxiety agents exhibit pronounced anticonflict activity. Male squirrel monkeys were trained to depress a bar for 5 sec to obtain food reinforcement. The 6 hr test session was comprised of an initial 3 hr period in which each 5 sec response was punished and then a 3 hr unpunished period. Trained monkeys would rarely be shocked and would make most of their responses during the non-punished period. Both benzodiazepine (chlordiazepoxide and diazepam) and non-benzodiazepine (meprobamate and phenobarbital) anxiolytics produced pronounced and unequivocal increases in punished responding. Other psychoactive agents (damphetamine, chlorpromazine, ethanol, morphine, amitriptyline and imipramine) did not produce an increase in punished responding. Sensitivity (i.e., large magnitude effects), selectivity, stable baseline performance and fully automated features make this test useful in identifying potential anxiolytic agents in primates.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7178177&dopt=Abstract
Pol J Pharmacol Pharm. 1987 Mar-Apr;39(2):203-11.
Studies on the biochemical mode of action of EGYT-475, a new antidepressant.
Tekes K, Tothfalusi L, Malomvolgyi B, Herman F, Magyar K.
Department of Pharmacodynamics, Semmelweis University of Medicine, Budapest, Hungary.
We studied the mode of action of N-benzyl-piperazine-picolinylfumarate (EGYT-475) and of its metabolite N-benzyl-piperazine (EGYT-2760) in CFY rats. It was found that EGYT-475 had no uptake-inhibitory effect but EGYT-2760 inhibited the high-affinity uptake of 3H-noradrenaline, 3H-dopamine and especially that of 3H-serotonin both in vitro and ex vivo. Neither of the two compounds changed the serotonin turnover. Only EGYT-2760 evoked hyperthermia in rats at a high ambient temperature (28 degrees C). This effect was abolished by cyproheptadine but not by amitriptyline. EGYT-2760 antagonized serotonin-induced contractions of the stomach fundus but it was inactive in inhibiting the serotonin-induced platelet aggregation. Our results suggest that EGYT-2760, an active metabolite of EGYT-475, has a central serotoninomimetic action which involves 5-HT uptake-inhibition and 5-HT1 receptor agonistic effect.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2448760&dopt=Abstract
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