Drugs online research references
Acta Pharmacol Toxicol (Copenh). 1975;36(5):382-94.
Tricyclic antidepressant agents. I. Comparison of the inhibition of the uptake of 3-H-noradrenaline and 14-C-5-hydroxytryptamine in slices and crude synaptosome preparations of the midbrain-hypothalamus region of the rat brain.
Ross SB, Renyi AL.
The simultaneous uptake of 3-H-l-noradrenaline (NA) and 14-C-5-hydroxytryptamine (5-HT) in slices from the midbrain-hypothalamus region of the rat brain was compared with the corresponding uptake in crude synaptosome preparations of the same brain region. In both preparations the uptake of the two amines was selective at the concentration used (1 times 10- minus 7 M or lower). The KM values for the amines (NA: 2 times 10- minus 7 M in synaptosomes and 5 times 10- minus 7 M in slices; 5-HT: 8 times 10- minus 8 M in synaptosomes and 6 times 10- minus 7 M in slices) and the inhibitory concentrations (IC50) of the antidepressant agents were lower in the synaptosome experiments than in the slices experiments. Moreover the order of the inhibitory activities differed between the two preparations. In the slices experiments the NA uptake was inhibited most markedly by desipramine followed by imipramine greater than chlorimipramine = nortriptyline greater than or equal to amitriptyline greater than or equal to chlordesipramine whereas in the synaptosome experiments the order was desipramine greater than nortriptyline greater than or equal to chlordesipramine greater than or equal to imipramine greater than amitriptyline greater than or equal to chlorimipramine. For the 5-HT uptake in slices the order of activity was: chlorimipramine greater than imipramine greater than or equal to amitriptyline greater than or equal to chlordesipramine = desipramine greater than or equal to nortriptyline whereas in the synaptosome preparations the order was: chlorimipramine greater than imipramine greater than or equal to amitriptyline greater than or equal to chlordesipramine greater than nortriptyline = desipramine. The role of protein binding and diffusion barriers in the causation of the difference in the results obtained with the two preparations is discussed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1173528&dopt=Abstract
Clin Pharmacol Ther. 1982 May;31(5):609-16.
Steady-state plasma concentrations of cis- and trans-10-OH amitriptyline metabolites.
Bock JL, Giller E, Gray S, Jatlow P.
Plasma concentrations of the geometric isomers of 10-OH amitriptyline (10-OH AT) and 10-OH nortriptyline (10-OH-NT) were determined by reversed-phase high-pressure liquid chromatography. Steady-state concentrations of At, NT, and the four 10-OH metabolites were measured in 27 patients taking AT for depression. All of the unconjugated hydroxylated metabolites were usually detectable and trans-10-OH NT always predominated. Mean concentrations, expressed as percentage of the sum of all six compounds, were: AT 30%, NT 27%, cis-10-OH AT 1.1%, trans-10-OH AT 4.0%, cis-10-OH NT 4.0%, and trans-10-OH NT 33%. Repeated measurements on 10 patients over several weeks indicated that interindividual variations in absolute and relative 10-OH metabolite concentrations are much greater than day-to-day variations. Five patients who also received a phenothiazine had a lower proportion of 10-OH metabolites.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=6122526&dopt=Abstract
Acta Pharmacol Toxicol (Copenh). 1975;36(5):395-408.
Tricyclic antidepressant agents. II. Effect of oral administration on the uptake of 3-H-noradrenaline and 14-C-5-hydroxytryptamine in slices of the midbrain-hypothalamus region of the rat.
Ross SB, Renyi AL.
The inhibition of the simultaneous uptake of 3-H-l-noradrenaline (NA) and 14-C-5-hydroxytryptamine (5-HT) in slices of the midbrain-hypothalamus region of the rat brain after oral administration of desipramine, imipramine, nortriptyline, amitriptyline, chlordesipramine and chlorimipramine was determined. All compounds were more active in inhibiting the NA uptake than the 5-HT uptake. This difference was very marked for desipramine, imipramine, nortriptyline and chlordesipramine. Chlorimipramine was almost as active on the 5-HT uptake (ED50 = 35 mg/kg orally) as on the NA uptake (ED50 = 20mg/kg orally) and amitriptyline had low activity on both uptake mechanisms (ED50 greater than 50 mg/kg orally). Desipramine and imipramine were the most active compounds on the NA uptake (ED50 = 8 mg/kg orally for both compounds) and the duration of the action was very long. The ED50 values for nortriptyline and chlordesipramine in inhibiting the NA uptake were about 20 mg/kg orally for both compounds. The inhibition of the 5-HT uptake was less than 50% at 50 mg/kg orally for all compounds except for imipramine (ED50 = 50 mg/kg orally) and for chlorimipramine. The role of the biotransformation for the inhibitory activities of imipramine, chlorimipramine and amitriptyline was investigated in animals pre-treated with SKF 525 A. The inhibitory potency of imipramine was increased by the same factor for both uptake mechanisms probably due to the large increase in the concentration of imipramine in the rat brain, which was demonstrated after the administration of 14-C-imipramine. The inhibitory activity of chlorimipramine was somewhat more increased for the5-HT uptake than for the NA uptake. The low activity of amitriptyline seems to be mainly due to poor resorption, since pretreatment of the animals with SKF 525 A only slightly increased the potency whereas intraperitoneal injection of amitriptyline had a rather marked effect on the NA uptake (ED50 = 11 mg/kg intraperitoneally).
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1173529&dopt=Abstract
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