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At least 19 recordsLinked to original sources
PubMed1979

[Derivatives of 2,3,4,5,-tetrahydro-1H-pyrido-(3,2-b)azepine and 2,3,4,5-tetrahydro-1H-pyrido(2,3-b)azepine and their corresponding lactams. II. Synthesis and pharmacologic study of their psychotropic activity].

Preparation of the N-(2-diethylaminoethyl) derivatives of lactam (II) and of the N-(3-dimethylaminopropyl) derivative of lactam (XI) is described. Synthesis of the N-[4-(2-hydroxyethyl)piperazinylacetyl]- and 1-carbothiamide derivatives of azepine (I) and of the n-(chloroformyl)- and N-(carbamoyl) derivatives of azepine (XII) are also described. Some pharmacological results indicate a partial tranquilizing activity.

Animals↗
PubMed1978

[Tetrahydropyridoazepine and tetrahydropyridoazepinone derivatives. I. Derivatives of 2,3,4,5-tetrahydro-1H-pyrido[3,2b]azepine and of the corresponding lactam].

Preparation of N-derivatives of 2,3,4,5-tetrahydro-1H-pyrido[3,2-b]azepine and, in one case, of 2,3,4,5-tetrahydro-1H-pyrido[3,2-b]azepine-2-one was achieved by introducing the substituents COCl, CONH2, CO2(CH2)3N(CH3)2, COCH2Br and (CH2)3N(CH3)2. The pharmacological results indicate some effect on the ANS.

Adrenergic alpha-Antagonists↗
PubMed1977

[Derivatographic analysis of 6-beta-[(hexahydro-1H-azepin-1-yl) methylenamino]penicillanic acid].

Derivatographic analysis of 5 samples of 6-beta-(hexahydro-IH-azepin-I-yl)methylenamino penicillanic acid was performed. In addition to the antibiotic the samples had water and acetone in their composition. No effects associated with changes in the physical and chemical state of the substance were observed on the derivatogramme of the samples containing 0.2 and 0.8 per cent of water up 140 degrees C. With a further increase in the temperature an exothermic effect was observed with maximum at 152--153 degrees C connected with melting and chemical degradation of the substance. The derivatogrammes of the samples containing 89--96.4 per cent of the antibiotic were characterized by an endothermic effect with minimum at 65 degrees C caused by evaporation of acetone and partially water from them and by an exothermic effect with maximum at 120 degrees C practically not accompanied by any change in the weight resulting from chemical interaction of the antibiotic with water. The study showed sensitivity of 6-beta-(hexahydro-IH-azepin-I-yl)methylenaminopenicillanic acid to the presence of even insignificant amounts of water in it, maximum elimination of which from the antibiotic is an important factor of increasing its stability.

Crystallization↗
PubMed1976

[Stability of 6-beta-[(hexahydro-1H-azepin-l-yl)methyleneamino]-penicillanic acid in aqueous solutions].

Stability of acqueous solutions of 6-beta-[(hexahydro-IH-azepin-I-yl)methylenamino] penicillanic acid at various values of pH and temperature was studied. It was found that inactivation of the antibiotic in both the acid and the alkaline medium proceeded according to the equation of the 1st order. At pH 1.3 and a temperature of 35 degrees the half life of the antibiotic was 7 hours. The activation energy calculated according to the Arrenius equation was 13.5 kcal/mol at pH 1.3 and 22.2 kcal/mol at pH 10.5. The antibiotic was inactivated in glycol and phosphate buffers. Its qualitative analysis was performed according to an improved iodometric method.

Amidines↗
PubMed1979

A comparison between meptazinol and omnopon in the relief of postoperative pain.

In a random double-blind trial, meptazinol 100 mg, a new hexahydro-azepine derivative, was found to be comparable to Omnopon (papaveretum) 20 mg when given intramuscularly for the control of pain in 50 cases after hysterectomy. The onset of analgesia was rapid and the effect lasted for about 3 hours. Cardiovascular and respiratory systems remained stable. No significant difference as regards sedation and nausea was noticed between the two groups.

Adult↗
PubMed1977

Effect of lofepramine and other antidepressants on the uptake of 5-hydroxytryptamine and noradrenaline into rat brain monoaminergic neurons.

Lofepramine, (N-methyl-N-[4-chlorobenzoylmethyl]-3-[10,11-dihydro-5H-dibenz(b,f)-azepin-5-yl]-propylamine hydrochloride), is a new antidepressant with low toxicity and no peripheral anticholinergic activity. Its effect on 5-hydroxytryptamine (5-HT) and noradrenaline uptake into rat brain monoaminergic neurons was studied and compared with that of other antidepressants, particularly with that of imipramine and desipramine. Lofepramine inhibited both 5-HT and noradrenaline uptake into synaptosomal fractions in vitro but was 4 times more potent in inhibiting noradrenaline than 5-HT uptake, indicating the effect resembles that of desipramine. Noradrenaline uptake was also preferentially inhibited in synaptosomes from brain of rats treated previously with lofepramine or desipramine (i.p.). Pretreatment with SKF 525A (i.p.) did not diminish the effect of lofepramine, but rather potentiated it. Therefore it is suggested that the formation of desipramine is not necessary for lofepramine to exhibit, the effect on amine uptake in vivo. Both lofepramine and desipramine inhibited intraventricular noradrenaline uptake into synaptosomes without any effect on 5-HT uptake. These results suggest that lofepramine is qualitatively similar to desipramine with respect to preferential inhibition of noradrenaline uptake into central noradrenergic neurons.

Animals↗
PubMed1976

The action of psychotropic drugs on DOPA induced behavioural responses in mice.

The "DOPA potentiation" test in mice was investigated for its usefulness in the detection of compounds with antidepressant properties. It was found that the anti-depressant drugs imipramine, amitriptyline, 5-methylamino-acetyl-6-methyl-5,6-dihydro-phenanthridine-HCl (Org OI77) and 1,2,3,4,10,14b-hexahydro-2-methyl-dibenzo[c,f]pyrazino[1,2-a]azepine-HCl (mianserin, Org GB 94) potentiated the behavioural effect of DOPA in groups of mice which had been treated 17 h previously with the monoamine oxidase inhibitor (MAOI) iproniazid. However, the DOPA response was also potentiated by a variety of centrally acting drugs which do not have antidepressant properties (atropine, methysergide, chlordiazepoxide, apomorphine). The peptide hormones ACTH4-10 and desglycinamide lysine vasopressin had equivocal effects while melanocyte stimulating hormone release-inhibiting factor (MIF) had no effect on the DOPA response. The DOPA response was inhibited by the neuroleptics chlorpromazine and haloperidol. There appeared to be no correlation between the effects of the drugs on the behavioural responses elicited by DOPA and the changes found in the brain concentration of noradrenaline, dopamine, serotonin, gamma-aminobutyric acid, tryptophan and tyrosine. It is concluded that the "DOPA potentiation" test cannot be considered as a reliable test in the detection of anti-depressant compounds.

Animals↗
PubMed1976

[Double-blind clinical study of carpipramine/placebo (author's transl)].

A statistically planned double blind cross-over test with the substances 1-[3-(10,11-dihydro-5H-dibenz[b;f]-azepin-5-yl)-propyl]-4-piperidino-piperidine-4-carboxamide dihydrochloride-monohydrate (carpipramine, BAY b 4343 b) and placebo (BAY b 4343 a) was carried out on 30 long-term hospitalized schizophrenic patients. The study was evaluated by means of the kappa2-test and yielded the following results: 1. It could be statistically proved that carpipramine has a positive effect on psycho-pathological disorders in the behaviour of long-term hospitalized schizophrenic patients (kappa2 = 9.224; FG = 1; p greater than 0.05). 2. As regards the favourable influence of carpipramine on "productive" versus "non-productive" form of schizophrenia there were no differences. 3. Side effects or complications of a psychic, autonomic and/or motoric manner could not be seen. The usual laboratory tests showed no deviation from normal.

Adult↗
PubMed1976

[Activity profile of carpipramine. Results of an open trial and a double-blind trial versus doxepin].

During an uncontrolled trial 46 depressed patients (39 endogenous depressions, 5 schizoaffective psychoses and 2 paranoic schizophrenics with depressive syndromes) were treated for 43 days on the average with 3 X 100 mg 1-[3-(10,11-dihydro-5H-dibenz[b,f]-azepin-5-yl)-propyl]-4-piperidino-piperidine-4-carboxamide-dihydrochloride-monohydrate (carpipramine) daily. The clinical impression of the improvement and the results of the Hamilton-Scale for depressions (19 patients, 24 items) showed a clear antidepressive effect of carpipramine. During a double-blind trial 14 patients were treated with carpipramine and 16 with doxepine for 30 days. Most patients suffered from endogenous depressions with paranoic symptoms or from schizophrenia with depressive syndromes. Statistical analysis of the Hamilton-Scale for depressions and the AMP-System showed the antidepressive and antipsychotic effect of carpipramine. Analysis of covariance showed no significant difference between carpipramine and doxepine. Altogether we treated 60 depressive patients with carpipramine. 26 patients improved very well and 11 moderately, that means 37 patients out of 60 reacted positively to therapy with carpipramine. One endogenous depression and a schizoaffective psychosis changed into a manic phase. A provocation of schizophrenic symptoms was not noticed. Carpipramine was very well tolerated and can be classified as a non-sedative antidepressant with an antipsychotic effect.

Anti-Anxiety Agents↗
PubMedDate not supplied

Characterization of glucuronide metabolites of carbamazepine in human urine by gas chromatography and mass spectrometry.

Glucuronide metabolites of carbamazepine (5 H-dibenz[b,f]azepine-5-carboxamide) were identified in human urine following chromatography on XAD-2 resin, permethylation, and combined gas chromatography and mass spectrometry with an SE-30 capillary column. Eight glucuronide metabolites, previously unidentified in man, were characterized as their permethylated derivatives. These included carbamazepine N-glucuronide (M+. 482), three isomers of dihydroxycarbamazepine O-glucuronide (M+. 542), three isomers of hydroxymethoxycarbamazepine O-glucuronide (M+. 542), and one isomer of hydroxycarbamazepine O-glucuronide (M+. 512). Other glucuronide metabolites, previously identified following enzymatic hydrolysis, were characterized as the unhydrolyzed, permethylated glucuronides, 10,11-dihydro-10,11-di--hydroxy carbamazepine O-glucuronide (M+. 544), and three isomers of monohydroxycarbamazepine O-glucuronide (M+. 512).

Biotransformation↗
PubMed1977

[Studies on cardio-circulatory effects of carpipramine. Results of a double-blind study (author's transl)].

For eight weeks 30 psychotic patients with a healthy cardiovascular system received 3 X 50 mg 1-[3-(10,11-dihydro=5H-dibenz[b,f]-azepin-5-yl]-propyl]-4-piperidiono-piperdine-4-carboxamide dihydrochloride-monohydrate (carpipramine) per day with a placebo phase of three weeks either previous to the medication of succeeding it. In addition there was a group of similar patients without any medication. From this study it was concluded that carpipramide has no depressive effect on the cardiovascular system. The differences in blood pressure and heart rate after the change from medication to placebo indicate a certain vegetative lability in this phase. In the ECG, no irregularities of the atrioventricular and intraventricular conduction and its repolarisation in form of a lengthening were observed; only the WPW-syndrome noticed with one patient might be related to the medication since it occurred at the end of the three weeks during which carpipramine had been administered.

Adult↗
PubMedDate not supplied

[The place of mianserin among the antidepressants (author's transl)].

The originality of mianserin lies mainly in its chemical formula ; it is a tetracyclic piperazino-azepine compound. Moreover its pharmacological profile differs from that of other antidepressant drugs because it is devoid of central anticholinergic effects, it inhibits 5-hydroxytryptophane (the precursor of serotonine) and contrary to the tricyclics it does not affect the re-uptake of the amine-transmitters but increases the turnover of noradrenaline. It has been shown in a clinical trial that mianserin induces a hypomania in some manic-depressed patients. Regarding the antidepressive effect, mianserin is superior to placebo and as effective as imipramine and amitriptyline. It simultaneously works on anxiety, psychomotoric retardation and suicidal tendency; sleep improves under mianserin's influence. The value of mianserin is proved by its safety in use. It has no cardiotoxic effect and does not interact with coumarin-type anticoagulants. Since there are no anticholinergic effects, mianserin can be given to patients suffering from glaucoma or prostatic hypertrophy. Finally it appears that mianserin lowers the suicidal risk through its sedative properties.

Animals↗
PubMed1977

The mechanisms of lethal action of arabinosyl cytosine (araC) and arabinosyl adenine (araA).

Certain D-arabinosyl nucleosides, notably arabinosyl cytosine (araC) and arabinosyl adenine (araA), are useful in the treatment of certain leukemias and some DNA virus infections, respectively. The compounds are lethal to animal cells and some bacteria. Despite extensive deamination, the parent nucleosides are transported within sensitive cells and phosphorylated to the mono-, di- and triphosphates. AraCTP and araATP are good specific competitive inhibitors of tumor cell of virus-induced DNA polymerases, competing with dCTP and dATP respectively. In addition to markedly inhibiting DNA synthesis, the aranucleotides enter newly formed DNA in internucleotide linkage. Sensitivity to the nucleosides appears to correlate with the relative ratio of formation of the triphosphate via a nucleoside kinase to degradation of the nucleoside via a nucleoside deaminase. Inhibition of the deaminase increases formation of the aranucleoside triphosphate in leukemic or virus-infected cells and markedly increases the toxicity of the nucleosides. Combinations of inhibitors of the deaminases and of the aranucleoside are being explored in clinical situations. In addition, the slow penetration of aranucleotides into cells has been observed and some of these 5'-phosphates are useful antiviral agents, e.g., against herpes virus in herpetic kiratitis.

Adenine↗
PubMed1977

The effect of adenosine on lymphoid cell proliferation and antibody formation.

The discovery of an association of certain primary defects in human purine metabolism with immunodeficiency disease has served to focus attention on the possible role of purine compounds in the functional activity of lymphoic cells. Considerable evidence has accumulated of the need within the intact organism for purine and pyrimidine compounds supplied by the liver as a supplementary nutritional requirement for the growth of the rapidly proliferating tissues of certain organ systems. Likewise, lymphoid cells cultured in vitro show evidence of an enhancement of indices of cellular proliferation and of antibody synthesis when exogenous adenosine is added to the medium. These functions are inhibited by high concentrations of adenosine and there is some evidence that T-cell proliferation shows a greater sensitivity to inhibition by adenosine than B-cells. These observations may be significant in relation to the known defects in human purine metabolism and their mechanism for producing immunodeficiency.

Adenosine↗
PubMed1979

In vitro mutagenicity and cell transformation screening of caprolactam.

Caprolactam was tested for genetic activity in bacterial and mammalian screens. It was inactive in the following tests: a) Salmonella/microsome mutagenicity; b) Chinese hamster ovary cell mutagenicity (induction of 6-thioguanine mutants); c) Enhancement of SA7 virus transformation of primary hamster embryo cells, when administered before or after virus, and; d) Chemical transformation of secondary hamster embryo cells.

Animals↗
PubMedDate not supplied

A double-blind comparison of meptazinol with placebo in postoperative pain.

In a double-blind clinical trial, meptazinol (400-mg capsules) was shown to be significantly better than placebo in relieving postoperative pain in patients who had under gone total abdominal hysterectomy operations. Analgesic activity was assessed by patients rating their pain before and 1 hour after the administration of each treatment, by sequential analysis of patient and investigator preference for treatment, and by calculating the time interval between doses of the two treatments.

Adult↗