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Query: UMLS:C0033377 (prolapse)
 11,717 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

RMI 61 140, RMI 61 144 and RMI 61 280 are newly synthetized N-[8-R-dibenzo(b,f)oxepin-10-yl]-N'-methyl-piperazine-maleates which show interesting psychopharmacologic effects. This work contains the results of a study performed with these three compounds, in order to demonstrate their neuropsycholeptic activity in comparison with chloropromazine (CPZ) and chlordiazepoxide (CPD). The inhibition of motility observed in mice shows that the compounds reduce the normal spontaneous motility as well as the muscle tone. The central-depressant activity is evidenced by increased barbiturate-induced sleep and a remarkable eyelid ptosis can also be observed. Our compounds do not show any activity on electroshock just as do CPZ and CPD. As to the antipsychotic outline, our compounds show strong reduction of lethality due to amphetamine in grouped mice and a strong antiapomorphine activity. They show also an antiaggressive effect and an inhibitory activity on avoidance behaviour much stronger than CPZ. We have also found extrapyramidal effects, as catalepsy, common to many tranquillizers of the kind of the standards used by us. As for vegetative phenomena, the compounds show hypotensive dose related action ranging from moderate to strong, probably due to an a-receptor inhibition. Adrenolytic activity against lethal doses of adrenaline, antiserotonin and antihistaminic effects, as well as other actions (hypothermia, analgesia, etc.) confirm that RMI 61 140, RMI 61 144 and RMI 61 280 are endowed with pharmacologic properties similar and more potent than those of CPZ. Studies on the metabolism of brain catecholamines show that they are similar to CPZ, although with less effect on dopamine level.
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PMID:Pharmacological properties of new neuroleptic compounds. 0 25

Amoxapine possesses a broad spectrum of psychotropic actions, including antidepressant and neuroleptic effects in animals. Antidepressant activity is characterized by its ability to inhibit tetrabenazine-induced depression, antagonize reserpine-induced hypothermia and enhance yohimbine lethality. Neuroleptic activity is demonstrated by the ability of amoxapine to decrease locomotor activity, induce ptosis and catalepsy, inhibit apomorphine gnawing and amphetamine stereotyped behavior and by characteristic changes in monkey discriminated avoidance behavior. The fact that punished responding in squirrel monkeys was present was present after repeated administration may indicate an anti-anxiety action of this drug. Evidence is offered that the conversion of the tertiary terminal nitrogen to a secondary amine may alter the pharmacologica properties of dibenzoxazepines in a similar way to the for the phenothiazines.
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PMID:The neuropharmacological actions of amoxapine. 2 99

The tranquillising activity of 3-[gamma-(p-fluorobenzoyl)propyl]-2,3,4,4a,5,6-hexahydro-1-(H)-pyrazino [1, 2-a]quinoline hydrochloride (centpyraquin), a new adrenergic neurone blocking antihypertensive agent, has been evaluated in various laboratory animals. The compound has a calming effect in mice, rats, cats and monkeys. In low doses it reduces the spontaneous motor activity followed in progressively higher doses by hypothermia, ptosis and catalepsy and a taming effect in monkeys and cats. It potentiates pentobarbitone-, hexobarbitone- and ethanol-induced sleep and antagonises amphetamine induced toxicity in mice. It, however, fails to antagonise morphine induced mania and hyperactivity in cats. It blocks conditioned avoidance response in rats at a much lower dose (ED50 = 2.73 mg/kg) than the unconditioned response (ED50 = 10,9 mg/kg). In cats centpyraquin increases the voltage and slows the frequency of cortical EEG discharges. Centpyraquin has the profile of activity of a neuroleptic on the central nervous system.
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PMID:Pharmacological studies on 3-[gamma-(p-fluorobenzoyl)propyl]-2,3,4,4a,5,6-hexahydro-1-(H)-pyrazino ]1,2-a] quinoline hydrochloride (compound 69/183). Part III: Assessment of tranquillising activity. 3 55

The interaction between neuroleptics and an anticholinergic, biperiden, in the antiavoidance, catalepsy and ptosis tests was investigated in mice for the purpose of predicting the extrapyramidal side-effects of neuroleptics. The cataleptic effect of most neuroleptics used was antagonized to some extent by biperiden, while the ptotic effect was hardly influenced. The antiavoidance effect of haloperidol, trifluperidol and perphenazine was markedly antagonized and that of chlorpromazine moderately. However, the effect of thioridazine, chlorprothixene, levomepromazine and clozapine was little antagonized. In neuropharmacological tests, haloperidol, trifluperidol and perphenazine exhibited a selective antidopaminergic activity, while chlorprothixene, levomepromazine and clozapine showed antidopaminergic, antiadrenergic and also anticholinergic activities when similar doses were given. These results indicate that biperiden antagonism may be marked in the tests related to the extrapyramidal symptoms and in drugs liable to induce extrapyramidal side effects, however, there would be little or no antagonism in drugs possessing the anticholinergic property and eliciting few extrapyramidal side-effects.
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PMID:Differential antagonism of antiavoidance, cataleptic and ptotic effects of neuroleptics by biperiden. 4 13

The behavioral effects of lopramine [N-methyl-N-(4-chlorobenzoyl-methyl)-3-(10, 11-dihydro-5H-dibenz (b,f) azepin-5-yl) propylamine hydrochloride] were investigated in mice and rats and compared with those of amitriptyline and imipramine. Lopramine inhibited reserpine hypothermia and haloperidol catalepsy in mice and tetrabenazine ptosis in rats. In addition the drug potentiated the effects of methamphetamine, and DOPA- or apomorphine-induced stereotypy in mice, whereas it suppressed muricide of the rat induced by either olfactory bulbectomy or delta9-tetrahydrocannabinol, similar to the responses seen with imipramine and amitriptyline. On the other hand,lopramine increased spontaneous motor activity and markedly potentiated methamphetamine hyperactivity. In contrast to imipramine and amitriptyline, lopramine failed to counteract both the lethal effect of physostigmine and oxotremorine tremor in mice, indicating that the drug had no central anticholinergic effect. Lopramine, even at such a large dose as 5,000 mg/kg p.o., caused neitherimpairment of coordinated motor activity nor muscle relaxation. It is concluded that lopramine is a new type of tricyclic antidepressant with extremely low toxicity and without central anticholinergic action.
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PMID:[Behavioral pharmacology of a new antidepressant, lopramine]. 103 9

Ergometrine, a spasmolytic which also stimulates dopamine receptors, was investigated as a potential central stimulant. It did not influence the locomotor activity of normal rats and mice, and in high doses even depressed it. The locomotor activity depressed by reserpine, spiroperidol, and pimozide was elevated by ergometrine. Ergometrine antagonized neuroleptic-induced catalepsy and abolished ptosis and hypothermia produced by reserpine. Given alone ergometrine depressed the body temperature in rats and mice, and this effect was abolished by pimozide in both species, and by spiroperidol and haloperidol in mice. The hypothermia was not antagonized by atropine. In several respects the central action of ergometrine resembles that of apomorphine.
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PMID:Central action of ergometrine. 103 20

Butaclamol hydrochloride (AY-23,028) is a member of a new chemical class for which antipsychotic activity in humans has recently been demonstrated. The compound antagonized amphetamine-induced stereotyped behavior in rats, amphetamine toxicity in aggregated mice and apomorphine-induced emesis in dogs. It depressed both discriminated avoidance and continuous lever-pressing behavior in rats and inhibited ambulation and rearing in the open field. At higher doses, AY-23,028 induced catalepsy. Adrenergic blocking activity, measured by the antagonism of epinephrine-induced mortality, was weak. These pharmacological actions are characteristic of neuroleptic drugs. In the dose range where the aforementioned effects were observed AY-23,028 did not antagonize either the tetrabenazine-induced ptosis or the tremorine syndrome and did not cause either hypothermia or ataxia. The potency and onset of action of AY-23,028 were comparable to those of fluphenazine but AY-23,028 was of longer duration. The results are discussed in relation to current concepts of neuroleptic mechanisms.
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PMID:The behavioral pharmacology of butaclamol hydrochloride (AY-23,028), a new potent neuroleptic drug. 117 96

Six hours after intracerebral administration, the central effects of metaraminol were examined with the following results. 1) Metaraminol in doses of 40 approximately 160 mug decreased spontaneous motor activity in mice as measured by the photo-cell counters method, the wheel cage method or the open-field test. Ptosis and catalepsy induced at these doses. 2) Metaraminol in doses of 40 approximately 80 mug which influenced the spontaneous motor activity in mice, blocked the avoidance behaviour but not escape. 3) Metaraminol in doses of 1.25 approximately 10 mug which did not influence the spontaneous motor activity in mice, markedly blocked the attaching response induced by the electroshock. 4) Ten min after intraventricular administration, metaraminol in a dose of 500 mug induced the arousal pattern of EEG in sensory cortex of cats and this pattern lasted for 30 min. Ninety min after administration, EEG tracings reverted to the drowsy pattern.
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PMID:[Effect of beta-phenylethylamine derivatives on the central nervous system. II. Pharmacological effect of the intracerebral administration of metaraminol on the central nervous system]. 117 7

Influence of metaraminol on behavioural changes in mice was studied with the following results. 1) When metaraminol was injected i.c., spontaneous motor activity as tested by either the photocell counters method or open-field test markedly increased within 90 min after injection, while on the contrary greatly decreased 3 hr later as compared with control group. Thus, these biphasic effects of metaraminol were clearly established. 2) 30 min after injection, metaraminol in doses of 160 mug did not alter brain catecholamines in mice, however, 6 hr after injection, brain dopamine and norepinephrine markedly decreased. 3) When metaraminol was injected into mice pretreated with reserpine of 6-hydroxydopamine, spontaneous motor activity tested by photo-cell counters method markedly increased and anti-6-hydroxydopamine activity of metaraminol was stronger than anti-reserpine. 4) Metaraminol completely antagonized ptosis and catalepsy induced by rerserpine. 5) Six hr after injection, anti-methamphetamine activity was observed.
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PMID:[Effect of beta-phenylethylamine derivatives on the central nervous system. III. Motor activity changes in mice due to the intracerebral administration of metaraminol]. 117 9

The effect of maprotiline (N-methyl-9, 10-ethanoanthracene-9 (10H)-propylamine) on animal behavior was investigated in mice and rats and compared with those of amitriptyline and imipramine. Maprotiline inhibited reserpine hypothermia in mice and tetrabenazine ptosis in rats, while it potentiated the effects of methamphetamine, L-DOPA and apomorphine in mice, in a similar manner to that of amitriptyline and imipramine. Maprotiline was more potent than anitriptyline and imipramine in antagonizing haloperidol-induced catalepsy as well as in suppressing muricide induced by either olfactory bulbectomy or delta-9-tetrahydrocannabinol in rats. Maprotiline potentiated anesthesia induced by thiopental or ether in mice to a lesser degree than did amitriptyline, and failed to counteract the lethal effect of physostigmine or oxotremorine tremor in mice, indicating that this drug has no central anti-cholinergic effect. Maprotiline markedly inhibited hyperemotionality of the rat with either septal lesions or olfactory bulb ablations, suggesting that it does have a tranquilizing effect. Inhibition of conditioned avoidance response of the rat in the shuttle box and reduction of methamphetamine group toxicity with maprotiline were similar to those with amitriptyline. Maprotiline exaggerated pentetrazol convulsion, decreased muscle tone and impaired coordinated motor activity in mice to a much lesser degree than amitriptyline and imipramine. LD50 of maprotiline was approximately twice that of imipramine and three times that of amitriptyline. These results indicate that maprotiline is a new type of antidepressant, has a low toxicity and shares both potent antidepressant and some tranquilizing effect, without possessing central anticholinergic action.
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PMID:[Behavior pharmacology of maprotiline, a new antidepressant]. 124 Aug 30


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