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Results for “Piperazines”

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At least 1,441 records · Page 80Linked to original sources
PubMed1978

[Bicyclic piperazine homologues XIV (1). Synthesis and analgesic activity of 3,8-diaza-bicyclo[3.2.1.] octane derivatives].

The synthesis of two new series of 3,8-diazabicyclo [3.2.1] octane derivatives is described. The first series includes some 3-(or 8)-allyl and 3-(or 8)-(3,3-dimethylallyl) derivatives of 3,8-diazabicyclo [3.2.1] octane and 3,8-diazabicyclo [3.2.1] octane-2-one. The second series includes some esters and carbamates of 3-(3-hydroxy-3-methyl)butyl-3,8-diazabicyclo [3.2.1] octane. Two new 3,8-diazabicyclo [3.2.1] octane derivatives structurally related to propoxyphene are also described. Some pharmacological data of these compounds are reported.

Analgesics↗
PubMed1977

[Bicyclic analogs of piperazine. XII. (1) - Synthesis of 3,8-diazabicyclo/3,2,1/octanes as potential antiparkinson agents].

As a part of research on 3,8-diazabicyclo [3,2,1] octanes, the Authors report on the synthesis of some amides of methyl, phenyl and cyclohexyltropic acid, potentially active as antiparkinson agents. Also reported is the synthesis of some compounds similar to two known drugs, Caramiphene and Cycrimine. These compounds differ from the said drugs in having a 3,8-diazabicyclo [3,2,1] octane as a basic moiety.

Antiparkinson Agents↗
PubMed1996

[The effect of piperazine analogs of aryloxyaminopropanol (IIIq and IIIb) on the occurrence of reperfusion dysrhythmias in an in vivo experiment on rats].

The present experimental study reports the beneficial effects of newly synthetized substances IIIq and IIIb in vivo. These aryloxyaminopropanol drugs have been shown to antagonize the contraction caused by calcium comparable to verapamil and flunarizine in the model of the isolated guinea pig terminal ileum. Effects of substances on both the incidence of arrhythmias during ischemia and the reperfusion period and mortality were investigated in the rat model ischemia-reperfusion injury. We can conclude that compound IIIq in a dose of 10(-6) mol/kg is effective in reducing the incidence of reperfusion-induced arrhythmias. Substance IIIb (10(-6) mol/kg) administered before ischemia was not able to suppress arrhythmias in the rat model of myocardial infarction and reperfusion.

Animals↗
PubMed1996

[Piperazine analogs of aryloxyaminopropanols and a study of their effects on a model of the isolated guinea pig ileum].

Seven compounds belonging to the group of aryloxyaminopropanols with carbamate substitution of the aromatic ring and with derivatives of N-phenylpiperazine in the lipophilic part were prepared by a well-tried method. Selected drugs were pharmacologically evaluated by in vitro experiments. Aryloxyaminopropanol drugs confirmed their anti-calcium activity on the intestinal model. Significant anti-calcium activity of agents IIIq and IIIb (pA2 = 6,83 +/- 1,47; 7, 12 +/- 1, 12 was comparable to that found for the standards verapamil and flunarizine. These compounds were selected for in vivo experiments and evaluated for their effect on reperfusion-induced arrhythmias in anaesthetized rats. Results of these evaluations are given in the next article.

Animals↗
PubMedDate not supplied

Structure-activity relationship in a series of new 1-(2-pyrimidinyl)piperazine derivatives with hypnotic activity.

Preparation, biological properties and QSAR of new derivatives of 1-[4-(2-pyrimidinyl)-1-piperazinyl]-1, 3-butandione (11-13, and 15-18) and 3-[4-(2-pirimidinyl)-1-piperazinyl]-3-oxopropanoate (20-22) exhibiting hypnotic activity in mice are reported. The best therapeutic indices (TI = LD50/ED50) 4.7 and 9.4 for po and ip administration, respectively, were found for 1-[4-(2-pyrimidinyl)-1-piperazinyl]-2-n-pentyl-1,3-butandione (15). QSAR studies showed that the biological activity grows initially with an increase in lipophilicity to drop dramatically for log P > 2.5.

Amphetamine↗
PubMed1996

Effect of (+/-)-(E)-1-(3-fluoro-6,11-dihydrodibenz[b,e]-oxepine-11 -yl)-4-(3-phenyl-2-propenyl)-piperazine dimaleate on cerebral vasospasm and impairment of cerebral circulation in subarachnoid hemorrhage model in rats.

A subarachnoid hemorrhage (SAH) model in rats was produced by the injection of homologous blood into the cisterna magna. Effects of AJ-3941 ((+/-)-(E)-1-(3-fluoro-6,11 -dihydrodibenz[b,e]-oxepine-11-yl)-4-(3-phenyl-2-propenyl)-p iperazine dimaleate, CAS 143110-70-7) on the development of cerebral vasospasm and the change of regional cerebral blood flow (rCBF) following SAH was investigated in this model. Cerebral vasospasm following SAH showed a biphasic pattern with an early phrase at 10 min and a late phrase on 1 day after blood injection. The physiological parameters (blood pressure, heart rate and blood gas contents) remained stable within the physiological range throughout the course of the experiment. AJ-3941 (0.01 mg/kg i.v. or 0.3 mg/kg p.o.) significantly prevented the development of late phase cerebral vasospasm. Cisternal injection of homologous blood significantly reduced rCBF immediately after the injection and the reduction lasted during the observation period (30 min). Reduction in rCBF after the injection of homologous blood was prevented by AJ-3941 (0.01 mg/kg i.v.). rCBF in AJ-3941-treated rats completely returned to the basal values after 30 min. The present suggest that AJ-3941 may be useful in the prevention of late spasm and in the improvement of cerebral circulation impaired with SAH.

Animals↗
PubMed1997

Cerebrovascular selectivity and vasospasmolytic action of the novel calcium antagonist (+/-)-(E)-1-(3-fluoro-6, 11-dihydrodibenz[b,e]oxepin-11-yl)-4-(3-phenyl-2-propenyl)-piperazine dimaleate in isolated cerebral arteries of the rabbit and dog.

The cerebrovascular selectivity and vasospasmolytic action of AJ-3941 ((+/-)-(E)-1-(3-fluoro-6, 11-dihydrodibenz[b,e]oxepin-11-yl)-4-(3-phenyl-2-propenyl)-p iperazine dimaleate. CAS 143110-70-7), a new calcium antagonist, were studied in isolated rabbit and dog arterial preparations. In rabbit arterial ring preparations, AJ-3941 dose-dependently inhibited the contractions of various arteries caused by high K(+)-depolarization (high K+) and prostaglandin F2 alpha (PG). The inhibitory potency of AJ-3941 varied in different arteries, in descending order as follows: high K+: basilar > coronary > femoral > renal > mesenteric artery, PG: basilar > coronary > > femoral and renal artery. The median inhibitory concentration (IC50) in the basilar artery was over 40 times lower than that in the mesenteric or femoral artery for which the weakest inhibition in the examined arteries was observed. This selective action of AJ-3941 for cerebral artery was also observed in the frontal and middle cerebral arteries of dogs. The selectivity for the rabbit basilar artery was higher than those of flunarizine and nicardipine. Additionally, the contractile response of the rabbit basilar artery induced by phorbol 12,13-dibutyrate (PDBu), an activator of protein kinase C (PKC), was greater than those of the arteries examined such as the coronary, femoral and mesenteric arteries. The response in the basilar artery was greatly reduced in Ca(2+)-free medium, while this was not the case in other arteries. AJ-3941 as well as H-7, an inhibitor of PKC, potently inhibited PDBu-induced contractile response in the basilar artery in the presence, but not in the absence of Ca2+ in the medium, whereas the existing calcium antagonists, diltiazem and nicardipine, did not inhibit the contractile response in both conditions. These results suggest that the PKC-dependent system which is mediated by influx of extracellular Ca2+ profoundly contributes to the contraction of the cerebral artery and that the cerebroselective-vasodilating effect of AJ-3941 may depend, at least partly, on the inhibition of the PKC-mediated contractile response. In rabbit basilar arteries, AJ-3941 caused a dose-dependent inhibition of the contraction induced by various vasospasmogens, such as endothelin-1 (ET), arachidonic acid, 15-hydroperoxy-eicosatetraenoic acid and the thromboxane A2-mimetic U-46619. Furthermore, when isolated basilar arteries of the dog were perfused intraluminally with AJ-3941 at the concentration that inhibits high K(+)- or PG-induced contraction in the rabbit basilar artery, AJ-3941 effectively antagonized the vasospasm induced by extraluminal application of PG or ET. However, when flunarizine, nicardipine, diltiazem or verapamil was used for intraluminal perfusion of the same preparations, none of these drugs exerted spasmolytic effect. These results indicate that AJ-3941 has cerebrovascular selective-vasospasmolytic action, and consequently is thought to be effective in cerebrovascular disorder such as vasospasm following subarachnoid hemorrhage.

Animals↗