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At least 343 records · Page 19Linked to original sources
PubMed1984

Effects of the new oral angiotensin converting enzyme inhibitor 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-L-alanyl]-(1S,3S,5S)-2- azabicyclo[3.3.0]octane-3-carboxylic acid (Hoe 498) in essential hypertension.

In a dose titration study patients with mild to moderate essential hypertension were treated with increasing doses of 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-L-alanyl]-(1S,3S, 5S)-2-azabicyclo[3.3.0]octane-3-carboxylic acid (Hoe 498) (up to 8 mg daily) for 3 weeks. Hoe 498 was tolerated well. 9 out of 20 patients responded to 1 mg b.i.d., the blood pressure in a further 5 patients normalized with 2 mg b.i.d. Six patients did not respond to Hoe 498 treatment (4 mg b.i.d. in the last week) according to the criterion: recumbent diastolic blood pressure less than or equal to 90 mm Hg. But all 6 patients showed a clear decrease in blood pressure during treatment.

Adult↗
PubMed1983

Derivatives of 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane with hypotensive activity. I.

The synthesis of three series of glycinamides (IV), amides (V) and diamines (VI) starting from 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane is described. Some of compounds (IV), (V) and (VI) showed a moderate hypotensive activity in rats. Effects on heart rate in rats, infiltration anesthesia and antiarrhythmic activity in mice, as well as antiacetylcholine activity in vitro, are also reported.

Acetylcholine↗
PubMed1983

Derivatives of 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane with hypotensive activity. II.

The synthesis of a series of alkyl and aryl ureas (II) starting from 1,3,3-trimethyl-6-azabicyclo[3.2.1]octane is described. Some of these compounds showed a moderate hypotensive activity in rats. Effects on heart rate in rats, infiltration anesthesia and antiarrhythmic activity in mice, as well as antiacetylcholine activity in vitro, are also reported.

Acetylcholine↗
PubMed1981

Ester of 6-cis-dialkylamino-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-5-trans-ol with hypotensive and other activities.

Three series of esters of 6-cis-dialkylamino-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-5-trans-ol (dialkylamino = pyrrolidino, piperidino, morpholino) are described. A number of these compounds showed strong hypotensive activity in rats, as well as infiltration anesthesia and antiarrhythmic activity in mice. The lowering effects on heart rate in rats are also described.

Anesthetics, Local↗
PubMed1980

Derivatives of 1,2,3,3-tetramethyl-2-azabicyclo[2.2.2]octan-5-trans-ol with antiarrhythmic and other activities. III.

A new series of aliphatic and aromatic esters of 1,2,3,3-tetramethyl-2-azabicyclo[2.2.2]octan-5-trans-ol is described. A number of these compounds showed antiarrhythmic activity in guinea pigs and mice, as well as surface anesthesia in rabbits and infiltration anesthesia in mice, superior or similar to that of lidocaine. The circulatory, cardiac and respiratory effects in dogs and hens are also described.

Anesthetics, Local↗
PubMed1980

Derivatives of 1,2,3,3-tetramethyl-2-azabicyclo[2.2.2]octan-5-trans-ol with antiarrhythmic and other activities. IV.

A new series of aliphatic and aromatic amides of 5-trans-(3-aminopropoxy)-1,2,3,3-tetramethyl-2-azabicyclo[2.2.2] octane is described. A number of these compounds showed antiarrhythmic activity in guinea pigs and mice, as well as surface anesthesia in rabbits and infiltration anesthesia in mice, superior or similar to that of lidocaine. The circulatory, cardiac and respiratory effects in dogs and hens are also described.

Anesthetics, Local↗
PubMed1994

O-(2-dialkylaminoethyl)oximes of 5-(arylmethylene)-1,3,3-trimethyl-2-oxabicyclo [2.2.2]octan-6-ones with hypotensive, antiarrhythmic and other activities.

The synthesis of some O-(2-dialkylaminoethyl)oximes of 5-[(4-methoxy- or 4-methylthiophenyl)methylene]-1,3,3-trimethyl-2-oxabicyclo[2.2.2] octan-6-ones 5 by reaction of the corresponding oximes as sodium salts with the appropriate 2-chloroethyldialkylamine in dry ethanol solution is described. Some aminoethers 5 showed appreciable hypotensive and antiarrhythmic activities in rats, as well as a weak platelet antiaggregating activity in vitro and a moderate infiltration anesthesia in mice.

Anesthetics, Local↗
PubMed1993

Synthesis and opioid receptor affinity of bivalent ligands derived from 3,8-diazabicyclo(3.2.1)octanes.

A new series of bivalent ligands (2a-d), derived from the previously reported analgesic 3-cinnamyl-8-propionyl-3,8-diazabicyclo(3.2.1)octane (1a), has been synthesized and tested in vitro for their affinity towards opioid receptors and in vivo for their analgesic potency. None of the new compounds showed either appreciable affinity for opioid receptors or analgesic activity comparable to that of the model 1a.

Analgesics↗
PubMed1977

[Effect of exogenous superoxide dismutase and 1,4-diazobicyclo-(2,2,2,)-octane on the resistance of mice to acute oxygen poisoning].

Single injection to mice of a perified preparation of superoxide dismutase (1000 units, intravenously) combined with catalase (0.5 mg) or without it failed to protect from the toxic action of 100% oxygen under the pressure of 5 ata. 1,4-diazobicyclo (2.2.2) octane (6 mg, intraperitoneally) increased the preconvulsive survival period of mice under these conditions. The formation of single oxygen under hyperoxia in vivo is supposed.

Acute Disease↗
PubMed1996

LD50 value, phototoxicity and convulsion induction test of the new quinolone antibacterial agent (S)-10-[(S)-(8-amino-6-azaspiro[3,4]octan-6-yl)]-9-fluoro-2, 3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxyl ic acid hemihydrate in laboratory animals.

(S)-10-[(S)-(8-Amino-6-azaspiro[3,4]octan-6-yl)]-9-fluoro-2, 3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxyli c acid hemihydrate (CAS 151390-79-3, DV-7751a) a new quinolone antibacterial agent, was examined for LD50 value, phototoxicity and convulsion inducing potential in laboratory animals. A single oral administration of DV-7751a induced soft stool in rats at 1000 and 2000 mg/ kg and in monkeys at 250 mg/kg and vomiting in monkeys at 500 mg/kg or more. A single intravenous administration caused a decrease in locomotor activity, respiratory depression, convulsion, pulmonary edema and death in rats and mice. The LD50 values with oral administration were more than 2000 mg/ kg for rats and mice and more than 250 mg/kg for monkeys, and those with intravenous administration were 164.3 mg/kg for rats of both sexes at an injection rate of 2 ml/min, 118.8 mg/kg for male rats and 104 to 125 mg/kg for female rats at 0.5 ml/min, and 184.7 mg/kg for male mice and 187.4 mg/kg for female mice. DV-7751a showed very weak phototoxicity in mice after single oral administration of 600 mg/kg, followed by UVA irradiation, but no convulsion after oral administration of 200 or 1000 mg/kg in combination with 4-biphenylacetic acid at 400 mg/kg.

Administration, Oral↗
PubMed1996

One-month oral toxicity study of the new quinolone antibacterial agent (S)-10-[(S)-(8-amino-6-azaspiro[3,4]octan-6-yl)-9-fluoro-2,3-dihydro-3- methyl-7-oxo-7H-pyrido [1,2,3-de] [1,4] benzoxazine-6-carboxylic acid hemihydrate in rats and cynomolgus monkeys.

One-month oral toxicity of (S)-10-[(S)-(8-amino-6-azaspiro[3,4] octan-6-yl)]-9-fluoro-2,3-dihydro-3-methyl-7-oxo-7H-pyrido[1,2,3-de] [1,4]benzoxazine-6-carboxylic acid hemihydrate (CAS 151390-79-3, DV-7751a) a new quinolone antibacterial agent was investigated in Sprague-Dawley rats at doses of 12.5, 50, 200 and 800 mg/kg/d and in cynomolgus monkeys at 10, 30 and 100 mg/kg/d. Rats receiving 200 mg/ kg showed abnormal urine crystals, enhanced deposition of lipid in hepatocytes and exacerbation of osteochondrotic lesions in the femoral condyle. In addition, dosing at 800 mg/kg induced decrease in body weight gain and increased levels of serum alkaline phosphatase (ALP), cholinesterase, leucine aminopeptidase and total cholesterol. Monkeys receiving 100 mg/kg showed abnormal urine crystals and increases in serum glutamic oxaloacetic transaminase, glutamic pyruvic transaminase and ALP levels. The non-toxic doses of DV-7751a in rats and monkeys were 50 and 30 mg/kg, respectively, under the present experimental conditions.

Animals↗
PubMed1996

Synthesis of ethylammonium iodides of omega-dialkylaminoethyl ethers of 5-(arylmethylene)-1,3,3-trimethyl-2-oxabicyclo [2.2.2.] octan-6-hydroxyimines as potential cosmetic ingredients.

The synthesis of nine quaternary ammonium iodides derived from omega-dialkylaminoethyl ethers of 5-(arylmethylene)-1,3, 3-trimethyl-2-oxabicyclo[2.2.2]octan-6-hydroxyimines, as potential cosmetic ingredients, is described. They are routinely prepared starting from cineole aminoethers by reaction with iodoethane and their physics-chemical data are reported. These substances were studied for their UV absorption and three of these compounds were also submitted to microbiological assays on five test organisms. The substances have their UV absorption maxima at 284-321 nm, and one compound is active on Staphylococcus aureus, Streptococcus faecalis and Candida albicans. These preliminary findings seem to indicate that some of these compounds could be considered as potential UV sunscreens; one compound, having a moderate antimicrobial activity, could be considered a potential active compound in cosmetics as deodorants, toothpastes, mouthwashes and other oral care products.

Anti-Infective Agents↗
PubMedDate not supplied

Synthesis and anxiolytic activity of N-substituted cyclic imides N-[4-[(4-aryl)-1-piperazinyl]alkyl]-5,7-dioxabicyclo[2.2.2]octane-2, 3-dicarboximide.

The preparation of N-substituted cyclic imides N-[4-[(4-aryl)-1-piperazinyl]alkyl]-5,7-dioxabicyclo[2.2.2]octane- 2, 3-dicarboximides by condensation of N-(3-chloropropyl)- or N-(4-chlorobutyl)imides with appropriate amine has been described. One of compounds was tested in the Vogel's test and displayed an expected activity on CNS.

Animals↗
PubMed1996

[Catalytic properties of catalase in microemulsions of surface-active agents in octane].

The rate constants of H2O2 decomposition, interaction of catalase complex I with H2O2, and the effective rate constants of catalase inactivation during enzymatic catalysis (k(in)) were determined by transformation of complete kinetic curves of H2O2 decomposition by catalase in reversed micelles of Aerosol OT (AOT) in octane and aqueous solution. Effects of hydration of micelles and AOT, H2O2, and catalase concentrations in the micellar systems on each of three kinetic constants were investigated. Optimal conditions were found which provide for high operational stability and catalytic activity of catalase in micellar systems versus aqueous solutions. Stability of catalase enhances (decreased k(in)) in the presence of reduced glutathione and ethanol in AOT micelles. In reversed AOT micelles, catalase partially dissociates to subunits because their peroxidase activity was demonstrable in cumene hydroperoxide-dependent oxidation of tetramethylbenzidine. Catalase dissociation to monomers is significantly decreased in mixed micelles composed of AOT, Triton X-45, Triton X-100, or Tween-85 and octanol.

Catalase↗
PubMed1998

The heterocyclic substituted pyridine derivative (+/-)-2-(-3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429): a selective ligand at nicotinic acetylcholine receptors.

The present report describes in vitro studies demonstrating that the heterocyclic substituted pyridine compound (+/-)-2-(3-pyridinyl)-1-azabicyclo[2.2.2]octane (RJR-2429) is extremely potent in activating human muscle nicotine ACh receptor (nAChR) (EC50 = 59 +/- 17 nM; Emax = 110 +/- 09% vs. nicotine). RJR-2429 is markedly less potent in activating nAChRs in the clonal cell line PC12, with EC50 = 1100 +/- 230 nM and Emax = 85 +/- 20% when compared with nicotine. The activation of a putative alpha 3 beta 4-containing nAChR in PC12 by RJR-2429 reveals a potency intermediate between nicotine and epibatidine (EC50 of 20,000 nM for nicotine and 30 nM for epibatidine). Dose-response curves for agonist-induced ileum contraction indicate that RJR-2429 is equipotent with nicotine, having an EC30 of approximately 2 microM. RJR-2429 binds with high affinity to alpha 4 beta 2 receptor subtype (Ki = 1.0 +/- 0.3 nM), and chronic exposure results in significant up-regulation of the high-affinity [3H]nicotine binding sites. In addition, RJR-2429 does not activate nAChRs present in rat thalamic preparations but is a potent inhibitor of this receptor subtype. It antagonizes nicotine-stimulated ion flux in thalamic synaptosomes with an IC50 of 154 +/- 37 nM. It also is a potent partial agonist at nAChRs mediating dopamine release from rat synaptosomal preparations (EC50 = 2 +/- 1 nM; Emax = 40%; epibatidine and nicotine have EC50 values of 0.4 and 100 nM, respectively). A model for the structure-activity profile of RJR-2429, nicotine and epibatidine was derived by molecular forcefield and quantum mechanics calculations and may provide important clues for the development of ligands selective for nAChR subtypes as probes in the life sciences or as potential therapeutic tools.

Animals↗
PubMed1998

Thermobarostability of alpha-chymotrypsin in reversed micelles of aerosol OT in octane solvated by water-glycerol mixtures.

Thermostability of alpha-chymotrypsin at normal pressure in reversed micelles depends on both an effective surfactant solvation degree and glycerol content in the system. The difference in alpha-chymotrypsin stability in reversed micelles at various glycerol concentrations [up to 60% (v/v)] was more pronounced at high surfactant degrees of solvation, R >/= 16. After a 1-h incubation at 40 degrees C in "aqueous" reversed micelles (in the absence of glycerol), alpha-chymotrypsin retained only 1% of initial catalytic activity and 10, 22, 59, and 48% residual activity in glycerol-solvated micelles with 20, 30, 50, and 60% (v/v) glycerol, respectively. The explanation of the observed effects is given in the frames of micellar matrix structural order increasing in the presence of glycerol as a water-miscible cosolvent that leads to the decreasing mobility of the alpha-chymotrypsin molecule and, thus the increase of its stability. It was found that glycerol or hydrostatic pressure could be used to stabilize alpha-chymotrypsin in reversed micelles; a lower pressure is necessary to reach a given level of enzyme stability in the presence of glycerol.

Aerosols↗