Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “Cyclohexanols”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 505 records · Page 28Linked to original sources
PubMed1978

[Therapeutic study on ambroxol in chronic bronchopulmonary diseases (author's transl)].

The clinical activity of trans-4-[(2-amino-3,5-dibromo-benzyl)-amino]-cyclohexanol-hydrochloride (ambroxol, NA 872) as well as its influence on lung function was examined in a total of 63 patients (34 suffering from silicosis, 28 from chronic obstructive bronchitis and 1 from cryptococcosis). Additionally, the content of phospholipids was controlled in the sputum of the patient group. It was shown that the activity of ambroxol was better in the silicosis group than in the bronchitis group. The cause was discussed. Presumably the twofold site of action in the silicosis group (secretolysis and surfactant stimulation) might be the reason for this.

Ambroxol↗
PubMed1978

[Clinical experience with ambroxol syrup (author's transl)].

In an open trial trans-4-[(2-amino-3,5-dibromo-benzyl)-amino]-cyclohexanol hydrochloride (ambroxol, NA 872) in the form of ambroxol syrup was given to non-hospitalised patients suffering from acute and chronic bronchitis. A marked reduction in coughing and dyspnoea as well as an improvement in expectoration was apparent. The maximum effect was reached on the third day of treatment. The effect can be maintained by consistent prolongation of the therapy. There were no side effects.

Administration, Oral↗
PubMed1978

[Results of a clinical trial with ambroxol as to postoperative therapy of bronchitis (author's transl)].

The clinical testing of trans-4-[(2-amino-3,5-dibromo-benzyl)amino]cyclohexanol-hydrochloride (ambroxol, NA 872) in surgical patients was carried out over a period of 7 days. Regular application of 60 mg/day showed a clear improvement in subjective symptoms, particularly in cases of bronchitic syndrome. In some patients improvement could be demonstrated objectively by means of sputum viscosimetry. The clinical effect is principally one of facilitation of expectoration and fluidification of mucus, which often prior to therapy is rather viscous. This leads to a favourable influence of the post-operative treatment period. As a rule the substance is well-tolerated. The recommended dose of the drug for the average treatment is 2 ampoules/day i.v. (30 mg) and a single to twice daily inhalation of 2 ml (15 mg) for 5--7 days post-operatively.

Aged↗
PubMedDate not supplied

[The Homogeneous immunocofactor method of determining insulin].

An immunocofactor quantitative method of measuring insulin in solution was developed. The method uses antibody competitive binding of free and NAD labeled insulin. The NAD-insulin conjugate was obtained by covalent binding of the C(6)-aminogroup modified cofactor with insulin by means of soluble carbodiimide. To determine the NAD-insulin conjugate, which was not bound with antibodies, in the presence of antibodies and free insulin, an enzymic system of the cofactor regeneration with conjugated substrates of horse liver alcohol dehydrogenase, cyclohexanol and p-nitroso-N,N-dimethyl aniline, was employed. The sensitivity of insulin assay was about 5.10(-7) M.

Animals↗
PubMed1983

Pharmacological characterization of the acetylcholine transport system in purified Torpedo electric organ synaptic vesicles.

A wide variety of pharmacologically active compounds was surveyed for effects on active transport of [3H]acetylcholine by synaptic vesicles isolated from the electric organ of Torpedo californica. In over 80 compounds tested, inhibitors of a wide range of potencies were found. The most potent inhibitor was 2-(4-phenylpiperidino)cyclohexanol (AH5183), which half-inhibited transport at 40 nM. This compound had been predicted by Marshall [Br. J. Pharmacol. 38:503-516 (1970)] to block acetylcholine storage by vesicles in vivo. The synaptic vesicle active transport system is shown to be pharmacologically distinct from other cholinergic systems. The site of action of AH5183 and other potent inhibitors is not certain, but the possibility of trivial action on the vesicle ATPase or a vesicle proton gradient was eliminated. The results constitute new evidence supporting vesicle exocytosis as the source of evoked acetylcholine release by nerve terminals. AH5183 appears to be the prototype for a new family of anticholinergics. The possibility that some drugs that exhibit secondary anticholinergic effects act in part by antagonizing acetylcholine storage is discussed.

Acetylcholine↗
PubMed1981

Influence of ambroxol on the bronchopulmonary level of antibiotics.

Antibiotic levels in bronchopulmonary tissue following oral administration of ampicillin, erythromycin and amoxycillin dosed 50 mg/dg were compared with those obtained by the same treatments n0 mg/dg p.o of trans-4-[(2-amino-3,5-dibromo-benzyl)amino]cyclohexanol (ambroxol, Mucosolvan) in several groups of rats. The addition of ambroxol was correlated with an increase of 234% in the pulmonary average concentration of ampicillin, 27% in that of erythromycin 27% in that of amoxycillin; the statistical evaluation of these differences resulted in less than 0.05 in each case. It may be concluded that ambroxol, through a mechanism still unclear, can increase the antibiotic levels in the lungs of the rat.

Ambroxol↗
PubMed1994

The role of endogenous adenosine in a poststimulation increase in the acetylcholine content of a sympathetic ganglion.

Previous experiments showed that exposure of sympathetic ganglia to exogenous adenosine increased acetylcholine (ACh) content and its subsequent release. This effect was not mediated through extracellular adenosine receptors, but at an intracellular site following its uptake through nitrobenzylthioinosine (NBTI)-resistant nucleoside transporters. We postulated that endogenous adenosine may play a role in modulating synaptic transmission in the superior cervical ganglion. The present study tested whether adenosine is involved in the activation of ACh synthesis that occurs during a rest period following prolonged presynaptic tetanic activity. Conditioning of ganglia with high-frequency stimulation (15 Hz) for 45 min followed by a 15 min rest increased their ACh content by 45%. The appearance of this "rebound ACh" showed sensitivity to nucleoside transport inhibitors; it was prevented by dipyridamole, but not by NBTI or meclonazepam, and it was reduced in the presence of RO 11-3624, suggesting an involvement of NBTI-resistant transporters. The effect of dipyridamole was specific for the synthesis of rebound ACh in that it did not inhibit ACh release or ACh synthesis during stimulation. The inhibitory action of dipyridamole on the synthesis of rebound ACh was not evident if it was present only during the tetanic stimulation but it was if dipyridamole was present during the rest period following it, suggesting that adenosine's presence after tetanic stimulation is of importance. This conclusion was strengthened by experiments showing that the presence of cyclopentyltheophylline, an antagonist at inhibitory adenosine receptors, increased ACh output evoked by test stimulation immediately following tetanic activity, as if endogenous adenosine was available at that time to activate the adenosine receptors that inhibit transmitter release. ACh release from conditioned ganglia was 44% greater than that from the controls. However, the rebound ACh was not mobilized in the presence of 2-(4-phenylpiperidino)cyclohexanol (vesamicol), a vesicular ACh transporter inhibitor. These results suggest that endogenous adenosine released after tetanic stimulation activates ACh synthesis, which results in an increase of ganglionic ACh that is available for subsequent mobilization and release.

Acetylcholine↗
PubMed1993

The effect of cigarette smoking on the indexes of immunity and acute phase reaction in subjects with occupational exposure to organic solvents.

The study was carried out in 156 men, including 49 nonsmokers and 47 smokers who had never been exposed to chemicals, 19 nonsmokers exposed to organic solvents, and 41 smokers exposed to organic solvents. The results of toxicological analysis of air in the working place carried out in the range depending on the type of solvents used in the process of lacquering of steel cans and on the data obtained from the producer showed that the solvents contained benzene, toluene, xylene and their derivatives partly hydrogenated, paraffin hydrocarbons, oleins, naphthenes (components of painter's naphtha), monohydric and polyhydric alcohols (butanol, cyclohexanol, butyloglycol), esters (ethylglycol acetate, butyl acetate) and ketones (methyl isobutyl ketone, cyclohexanone). Measured benzene concentrations varied from 0 to 370 mg x m-3 (0 to 116 ppm), with arithmetic mean annual averages of about 100 mg x m-3 (31 ppm) in the late 1960's and less than 50 mg x m-3 (16 ppm) in the 1970's. In the 1980's values for the TWA were 0-38 mg x m-3 (0-12 ppm) with arithmetic mean averages of about 19 mg x m-3 (6 ppm) and for the level of benzene 0-351 mg x m-3 (0-110 ppm), with arithmetic mean annual averages of about 48 mg x m-3 (15 ppm). Phenol concentration in the urine of the workers in groups was 7.9 +/- 3.5; 10.0 +/- 5.8; 16.8 +/- 6.2 and 18.4 +/- 9.7 mg x 1(-1) respectively. Hippuric acid concentration in the urine of the workers in groups was 496 +/- 326, 538 +/- 341, 982 +/- 420 and 1107 +/- 507 mg x 1(-1) respectively. The parameters of immunity and proteins acute phase reaction were determined, measuring the count of T, B, and "non-T, non-B" circulating lymphocytes, the concentration of immunoglobulins, lysozyme, C3c, C4, alpha 1-acid glycoprotein, haptoglobulin and ceruloplasmin in serum. The results of the presented study suggest the role of cigarette smoking as a co-factor in the immunological changes brought out by occupational exposure to organic solvents. This phenomenon is reflected in the changes of IgA, IgD, IgG, IgM and lysozyme in the serum, and number of circulating T cells.

Adolescent↗
PubMed1995

[Effect of cigarette smoking on T and NK cell count in blood of persons occupationally exposed to organic solvents].

The studies covered 139 men including two control groups: 40 nonsmokers and 41 smokers occupationally exposed to organic solvents. The results of toxicological analysiss of the air revealed the presence of benzene, toluene, xylene and their hydrogenated derivatives, paraffin hydrocarbons, oleins, naphthenes, alcohols (butanol, cyclohexanol), esters (ethylglycol acetate, butyl acetate) and ketones methyl isobutyl ketone, cyclohexanon). Absolute number of lymphocytes, T lymphocytes (CD 3+), T-helper (CD 4+), T-suppressor (CD 8+) and NK-cells (CD +16) were determined in the peripheral blood by indirect immunofluorescence test. A decreased number of lymphocytes and NK-cells as well as an increased number of T-suppressor lymphocytes were noted. That contributed to the decrease of T-helper/T-suppressor ratio in the subjects occupationally exposed to organic solvents. Cigarette smoking enhanced this disorder.

Adolescent↗
PubMed1996

The effect of cigarettes smoking on the blood counts of T and NK cells in subjects with occupational exposure to organic solvents.

The study was carried out in a population of 139 men, divided into two control groups: 40 non-smokers and 39 smokers not exposed to chemical compounds, and two groups exposed to them: 19 non-smokers and 41 cigarette smokers with occupational contact with organic solvents. The results of toxicological analyses of air and chromatographic analyses of solvents demonstrated the presence of benzene, toluene, xylene and their partly hydrogenated derivatives, paraffin hydrocarbons, oleins, naphthenes (components of painter's naphtha), monohydric and polyhydric alcohols (butanol, cyclohexanol, butylene glycol) esters (ethyleneglycol acetate, butyl acetate) and ketones (methylisobutyl ketone, cyclohexanone). In the time of the studies the TWA values for benzene were 0 to 38 mg x m-3 (0 to 12 ppm), with arithmetic mean averages of about 19 mg x m-3 (6 ppm) and for the level of benzene 0-351 mg x m-3 (0-110 ppm) with arithmetic mean annual averages of about 48 mg x m-3 (15 ppm). Mean phenol concentration in the urine of the workers in groups I, II, III and IV respectively was: 7.9 +/- 3.5; 10.0 +/- 5.8; 16.8 +/- 6.2 and 18.4 +/- 9.7 mg x l-1. Hippuric acid concentration in the urine of the workers in groups I to IV was: 496 +/- 326, 538 +/- 341, 982 +/- 420 and 1107 +/- 507 mg x l-1 respectively. The absolute counts were determined of T-cells (CD 3+), T-helper (CD 4+), T-suppressor (CD 8+) cells and natural killer (NK) cells (CD 16+) in the peripheral blood by indirect immunofluorescence. In the subjects with occupational exposure to organic solvents the counts of T-cells and NK-cells were reduced, and the number of T-suppressor cells was raised which resulted in a decrease of the T-helper/T-suppressor ratio. These changes were more pronounced in cigarette smokers. The assessment of the immunotoxic effect of organic solvents during occupational exposure should take into consideration the possibility of a synergistic action with tobacco and may be of practical use for monitoring the toxic effect of organic solvents on the lymphocyte system.

Adult↗
PubMed1994

Sensory physiological basis for attraction in mosquitoes.

Hematophagous insects use air-borne chemical cues to guide them to resources such as blood-meal hosts, plants, and oviposition sites. Research that combines behavioral and electrophysiological approaches to the study of how insects find these resources can result in useful information about what chemical signals a mosquito can detect and at what airborne concentrations such compounds are effective. Such studies have helped clarify the role of lactic acid, ammonia, carbon dioxide, octenol, phenols, temperature, and humidity in the attraction of mosquitoes, tsetse flies, and ticks to blood-meal hosts. Egg raft pheromone, indoles, cresols, methyl cyclohexanol, 2-butoxy ethanol, and fatty acid esters have been examined with respect to oviposition site location and selection. Plant volatiles have received less attention but electrophysiological responses to terpenes and green plant volatiles have been observed. Information from studies of this type can be useful in the design of both attractants and more effective repellents.

Animals↗
PubMed1997

New radiopaque polyHEMA-based hydrogel particles.

New iodine-containing polymeric hydrogel particles were prepared by suspension radical copolymerization of 2-hydroxyethyl methacrylate (HEMA), 3-(methacryloylamidoacetamido)-2,4,6-triiodobenzoic acid (MABA) and ethylene dimethacrylate (EDMA) in an aqueous medium using azobisisobutyronitrile as an initiator and magnesium hydroxide as a suspension stabilizer. To impart porosity to the product, cyclohexanol and 1-dodecanol were added as inert diluents to the polymerization mixture. Particles containing 27 wt % iodine produced radiopacity sufficient to observe a clearly visible X-ray image. The equilibrium swelling behavior of the particles in water was characterized. Swelling of the particles dramatically increased by converting the acid groups of MABA into their Na+ form. The more MABA the copolymer particle contain, the higher is their swelling in the Na+ form.

Biocompatible Materials↗
PubMed1998

Evaluation of hair root analysis for acute phencyclidine poisoning and behavior of phencyclidine metabolites in rat hair root.

We evaluated the usefulness of hair root analysis to diagnose acute phencyclidine (PCP) poisoning. Male rats were i.p. administered acute poisonous doses (80, 100 and 120 mg/kg) of PCP hydrochloride and the hair roots were plucked out with hair nippers at certain times after administration. The hair root samples were extracted with methanol/HCl. After evaporation of the solvent, the residue was derivatized with N,O-bis(trimethylsilyl) acetamide and analyzed with GC/MS. PCP was detected at high concentrations (up to 181.7 ng/mg) from all samples. The peak concentrations at every dose were observed at 6 h. The concentrations of PCP in the rat hair roots increased dose-dependently in the range of the doses. 1-(1-Phenylcyclohexyl)-4-hydroxypiperidine (PCHP) and trans-1-phenyl-1(4'-hydroxypiperidino)-4-cyclohexanol (t-PCPdiol) were also detected from 5 and 15 min to 48 h after administration, respectively. It is concluded that hair root is a useful specimen for the diagnosis of acute PCP poisoning because PCP, PCHP and t-PCPdiol are detected very soon after administration and a large amount of them is retained in hair root for a long time. PCHP was found from the early stage in hair roots and its concentration was higher than that of t-PCPdiol for 6 h. However, the concentration of t-PCPdiol became higher than that of PCHP after 6 h. These phenomena could be explained by the time lag of production of the primary (PCHP) and the secondary metabolite (PCPdiol).

Acute Disease↗
PubMed2000

Evidence of the dual mechanisms of action of venlafaxine.

BACKGROUND: Indirect evidence suggests that the antidepressant venlafaxine hydrochloride selectively inhibits serotonin (5-HT) uptake at low doses, whereas at high doses, it inhibits both 5-HT and norepinephrine (NE) uptake. We hypothesized that, in vivo, both high and low doses would inhibit the 5-HT uptake of platelets but that the higher dose would differentially blunt the pressor response to tyramine, a marker for NE uptake. METHODS: Healthy male volunteers aged 18 to 45 years received either 75 mg or 375 mg of venlafaxine hydrochloride per day, the 5-HT uptake inhibitor sertraline hydrochloride (50 mg/d), or the NE uptake inhibitor maprotiline hydrochloride (150 mg/d) (n = 8 for each of 4 treatment groups). Changes in platelet 5-HT uptake and the pressor response to intravenous tyramine were assessed following the initial dose and after 1 and 2 weeks of drug administration. RESULTS: Platelet 5-HT uptake was inhibited by venlafaxine across the dose range and by sertraline but not maprotiline. Inhibition was competitive, related to increases in affinity and not related to capacity. Steady-state drug levels were associated with a 5-HT uptake inhibition of 87% or more in subjects taking venlafaxine or sertraline. The pressor response to tyramine differentially distinguished maprotiline from sertraline and the low dose of venlafaxine but not from the high dose of venlafaxine. CONCLUSION: This study provides the first in vivo evidence in healthy humans that both 5-HT uptake and NE uptake inhibition are mechanisms of action sequentially engaged by venlafaxine over its clinically relevant dose range.

Adolescent↗