Changes in the brain kappa-opioid receptor levels of rats in withdrawal from physical dependence upon butorphanol

Changes in kappa-opioid receptor levels have been implicated in the development of physical dependence upon and withdrawal from the mixed agonist-antagonist opioid, butorphanol. Immunoblotting analysis was performed to determine the levels of kappa- and mu-opioid receptors in brain regions of rats in withdrawal from dependence upon butorphanol or morphine. Physical dependence was induced by a 72 h i.c.v. infusion with either butorphanol or morphine (26 nmol/microl/h). Withdrawal was subsequently precipitated by i.c.v. challenge with naloxone (48 nmol/5 microl/rat), administered 2 h following cessation of butorphanol or morphine infusion. Immunoblotting analysis of kappa-opioid receptors from butorphanol-withdrawal rats showed significant increases in 11 of 21 brain regions examined, including the nucleus accumbens, amygdala, dorsomedial hypothalamus, hypothalamus, paraventricular thalamus, thalamus, presubiculum, and locus coeruleus, when compared with saline treated, non-dependent controls. In addition, significant reductions were found in the hippocampus and in cortical brain regions, including the parietal cortex and temporal cortex from butorphanol-withdrawal rats. These findings contrasted with those from morphine-withdrawal rats, in which the only changes noted were increases in the thalamus and paraventricular thalamus. Changes in the levels of the mu-opioid receptor protein were observed in 11 of 21 brain regions examined in morphine-withdrawal rats, but only in three of 21 in butorphanol-withdrawal rats. These results implicate a substantive and largely unique role for kappa-opioid receptors in mediation of the development of physical dependence upon, and the expression of withdrawal from, butorphanol, as opposed to the prototypical opioid analgesic, morphine.     

Hydrolysis of Carbonates,Thiocarbonates, Carbamates,and Carboxylic Esters of α-Naphthol, β-Naphthol,and p-Nitrophenol by Human,Rat, and Mouse Liver Carboxylesterases

Thirty carbonates, thiocarbonates, carbamates, and carboxylic esters of -naphthol, -naphthol, and p-nitrophenol were synthesized and tested as substrates for liver carboxylesterases from the crude microsomal fractions of human and mouse, and purified isozymes, hydrolases A and B, from rat liver microsomes. The carbonates, thiocarbonates, and carboxylic esters of -naphthol were cleaved more rapidly than the corresponding -naphthol isomers by the mammalian liver esterases. -Naphthyl esters of acetic, propionic, and butyric acids were among the best substrates tested for these enzymes. The majority of the substrates was consistently hydrolyzed at higher rates by hydrolase B compared with hydrolase A, although the Michaelis–Menten constant (K _m) values of selected substrates differed widely with these two isozymes. Malathion was a 15-fold better substrate for hydrolase B than for hydrolase A. Compared with the corresponding carboxylates, the carbonate moiety of - and -naphthol and p-nitrophenol lowered the specific activities of the enzymes by about fivefold but improved stability under basic conditions. The optimum pH of mouse liver esterase with the acetate, methylcarbonate, and ethylthiocarbonate of -naphthol was between pH 7.0 and pH 7.6. Human and mouse liver microsomal esterase activities were about five orders of magnitude lower than the esterase activities of purified rat liver hydrolase B. A relationship between the catalytic activity of the enzymes and the lipophilicity of the naphthyl substrates indicated that (i) in the - and -naphthyl carbonate series, an inverse relationship between enzyme activity and lipophilicity of the substrates was observed, whereas (ii) in the -naphthyl carboxylate series, an increase in enzyme activity with increasing lipophilicity of the substrates up to a log P value of about 4.0 was observed, after which the enzyme activity decreased.     

The normal width of anterior hip synovial recess in children

To establish the diagnostic criteria for hip joint effusion, the normal width of the anterior hip synovial recess in children and the difference between both hips of the same child were examined in this study. Eight kindergarten schools were randomly selected for study in Kaohsiung City. The width of anterior hip synovial recess of 1,568 hips in 784 children (421 boys, 363 girls) was measured by ultrasound scanner with 7.5-MHz linear probe. The age of children ranged from 2.5 to 6.6 years old. During measurement, the children were put in supine position with hips and knees in extension and patella facing up. The results revealed that the mean width of the anterior synovial recess was 7.29+/-1.15 mm. Linear correlation of the width of synovial recess to age and height was disclosed and expressed as follows: width (millimeters) equal to 6.52+0.013x age (months), or width (millimeters) equal to 3.97+0.030x height (centimeters). The mean difference between both hips of the same child was 0.611+/-0.523 mm, and the difference was independent from the factors of age, gender, height, or weight (p>0.05). Ninety-five percent of the differences should be < or =1.46 mm, so that if the difference between hips is >1.46 mm, hip joint effusion should be suspected.     

Randomized trial of two intravenous schedules of the topoisomerase I inhibitor liposomal lurtotecan in women with relapsed epithelial ovarian cancer: a trial of the national cancer institute of Canada clinical trials group.

PURPOSE: Liposomal lurtotecan (OSI-211) is a liposomal formulation of the water-soluble topoisomerase I inhibitor lurtotecan (GI147211), which demonstrated superior levels of activity compared with topotecan in preclinical models. We studied two schedules of OSI-211 in a randomized design in relapsed ovarian cancer to identify the more promising of the two schedules for further study. PATIENTS AND METHODS: Eligible patients had measurable epithelial ovarian, fallopian, or primary peritoneal cancer that was recurrent after one or two prior regimens of chemotherapy. Patients were randomly assigned to receive either arm A (OSI-211 1.8 mg/m(2)/d administered by 30-minute intravenous infusion on days 1, 2, and 3 every 3 weeks) or arm B (OSI-211 2.4 mg/m(2)/d administered by 30-minute intravenous infusion on days 1 and 8 every 3 weeks). The primary outcome measure was objective response, which was confirmed by independent radiologic review, and a pick the winner statistical design was used to identify the schedule most likely to be superior. RESULTS: Eighty-one patients were randomized between October 2000 and September 2001. The hematologic toxic effects were greater on arm A than on arm B (grade 4 neutropenia, 51% v 22%, respectively), as was febrile neutropenia (26% v 2.4%, respectively). Of the 80 eligible patients, eight patients (10%) had objective responses; six responders (15.4%; 95% CI, 6% to 30%) were in arm A and two responders (4.9%; 95% CI, 1% to 17%) were in arm B. CONCLUSION: The OSI-211 daily for 3 days intravenous schedule met the statistical criteria to be declared the winner in terms of objective response. This schedule was also associated with more myelosuppression than the schedule of OSI-211 administered in arm B.     

Pretreatment of coir lignocellulose for preparation of a porous coir–polyurethane composite with high oil adsorption capacity

In this present work, different treatment methods of coir biomass were investigated to improve the oil sorption capacity. The treated coir material was then used to fabricate an efficient porous coir–polyurethane composite sorbent by incorporating coir into a polyurethane matrix. The new composite possessed an open cell structure with high porosity and high oil sorption efficiency. The suitable technical parameters of the coir treatment process were selected as: hot water treatment at 170 °C for 120 minutes. After treatment under this suitable condition, treated coconut fiber exhibited an oil adsorption capacity of 4.1 g g⁻¹, with an increase of 78.3% compared to that of the original coconut fiber. Furthermore, the application of the as-fabricated porous composite sorbent for oil treatment was examined under various conditions. It was observed that the oil uptake capacity of the new composite sorbent was high, up to 15.2 g g⁻¹ when 20% treated coir material with a particle size of 1 mm was added into the polyurethane matrix. Several advantages of the new porous composite sorbent obtained from coir biomass and polyurethane such as low cost, being eco-friendly, ready availability and high buoyancy make it an efficient sorbent material for oil spill treatment.

An efficient porous coir–polyurethane composite with high porosity and high oil sorption efficiency has been successfully prepared by incorporating coir into a polyurethane matrix.     

Impact of blinking on ocular surface and tear film parameters

Purpose

To investigate the influence of blinking on tear film parameters, ocular surface characteristics, and dry eye symptomology.