Drugs online research references
Eur J Pharmacol. 1994 Jul 15;268(2):257-62.
Characteristics of [3H]mepyramine binding in DDT1MF-2 cells: evidence for high affinity binding to a functional histamine H1 receptor.
Dickenson JM, Hill SJ.
Department of Physiology and Pharmacology, Medical School, Queen's Medical Centre, Nottingham, UK.
The binding characteristics of [3H]mepyramine to histamine H1 receptors in the smooth muscle cell line, DDT1MF-2, have been investigated. Competition binding experiments produced dissociation constants (Ki) for mepyramine, (+)-chlorpheniramine, and promethazine of 3.4 nM, 2.6 nM and 0.66 nM, respectively. Saturation binding using [3H]mepyramine produced a Kd of 2.1 nM and a Bmax of 47 fmol/mg protein. These data suggest that a high-affinity [3H]mepyramine binding site can be detected with the characteristics of the "classical" histamine H1 receptor. The low-affinity [3H]mepyramine binding site reported previously [Mitsuhashi, M. and Payan, D.G. (1988) J. Cell. Physiol. 134, 367-375] is predominantly to a secondary [3H]mepyramine site. The "low affinity" or secondary [3H]mepyramine binding site on DDT1MF-2 cells is insensitive to quinine (10 microM) and is therefore distinct from the [3H]mepyramine binding protein found in rat liver.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7957647&dopt=Abstract
Ma Zui Xue Za Zhi. 1993 Sep;31(3):157-64.
[Intravenous midazolam for sedation in epidural anesthesia]
[Article in Chinese]
Chau SW, Chen CD, Yip WH, Hsu TL, Yu KL, Chang HC, Tseng CK.
Department of Anesthesiology, Kaohsiung Medical College.
30 cases receiving epidural anesthesia for lower extremities and abdominal surgery were selected in this study. Their physical status and average age were ASA I or II and 41 +/- 10.0 years old. Premedication included intramuscular injection of pethidine, atropine and promethazine. Epidural anesthesia was accomplished with 15 ml 2% lidocaine with epinephrine (1:80,000). After the stabilization of vital signs, the patients were put asleep by 0.1 mg/kg of midazolam intravenously. They were then evaluated by the sedative, cardiovascular, respiratory and recovery effects of intravenous midazolam in epidural anesthesia. The results were as follows: The patients receiving IV midazolam averagely fell asleep in 61.6 +/- 20.5 seconds and maintained asleep for 55.4 +/- 12.7 minutes. Pain on injection was not noted in these cases. Cardiovascular parameters revealed midazolam with general depression on systolic pressure (17.4 +/- 7.3%), diastolic pressure (13.4 +/- 8.4%), mean arterial pressure (12.7 +/- 7.0%), heart rate (10.9 +/- 7.2%), stroke volume (13.7 +/- 8.9%) and cardiac output (18.4 +/- 7.0%) respectively. The peak depression reached around 10 minutes after drug administration. Respiratory parameters dropped with SaO2 (1.1 +/- 1.6%) and respiratory rate (9.7 +/- 5.7%) and fell into trough after 5 minutes of drug administration. Although all the above parameters measured were statistically significant, they were of no clinical importance that required further management. No case had delirium, anxiety and vomiting in the recovery period. Conclusively, patients receiving epidural anesthesia with supplement of intravenous midazolam provides a good sedative effect. Clinically, there was less severe untowards reaction either in cardiovascular or respiratory systems. Smooth and stable recovery was also noted.(ABSTRACT TRUNCATED AT 250 WORDS)
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7968337&dopt=Abstract
Biol Pharm Bull. 1994 Mar;17(3):419-22.
Effect of cumene hydroperoxide on lipid peroxidation in cultured rat hepatocytes supplemented with eicosapentaenoic acid.
Furuno K, Sugihara N.
Faculty of Pharmacy and Pharmaceutical Sciences, Fukuyama University, Hiroshima, Japan.
The present study was undertaken to examine whether the oxidative effect of organic hydroperoxide on cultured rat hepatocytes is enhanced by eicosapentaenoic acid (EPA). The cells were pretreated with 0.8 mM EPA which was complexed to bovine serum albumin (EPA-BSA) for 4 h, and then challenged to cumene hydroperoxide (CMHP). By the addition of CMHP to the cell culture, lipid peroxidation estimated as production of malondialdehyde (MDA) was provoked to a much greater extent in the EPA-loaded hepatocytes than in the non-loaded cells. The CMHP treatment also resulted in more severe cell injury in association with the decrease in intracellular levels of glutathione and protein thiols in the EPA-loaded cells as compared with results in the non-loaded cells. The addition of antioxidants such as N,N'-diphenyl-p-phenylenediamine (DPPD), promethazine and gamma-tocopherol to the culture medium prevented the CMHP-induced oxidative injury effectively for the EPA-loaded cells but had little effect for the non-loaded cells. The potency of other unsaturated fatty acids with different numbers of double bonds in enhancing the CMHP-induced lipid peroxidation and injury was also examined. The deleterious effects of CMHP were little affected by unsaturated fatty acids with one or two double bonds but were markedly intensified by those with more than 4 double bonds. These data showed that the supplementation with highly unsaturated fatty acids makes the cells susceptible to the drug-induced oxidative stress.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8019509&dopt=Abstract
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