Drugs online research references
Agents Actions. 1989 Apr;27(1-2):33-5.
Beta-adrenoceptor blocking drugs and calcium transport in isolated rat mast cells.
Drabikova K, Pecivova J, Nosal R.
Centre of Physiological Sciences, Slovak Academy of Sciences, Bratislava, Czechoslovakia.
The beta-adrenoceptor blocking (BAB) drugs exaprolol (EXA), metipranolol (MET) and propranolol (PRO) inhibited histamine liberation and degranulation from isolated rat mast cells stimulated with the calcium ionophore A23187. MET was the most and EXA the least active. Atenolol (ATE) had no effect. Inhibition by BAB drugs of secretion induced with A23187 was not accompanied by any change in 45Ca uptake. On the other hand, EXA, MET and PRO significantly decreased 45Ca uptake by mast cells stimulated with 48/80. The effect of BAB drugs on inhibition of A23187-induced secretion from isolated mast cells was dependent on the lipid solubility of the studied drugs.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2473626&dopt=Abstract
J Pharm Pharmacol. 1998 May;50(5):467-73.
The effect of a drug-delivery system consisting of soybean phosphatidyl choline and medium-chain monoacylglycerol on the intestinal permeability of hexarelin in the rat.
Fagerholm U, Sjostrom B, Sroka-Markovic J, Wijk A, Svensson M, Lennernas H.
Department of Pharmacy, University of Uppsala, Sweden.
The aim of this study was to investigate if the effective in-situ permeability (Peff) of a new growth hormone-releasing peptide, hexarelin, along rat intestine was enhanced by a lipid matrix drug-delivery system comprising a mixture of soybean phosphatidyl choline and medium-chain monoacylglycerol (PC-MG). The study was performed with and without a protease inhibitor, Pefabloc SC. To enable better understanding of the mechanism of action of this delivery system we also studied the uptake of a small hydrophilic molecule, atenolol. PC-MG at a concentration of 15 mmol L(-1) increased the jejunal Peff of hexarelin approximately 20-fold, both in the presence and absence of Pefabloc SC, whereas Peff was not increased in the ileum and colon. PC-MG had no effect on the jejunal, ileal and colonic Peff of atenolol. Complete recovery of the non-absorbable molecule PEG 4000 showed that functional intestinal viability was maintained in all experiments. Although the results obtained in this study are promising, pharmacokinetic and toxicological studies are required to investigate if this delivery system is a suitable and safe candidate for improving the oral bioavailability of hexarelin.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9643439&dopt=Abstract
Eur J Pharmacol. 1992 Jun 24;217(1):43-8.
The effect of adrenergic drugs on serotonin metabolism in the nucleus raphe dorsalis of the rat, studied by in vivo voltammetry.
Clement HW, Gemsa D, Wesemann W.
Department of Neurochemistry, Philipps University, Marburg/Lahn, Germany.
The serotonin (5-HT) and norepinephrine (NE) system participate in the control of behavioural functions. The experiments were aimed at the question whether the NE system of the locus coeruleus interferes with the 5-HT activity of the nucleus raphe dorsalis and of which receptors are possibly involved. The alpha 1- and beta-adrenoceptor agonists methoxamine and isoproterenol, as well as a high dose (600 micrograms/kg i.p.) of the alpha 2-adrenoceptor agonist clonidine, increased extraneuronal 5-hydroxyindoleacetic acid (5-HIAA) levels in the nucleus raphe dorsalis as measured by in vivo voltammetry. In contrast, a low dose (60 micrograms/kg i.p.) of clonidine and the alpha 1-, alpha 2- and beta-adrenoceptor antagonists, prazosin, piperoxane, and atenolol, reduced the 5-HIAA concentration. In the locus coeruleus, the origin of NE projections to the nucleus raphe dorsalis, clonidine decreased whereas piperoxane enhanced extracellular 3,4-dihydroxyphenylacetic acid (DOPAC), an index of NE metabolism in the locus coeruleus. The results suggest that 5-HT neurotransmission in the nucleus raphe dorsalis is stimulated by the NE system of the locus coeruleus and that adrenoceptor drugs may affect 5-HT neuronal activity in addition to NE neurotransmission.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1383006&dopt=Abstract
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