European Journal of Pharmacology
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The influence of smooth muscle content and orientation in dissected human pregnant myometrial strips on contractility measurements
European Journal of Pharmacology 738:245 (2014)This study examined the hypothesis that the force generated by myometrial strips from pregnant women is influenced by the smooth muscle content and fibre orientation of the strips and that correcting for these structural variables will provide a more accurate measure of contractility. Myom...
Unique pharmacology of heteromeric α7β2 nicotinic acetylcholine receptors expressed in Xenopus laevis oocytes.
We have compared the pharmacological properties of recombinant homomeric α7 and heteromeric α7β2 nicotinic acetylcholine receptors in order to reveal the pharmacological consequences of β2 subunit incorporation into the pentamer. The non-selective agonist epibatidine did not distinguish α7β2 from α7...
Prevention of aortic calcification by etidronate in the renal failure rat model.
Our recent clinical study indicated that etidronate may inhibit the progression of aortic calcification in hemodialysis patients. To determine whether etidronate inhibits aortic calcification in renal failure rats, renal failure was induced by subtotal nephrectomy, in which 5/6 of the kidneys were r...
Mycophenolate mofetil prevents autoimmune glomerulonephritis and alterations of intrarenal adrenomedullin in rats
We studied the effects of mycophenolate mofetil, a specific inhibitor of inosine monophosphate dehydrogenase, on the mercuric chloride induced autoimmune glomerulonephritis in Brown Norway rats and also on the renal contents of adrenomedullin. In the rats with autoimmune glomerulonephritis, plasma a...
Physiological modulation of GABA(A) receptor plasticity by progesterone metabolites.
The possible functional relation between changes in brain and plasma concentrations of neurosteroids and the plasticity of gamma-aminobutyric acid type A (GABA(A)) receptors in the brain during pregnancy and after delivery was investigated in rats. The concentrations in the cerebral cortex and plasm...
SB-236057, a selective 5-HT1B receptor inverse agonist, blocks the 5-HT human terminal autoreceptor.
A novel compound, SB-236057 (1'-ethyl-5-(2'-methyl-4'-(5-methyl-1,3,4-oxadiazol-2-yl)biphenyl- 4-carbonyl)-2,3,6,7-tetrahydrospiro[furo[2,3-f]indole-3,4'-piperid ine]) has been shown to have high affinity for human 5-hydroxytryptamine1B (5-HT1B) receptors (pKi = 8.2) and displays over 75 or more-fol...
Effects of anticonvulsive drugs on pentylenetetrazol kindling and long-term potentiation in freely moving rats.
Drugs with anticonvulsive properties and different mechanisms of action were compared for their influence on long-term potentiation and pentylenetetrazol kindling in freely moving animals. Rats were chronically implanted with a stimulation electrode in the angular bundle and a recording electrode in...
Inhibition of ligand-gated cation-selective channels by tamoxifen.
We have investigated the action of tamoxifen and the related derivative toremifene on ligand-gated cationic nicotinic acetylcholine and 5-HT3 receptor channels. Tamoxifen and toremifene both inhibited cationic currents of adult-type human muscle nicotinic acetylcholine receptors expressed in Xenopus...
The response of rat colonic mucosa to 5-hydroxytryptamine in health and following restraint stress.
The present study characterized the rat colonic secretory response to 5-hydroxytryptamine (5-HT) and determined alterations in this response following stress. 5-HT stimulated rat colonic short-circuit current in a concentration-dependent fashion (pD2 = 5.19). This response was subject to desensitiza...
Evaluation of PD 154075, a tachykinin NK1 receptor antagonist, in a rat model of postoperative pain.
PD 154075 ([(2-benzofuran)-CH2OCO]-(R)-alpha-MeTrp-(S)-NHCH(CH3) Ph) is a selective tachykinin NK1 receptor antagonist. Its effect on development and maintenance of thermal and mechanical hypersensitivity was examined in a rat model of surgical pain. When administered 30 min before surgery, PD 154075...