Search results for "Locke"
showing 10 items of 332 documents
Mechanism of vascular relaxation by thaligrisine
2000
Abstract In the present study we examine the mechanism by which thaligrisine, a bisbenzyltetrahydroisoquinoline alkaloid, inhibits the contractile response of vascular smooth muscle. The work includes functional studies on rat isolated aorta and tail artery precontracted with noradrenaline or KCl. In other experiments rat aorta was precontracted by caffeine in the presence or absence of extracellular Ca 2 +. In order to assess whether thaligrisine interacts directly with calcium channel binding sites or with α-adrenoceptors we examined the effect of the alkaloid on [ 3 H]-(+)- cis diltiazem, [ 3 H]-nitrendipine and [ 3 H]-prazosin binding to cerebral cortical membranes. The functional studi…
Arginine-rich peptides are blockers of VR-1 channels with analgesic activity
2000
Vanilloid receptors (VRs) play a fundamental role in the transduction of peripheral tissue injury and/or inflammation responses. Molecules that antagonize VR channel activity may act as selective and potent analgesics. We report that synthetic arginine-rich hexapeptides block heterologously expressed VR-1 channels with submicromolar efficacy in a weak voltage-dependent manner, consistent with a binding site located near/at the entryway of the aqueous pore. Dynorphins, natural arginine-rich peptides, also blocked VR-1 activity with micromolar affinity. Notably, synthetic and natural arginine-rich peptides attenuated the ocular irritation produced by topical capsaicin application onto the eye…
Role for NK1 and NK2 receptors in the motor activity in mouse colon
2007
The present study examined the effects induced by endogenous and exogenous activation of NK(1) and NK(2) receptors on the mechanical activity of mouse proximal colon. Experiments were performed in vitro recording the changes in intraluminal pressure from isolated colonic segments. Electrical field stimulation in the presence of atropine and guanethidine produced a small relaxation, followed by nonadrenergic noncholinergic (NANC) contraction. SR140333, NK(1) receptor antagonist, or SR48968, NK(2) receptor antagonist, significantly reduced the contraction, although SR48968 appeared more efficacious. The co-administration of SR140333 and SR48968 virtually abolished the NANC contraction. [Sar(9…
Non-adrenergic non-cholinergic nerve-mediated inhibitory control of pigeon oesophageal muscle.
1996
Pigeon oesophageal smooth muscle in vitro has spontaneous electromechanical activity. In the presence of atropine and guanethidine, electrical field stimulation evokes a transient TTX-sensitive response comprising inhibition of electric bursting activity and muscular relaxation. This NANC inhibitory response was analysed using the K+ channel blockers TEA and apamin, TEA perfusion (0.1-5 mM) induced a concentration-dependent reduction in amplitude of EFS-evoked relaxation. Responses to higher stimulation frequencies were more sensitive to TEA than those to lower ones. The maximum reduction in amplitude (29% of control) was obtained on 30 Hz EFS evoked responses during 5 mM TEA perfusion. In …
Transmural myocardial ischaemia complicating recovery after dobutamine-atropine stress echocardiography in patients with non-significant coronary art…
2011
In the proposed selection of cases, traditional imaging is integrated with contemporary diagnostic tools available in the cath-lab to navigate the potential mechanisms underlying a very rare complication occurring in the recovery phase of dobutamine-atropine stress echocardiography. The data, collected in a time frame of nearly 15 years, provide interesting elements to possibly evolve from speculative considerations to plausible confirmation of the candidate pathophysiological mechanism mediating the occurrence of transmural myocardial ischaemia after beta-blockers administration.
Arginine vasopressin, via activation of post-junctional V1 receptors, induces contractile effects in mouse distal colon
2013
The aim of this study was to analyze whether arginine vasopressin (AVP) may be considered a modulator of intestinal motility. In this view, we evaluated, in vitro, the effects induced by exogenous administration of AVP on the contractility of mouse distal colon, the subtype(s) of receptor(s) activated and the action mechanism. Isometric recordings were performed on longitudinal and circular muscle strips of mouse distal colon. AVP (0.001 nM-100 nM) caused concentration-dependent contractile effects only on the longitudinal muscle, antagonized by the V1 receptor antagonist, V-1880. AVP-induced effect was not modified by tetrodotoxin, atropine and indomethacin. Contractile response to AVP was…
Mode and mechanism of neurotensin action in rat proximal colon
1997
Abstract This study examined the mechanism of action of neurotensin on intraluminal pressure in rat proximal colon. The direct and indirect contractile response to neurotensin (100 nM) was abolished in Ca 2+ -free solution, and was antagonized by nifedipine (1–5–10 nM) and potentiated by Bay K 8644 (methyl 1,4-dihydro-2,6-dimethyl-3-nitro-4-(2-trifluoromethylphenyl)-pyridine-5-carboxylate) (10–100–1000 nM). Neurotensin, in the presence of nifedipine (10 nM) and atropine (1 μM), induced a tetrodotoxin-insensitive inhibitory effect, which was antagonized by SR 48692 (2[(1-(7-chloro-4-quinolinyl)-5-(2,6-dimethoxy-phenyl)pyrazol-3-yl) carbonyl amino]tricyclo (3.3.1.1. 3.7 ) decan-2-carboxylic a…
La voie des idées, de Descartes à Hume
2015
International audience; Lorsque Descartes fait de la connaissance de l'esprit humain la principale tâche de la philosophie, il lui applique l'idée moderne de la science comme connaissance certaine et évidente. Durant les 150 ans qui suivront, aucun penseur ne reniera cette étincelle cartésienne. Dans son sillage mais aussi contre elle, dans le ciel de la philosophie apparaît une constellation de penseurs de premier ordre : Pascal, Hobbes, Spinoza, Malebranche, Leibniz, Locke, Berkeley, Hume. La recherche philosophique accompagnant la "révolution scientifique" commencée avec Galilée s'engage alors dans "la voie des idées". C'est donc sur cette voie que Pierre Guenancia nous entraîne, soulign…
Hypertension treatment in patients with sleep apnea from the European Sleep Apnea Database (ESADA) cohort - towards precision medicine.
2022
We recruited 5,970 patients with hypertension with obstructive sleep apnea (OSA) on current antihypertensive treatment from the European Sleep Apnea Database (ESADA) cohort. The group was subdivided into those receiving monotherapy (n = 3,594) and those receiving dual combined therapy (n = 2,376). We studied how major OSA confounders like age, gender, and body mass index as well as the degree of sleep apnea modified office systolic and diastolic blood pressure. Beta-blockers alone or in combination with a diuretic were compared with other antihypertensive drug classes. Monotherapy with beta-blocker was associated with lower systolic blood pressure, particularly in non-obese middle-aged male…
Role of calcium in E-selectin induced phenotype of T84 colon carcinoma cells
2003
The adhesion of cancer cells to the endothelium during the metastatic process involves the interaction of specific cell-cell adhesion receptors on the cell surface. E-selectin on endothelial cells and sialyl Lewis X carbohydrate component on tumor cells are mainly implicated in the adhesion of colon carcinoma cells to the endothelium of target organ. In this paper we show that binding of E-selectin to T84 colon tumor cells causes approximately a twofold increase in intracellular calcium concentration. In particular, using two inhibitors of receptor operated calcium channels, CAI and SK&F 96365, we present evidences that the augmentation in cytoplasmic calcium originates from ionic influx fr…