نتایج جستجو برای: مدل mk
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MK801 (MK), an N-methyl-D-aspartate (NMDA) receptor antagonist, attenuates tolerance to spinal opioids. Whether this applies to other G-protein-coupled receptor systems is unknown. This study examines the effects of continuous spinal MK on tolerance to the antinociceptive effect of continuous spinal infusion of the alpha-2 agonist ST91 (ST). Intrathecal (i.t.) infusion pumps were implanted in r...
The receptor tyrosine kinase c-Met is an attractive target for therapeutic blockade in cancer. Here, we describe MK-2461, a novel ATP-competitive multitargeted inhibitor of activated c-Met. MK-2461 inhibited in vitro phosphorylation of a peptide substrate recognized by wild-type or oncogenic c-Met kinases (N1100Y, Y1230C, Y1230H, Y1235D, and M1250T) with IC(50) values of 0.4 to 2.5 nmol/L. In c...
Erythropoietin (EPO) has been well known as a hematopoietic cytokine over the past decades. However, recent reports have demonstrated that EPO plays a neuroprotective role in the central nervous system, and EPO has been considered as a therapeutic target in neurodegenerative diseases such as ischemic stroke. Despite the neuroprotective effect of EPO, clinical trials have shown its unexpected si...
A graph G is k-linked if G has at least 2k vertices, and for every sequence x1, x2, . . . , xk, y1, y2, . . . , yk of distinct vertices, G contains k vertex-disjoint paths P1, P2, . . . , Pk such that Pi joins xi and yi for i = 1, 2, . . . , k. Moreover, the above defined k-linked graphG is k-linked modulo (m1,m2, . . . ,mk) if, in addition, for any ktuple (d1, d2, . . . , dk) of natural number...
We introduce a new method for preparing subpopulations of guinea pig megakaryocytes (MK). MK, partially purified by a density gradient, were separated according to size by sedimentation, starting as a monolayer, in an albumin gradient at unit gravity. Twenty-two fractions were collected. Cells were cytocentrifuged, ploidy was assessed by microdensitometry, and small MK were identified with anti...
Uraemic patients frequently demonstrate tendencies towards life-threatening bleeding. Reduced platelet counts and their functional immaturity seem to be caused, among other things, by disorders in the system of marrow megakaryocytes. The aim of the study was a histomorphometric evaluation of marrow megakaryocytes in the course of experimental uraemia in rats. Uraemia was induced by means of rig...
MK-212 (1 x 10(-7)M -- 1 x 10(-5)M) produced dose-dependent contractions of guinea pig ileum, taenia coil and rat fundus strip. The responses to MK-212 in all three preparations were blocked competitively by cyproheptadine (1 x 10(-8)M) a 5-HT receptor antagonist. Mepyramine (1 x 10(-8)M)-H1 receptor antagonist also inhibited competitively the responses of guinea pig ileum and taenia coli to MK...
We examined the effect of 1-amino-3,5-dimethyladamantane (memantine) and (+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (MK-801) on the inhibition of [(3)H]MK-801 binding to crude synaptic membranes of rat forebrains in the absence or presence of Ca(2+). Ca(2+) decreased the potency of memantine to inhibit [(3)H]MK-801 binding. The effect of Ca(2+) was apparently competitive w...
the effects of cholecystokinin (cck) receptor antagonists on hypothermia induced by cocaine or morphine have been studied in mice. in the present work, subcutaneous (sc) injection of cocaine (50-150 mg/kg) or morphine (125-500 mg/kg) induced hypothermia in mice. administration of ccka receptor antagonist mk-329 (0.5-1.5 mg/kg), cckb receptor antagonist l-365, 260 (0.5-1.5 mgl kg) and cck recept...
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