Physiological Selectivity
Mostrando 13-24 de 96 artigos, teses e dissertações.
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13. A model of the glycine receptor deduced from Brownian dynamics studies
We have developed a three-dimensional model of the α1 homomeric glycine receptor by using Brownian dynamics simulations to account for its observed physiological properties. The model channel contains a large external vestibule and a shallow internal vestibule, connected by a narrow, cylindrical selectivity filter. Three rings of charged residues from the p
The National Academy of Sciences.
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14. Differential Metal Selectivity and Gene Expression of Two Zinc Transporters from Rice1
Zinc is an essential mineral for a wide variety of physiological and biochemical processes. To understand zinc transport in cereals, we identified putative zinc transporters in gene databases. Three full-length cDNAs were identified and characterized from rice (Oryza sativa). Two of the cDNAs partially complemented a yeast (Saccharomyces cerevisiae) mutant d
The American Society for Plant Biologists.
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15. Vasopressin potentiates mineralocorticoid selectivity by stimulating 11 beta hydroxysteroid deshydrogenase in rat collecting duct.
Arginine vasopressin (AVP) and corticosteroid hormones are involved in sodium reabsorption regulation in the renal collecting duct. Synergy between AVP and aldosterone has been well documented, although its mechanism remains unclear. Both aldosterone and glucocorticoid hormones bind to the mineralocorticoid receptor (MR), and mineralocorticoid selectivity de
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16. N-Methyl-d-aspartate (NMDA) Receptor NR2 Subunit Selectivity of a Series of Novel Piperazine-2,3-dicarboxylate Derivatives: Preferential Blockade of Extrasynaptic NMDA Receptors in the Rat Hippocampal CA3-CA1 Synapse
N-Methyl-d-aspartate (NMDA) receptor antagonists that are highly selective for specific NMDA receptor 2 (NR2) subunits have several potential therapeutic applications; however, to date, only NR2B-selective antagonists have been described. Whereas most glutamate binding site antagonists display a common pattern of NR2 selectivity, NR2A > NR2B > NR2C > NR2D (h
The American Society for Pharmacology and Experimental Therapeutics.
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17. Revised estimates of human cochlear tuning from otoacoustic and behavioral measurements
We develop an objective, noninvasive method for determining the frequency selectivity of cochlear tuning at low and moderate sound levels. Applicable in humans at frequencies of 1 kHz and above, the method is based on the measurement of stimulus-frequency otoacoustic emissions and, unlike previous noninvasive physiological methods, does not depend on the fre
The National Academy of Sciences.
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18. K+/Na+ Selectivity in Toy Cation Binding Site Models Is Determined by the ‘Host’
The macroscopic ion-selective behavior of K+ channels is mediated by a multitude of physiological factors. However, considering the carbonyl-lined binding site of a conductive K+ channel as a canonical eightfold coordinated construct can be useful in understanding the principles that correlate the channel's structure with its function. We probe the effects o
The Biophysical Society.
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19. Single anion-selective channels in basolateral membrane of a mammalian tight epithelium.
Basolateral membrane chloride permeability of surface cells from rabbit urinary bladder epithelium was studied using the patch-clamp technique. Two types of anion-selective channel were observed. One channel type showed inward rectification and had a conductance of 64 pS at-50 mV when bathed symmetrically by saline solution containing 150 mM chloride; the ot
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20. Conformationally restricted analogs of somatostatin with high mu-opiate receptor specificity.
A series of cyclic, conformationally restricted analogs of somatostatin have been prepared and tested for their ability to inhibit the binding of [3H]naloxone and [D-Ala2, D-Leu5] [3H]enkephalin to rat brain membranes. The most potent analog, D-Phe-Cys-Tyr-D-Trp-Lys-Thr-Pen-Thr-NH2 where Pen is penicillamine in [D-Phe5, Cys6, Tyr7, D-Trp8, Pen11]somatostatin
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21. Pronounced pharmacologic deficits in M2 muscarinic acetylcholine receptor knockout mice
Members of the muscarinic acetylcholine receptor family (M1–M5) are known to be involved in a great number of important central and peripheral physiological and pathophysiological processes. Because of the overlapping expression patterns of the M1–M5 muscarinic receptor subtypes and the lack of ligands endowed with sufficient subtype selectivity, th
The National Academy of Sciences.
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22. Definitive Assignment of Proton Selectivity and Attoampere Unitary Current to the M2 Ion Channel Protein of Influenza A Virus
The viral ion channel protein M2 supports the transit of influenza virus and its glycoproteins through acidic compartments of the cell. M2 conducts endosomal protons into the virion to initiate uncoating and, by equilibrating the pH at trans-Golgi membranes, preserves the native conformation of acid-sensitive viral hemagglutinin. The exceptionally low conduc
American Society for Microbiology.
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23. Synthesis and biological activities of potent peptidomimetics selective for somatostatin receptor subtype 2
A series of nonpeptide somatostatin agonists which bind selectively and with high affinity to somatostatin receptor subtype 2 (sst2) have been synthesized. One of these compounds, L-054,522, binds to human sst2 with an apparent dissociation constant of 0.01 nM and at least 3,000-fold selectivity when evaluated against the other somatostatin receptors. L-054,
The National Academy of Sciences.
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24. Multiple opioid receptors in endotoxic shock: evidence for delta involvement and mu-delta interactions in vivo.
The use of selective delta and mu opioid antagonists has provided evidence that delta opioid receptors within the brain mediate the endogenous opioid component of endotoxic shock hypotension. The selectivity of these delta and mu antagonists was demonstrated by their differing effects upon morphine analgesia and endotoxic hypotension. The mu antagonist beta-