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Page 1
Anticonvulsant, but not antiepileptic, action of valproate on audiogenic seizures in metaphit-treated rats.
Stanojlović OP, Hrncić DR, Zivanović DP, Susić VT. Stanojlović OP, et al. Clin Exp Pharmacol Physiol. 2007 Oct;34(10):1010-5. doi: 10.1111/j.1440-1681.2007.04681.x. Clin Exp Pharmacol Physiol. 2007. PMID: 17714087
The blocking effects of valproate (2-propylpentanoic acid), a standard anti-epileptic drug, on metaphit (1-[1-(3-isothiocyanatophenyl)-cyclohexyl]-piperidine)-induced audiogenic seizures as a model of generalized, reflex audiogenic epilepsy in adult Wistar male rats were s …
The blocking effects of valproate (2-propylpentanoic acid), a standard anti-epileptic drug, on metaphit (1-[1-(3-isothiocyanatophenyl)-cy …
In vivo labelling of the neuronal dopamine uptake complex in the mouse striatum by [3H]GBR 12783.
Vaugeois JM, Bonnet JJ, Costentin J. Vaugeois JM, et al. Eur J Pharmacol. 1992 Jan 7;210(1):77-84. doi: 10.1016/0014-2999(92)90654-m. Eur J Pharmacol. 1992. PMID: 1350989
Specific binding was prevented by various dopamine uptake blockers, pyrovalerone, GBR 13069, GBR 12783, N-[1-2-benzo(b)thiophenyl)cyclohexyl] piperidine, cocaine, methylphenidate and was inhibited in a stereoselective manner by the enantiomers of nomifensine. ...
Specific binding was prevented by various dopamine uptake blockers, pyrovalerone, GBR 13069, GBR 12783, N-[1-2-benzo(b)thiophenyl)cyclohe …
Synthesis of New Potential Lipophilic Co-Drugs of 2-Chloro-2'-deoxyadenosine (Cladribine, 2-CdA, Mavenclad®, Leustatin®) and 6-Azauridine (z6 U) with Valproic Acid.
Knies C, Reuter H, Hammerbacher K, Bender E, Bonaterra GA, Kinscherf R, Rosemeyer H. Knies C, et al. Chem Biodivers. 2019 Mar;16(3):e1800497. doi: 10.1002/cbdv.201800497. Epub 2019 Feb 25. Chem Biodivers. 2019. PMID: 30614625
All products were characterized by (1) H- and (13) C-NMR spectroscopy and ESI mass spectrometry. The structure of the by-product 6 (N-cyclohexyl-N-(cyclohexylcarbamoyl)-2-propylpentanamide), formed upon valproylation of cladribine in the presence of N,N-dimethylaminopyridi …
All products were characterized by (1) H- and (13) C-NMR spectroscopy and ESI mass spectrometry. The structure of the by-product 6 (N-cyc …
NH3 permeation through the apical membrane of MDCK cells is via a lipid pathway.
Golchini K, Kurtz I. Golchini K, et al. Am J Physiol. 1988 Jul;255(1 Pt 2):F135-41. doi: 10.1152/ajprenal.1988.255.1.F135. Am J Physiol. 1988. PMID: 2839988
In comparison, apical membrane permeability at 37 degrees C to the weak acids, valeric acid and acetic acid, were 1.39 +/- 0.11 x 10(-2) cm/s (n = 4) and 6.93 +/- 0.11 x 10(-3) cm/s (n = 4), respectively. ...Heptanol (15 mM) significantly decreased the activation energy fo …
In comparison, apical membrane permeability at 37 degrees C to the weak acids, valeric acid and acetic acid, were 1.39 +/- 0.11 x 10( …
Resorcinarenes with 2-benzimidazolone bridges: self-aggregation, self-assembled dimeric capsules, and guest encapsulation.
Ebbing MH, Villa MJ, Valpuesta JM, Prados P, de Mendoza J. Ebbing MH, et al. Proc Natl Acad Sci U S A. 2002 Apr 16;99(8):4962-6. doi: 10.1073/pnas.072652599. Proc Natl Acad Sci U S A. 2002. PMID: 11959947 Free PMC article.
Longer dimeric carboxylic acids or larger substrates, like 2-adamantyl azide or cyclohexylcarbodiimide, do not encapsulate, but mixtures of a long and a short carboxylic acid (i.e., propionic-adamantyl or propionic-cyclohexyl) yield pairwise complexes....
Longer dimeric carboxylic acids or larger substrates, like 2-adamantyl azide or cyclohexylcarbodiimide, do not encapsulate, but mixtures of …
Anticonvulsant activity of novel derivatives of 2- and 3-piperidinecarboxylic acid in mice and rats.
Hinko CN, Crider AM, Kliem MA, Steinmiller CL, Seo TH, Ho B, Venkatarangan P, el-Assadi AA, Chang H, Burns CM, Tietz EI, Andersen PH, Klitgaard H. Hinko CN, et al. Neuropharmacology. 1996;35(12):1721-35. doi: 10.1016/s0028-3908(96)00105-0. Neuropharmacology. 1996. PMID: 9076751
Since preliminary data indicated that benzylamide derivatives of 2-PC displace [3H]1-[1-(2-thienyl)-cyclohexyl]piperidine (TCP) binding to the phencyclidine (PCP) site of the N-methyl-D-aspartate (NMDA) receptor in the micromolar range and such low affinity uncompetitive a …
Since preliminary data indicated that benzylamide derivatives of 2-PC displace [3H]1-[1-(2-thienyl)-cyclohexyl]piperidine (TCP) bindi …
N-methyl-D-aspartate receptor regulation of uncompetitive antagonist binding in rat brain membranes: kinetic analysis.
Bonhaus DW, McNamara JO. Bonhaus DW, et al. Mol Pharmacol. 1988 Sep;34(3):250-5. Mol Pharmacol. 1988. PMID: 2843744
To determine the mechanism of this regulation, we examined the kinetics of the binding of the radiolabeled uncompetitive antagonist [3H]N-(1-[thienyl]cyclohexyl) piperidine (TCP). Increasing concentrations of NMDA receptor agonists produced dose-dependent increases in the …
To determine the mechanism of this regulation, we examined the kinetics of the binding of the radiolabeled uncompetitive antagonist [3H]N-(1 …
Agents combining thromboxane receptor antagonism with thromboxane synthase inhibition: [[[2-(1H-imidazol-1-yl)ethylidene]amino]oxy]alkanoic acids.
Cozzi P, Giordani A, Menichincheri M, Pillan A, Pinciroli V, Rossi A, Tonani R, Volpi D, Tamburin M, Ferrario R, et al. Cozzi P, et al. J Med Chem. 1994 Oct 14;37(21):3588-604. doi: 10.1021/jm00047a016. J Med Chem. 1994. PMID: 7932586
Two close congeners of the latter series, (+/-)-(E)-5-[[[1-cyclohexyl-2-(1H-imidazol-1-yl)-3- phenylpropylidene]amino]oxy]pentanoic acid 23c and its p-fluorophenyl analog 23m, inhibited TxB2 production in vitro, in rat whole blood during clotting, with IC50 of 0.06 and 0.3 …
Two close congeners of the latter series, (+/-)-(E)-5-[[[1-cyclohexyl-2-(1H-imidazol-1-yl)-3- phenylpropylidene]amino]oxy]pentanoic a …
Interaction of Delta sleep-inducing peptide and valproate on metaphit audiogenic seizure model in rats.
Stanojlović O, Hrncić D, Rasić A, Loncar-Stevanović H, Djuric D, Susić V. Stanojlović O, et al. Cell Mol Neurobiol. 2007 Nov;27(7):923-32. doi: 10.1007/s10571-007-9222-5. Epub 2007 Oct 24. Cell Mol Neurobiol. 2007. PMID: 17957464
Effects of valproate (VPA), a conventional antiepileptic drug and natural delta sleep-inducing peptide (DSIP) on metaphit (1-[1-(3-isothiocyanatophenyl)-cyclohexyl]-piperidine)-induced audiogenic reflex epilepsy were studied. ...
Effects of valproate (VPA), a conventional antiepileptic drug and natural delta sleep-inducing peptide (DSIP) on metaphit (1-[1-(3-isothiocy …
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