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Development of a new physicochemical model for brain penetration and its application to the design of centrally acting H2 receptor histamine antagonists.
TLDR
A good correlation was found between the logarithms of the equilibrium brain/blood concentration ratios in the rat and the partition parameter, delta log P, defined as log P (1-octanol/water)-log P (cyclohexane/water), which suggests that brain penetration might be improved by reducing overall hydrogen-bonding ability. Expand
L-trans-pyrrolidine-2,4-dicarboxylate and cis-1-aminocyclobutane-1,3-dicarboxylate behave as transportable, competitive inhibitors of the high-affinity glutamate transporters.
TLDR
Results support an action of L-trans-PDC and cis-ACBD consistent with that of being competitive substrates rather than non-transportable blockers of the plasma membrane L-glutamate uptake system. Expand
Pharmacological studies with SK&F 93944 (temelastine), a novel histamine H1‐receptor antagonist with negligible ability to penetrate the central nervous system
TLDR
SK&F 93944 may have an advantage over classical histamine H1‐receptor antagonists in that it is likely to be devoid of untoward effects on the central nervous system. Expand
Association of c‐fos mRNA expression and excitotoxicity in primary cultures of mouse neocortical and cerebellar neurons
TLDR
The results suggest that the Q240/30 c‐fos mRNA ratio may be used as a predictive index for excitotoxic neuronal death, provide information on the identity of the receptor subtype mediating excittoxicity in different brain cell types, and aid in establishing the role of excitOToxicity during the development of neurons in vitro. Expand
Characterization of the 1H-cyclopentapyrimidine-2,4(1H,3H)-dione derivative (S)-CPW399 as a novel, potent, and subtype-selective AMPA receptor full agonist with partial desensitization properties.
TLDR
(S)-CPW399 (2b) appears to be a weakly desensitizing, full agonist at AMPA receptors and therefore represents a new pharmacological tool to investigate the role ofAMPA receptors in excitotoxicity and their molecular mechanisms of Desensitization. Expand
Comparison of the cardiovascular effects of the novel 5-HT(1B/1D) receptor agonist, SB 209509 (VML251), and sumatriptan in dogs.
TLDR
Data indicate that SB 209509 is a potent 5-HT(1B/1D)-receptor agonist that is rapidly absorbed from the duodenum that is long lasting and selective for the carotid vascular bed. Expand
Differential Changes in the Content of Amino Acid Neurotransmitters in Discrete Regions of the Rat Brain Prior to the Onset and During the Course of Homocysteine‐Induced Seizures
TLDR
Changes in amino acid concentrations were investigated in selected regions of rat brain prior to the onset and during the course of epileptiform seizures induced by l‐homocysteine, with the hippocampus exhibiting a dramatic increase after seizure onset. Expand
Zolantidine (SK&F 95282) is a potent selective brain‐penetrating histamine H2‐receptor antagonist
TLDR
Zolantidine is characterized as a potent selective brain‐penetrating H2‐receptor antagonist, and will be a valuable pharmacological tool for investigating possible physiological and pathological roles for histamine in the central nervous system. Expand
Mutual Inhibition Kinetic Analysis of γ‐Aminobutyric Acid, Taurine, and β‐Alanine High‐Affinity Transport into Neurons and Astrocytes: Evidence for Similarity Between the Taurine and β‐Alanine
TLDR
The similarity between the results obtained for β‐alanine and taurine uptake in addition to their competitive mode of mutual inhibition strongly suggest that these compounds share a common carrier in neurons and astrocytes and that neither amino acid in either cell type is transported appreciably, if at all, by the GABA carrier. Expand
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