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Potent and selective inhibition of nitric oxide-sensitive guanylyl cyclase by 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one.
ODQ is the first inhibitor that acts selectively at the level of a physiological NO "receptor" and, as such, is likely to prove useful for investigating the function of the cGMP pathway in NO signal transduction. Expand
NNC-711, a novel potent and selective gamma-aminobutyric acid uptake inhibitor: pharmacological characterization.
Following acute (3-h) in vivo pretreatment with NNC-711, behavioral tolerance developed to its motor impairing side effects (inhibition of traction, rotarod or exploratory locomotor activity) without corresponding tolerance to the anticonvulsant effects. Expand
Cholinergic mediation of the discriminative stimulus properties of clozapine
The results may indicate that the discriminative stimulus effects of CLZ primarily involve antagonism of central muscarinic acetylcholine receptors. Expand
(R)‐N‐[4,4‐Bis(3‐Methyl‐2‐Thienyl)but‐3‐en‐1‐yl]Nipecotic Acid Binds with High Affinity to the Brain γ‐Aminobutyric Acid Uptake Carrier
It is concluded that NO 328 is a potent and selective inhibitor of neuronal and glial GABA uptake and that [3H]NO 328 are a useful radioligand for labeling the GABA uptake carrier in brain membranes. Expand
Characterization of tiagabine (NO-328), a new potent and selective GABA uptake inhibitor.
Although tiagabine antagonized DMCM-induced convulsions, it exhibited neither CGS 9896 or diazepam-like interoceptive effects, nor did it block (or potentiate) pentylenetetrazol-discrimination, thus, GABA uptake inhibition represents a novel rationale for a valproate-like anticonvulsant drug therapy. Expand
NNC-112, NNC-687 and NNC-756, new selective and highly potent dopamine D1 receptor antagonists.
NNC-112, N NC-687 and NNC-756 are potent and selective dopamine D1 receptor antagonists that may be useful in the treatment of schizophrenia. Expand
Comparison of the preclinical anticonvulsant profiles of tiagabine, lamotrigine, gabapentin and vigabatrin
The data here presented show that tiagabine, lamotrigine, gabapentin and vigabatrin possess different preclinical anticonvulsant profiles which is of relevance to the clinical anticonventricular profiles of the drugs. Expand
Novel guanylyl cyclase inhibitor potently inhibits cyclic GMP accumulation in endothelial cells and relaxation of bovine pulmonary artery.
Results suggest that ODQ inhibits nitrovasodilator-induced and endothelium-dependent relaxation through inhibition of guanylyl cyclase activation, but also point to the presence of a cyclic GMP-independent component of relaxation in bovine pulmonary artery. Expand
[3H]GBR 12935 binding in vivo in mouse brain: labelling of a piperazine acceptor site.
Results for the in vitro binding of [3H]GBR 12935 indicate that this site could be a piperazine acceptor site, and the potencies of various dopamine uptake inhibitors to induce stereotyped behavior did not correspond to the inhibitory potencies in the [3 H]GBr 12935 binding assay. Expand
Rapid decline of stereotyped behavior in rats during constant one week administration of amphetamine via implanted ALZET√ Osmotic Minipumps
  • E. B. Nielsen
  • Medicine, Psychology
  • Pharmacology Biochemistry and Behavior
  • 1 August 1981
These results contrast the often reported development of sensitization to the behavioral effect of amphetamine observed with repeated injections and suggest tolerance development in rats. Expand