• Publications
  • Influence
PDE4 inhibitors induce emesis in ferrets via a noradrenergic pathway
TLDR
The studies suggest that the ferret is an appropriate model to study emesis induced by PDE4 inhibitors and that these compounds trigger the emetic reflex via a noradrenergic pathway, mimicking the pharmacological actions of a pre-synaptic alpha(2)-adrenoceptor inhibition. Expand
Assessing the emetic potential of PDE4 inhibitors in rats
TLDR
This model is functionally coupled to PDE4, specific to alpha2‐adrenoceptors and relevant to Pde4 inhibitor‐induced emesis and provides a novel way of evaluating the emetic potential of PDE 4 inhibitors in rats. Expand
Pyridazinones as selective cyclooxygenase-2 inhibitors.
TLDR
Pyridazinone was found to be an excellent core template for selective COX-2 inhibitors, which were highly efficacious in rat paw edema and rat pyresis models. Expand
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.
TLDR
5- Chloro-3-(4-methylsulfonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine 33 was identified as the optimum compound in this series and observed to inhibit COX-2 activity by introducing a substituent at C5 of the central pyridine. Expand
Involvement of NK1 and NK2 Receptors in Pulmonary Responses Elicited by Non‐adrenergic, Non‐cholinergic Vagal Stimulation in Guinea‐pigs
TLDR
Observations using antidromic vagal stimulation to stimulate sensory c‐fibres as a means of eliciting the release of endogenous tachykinins in propranolol‐ and atropine‐treated guinea‐pigs are extended. Expand
Effect of dexamethasone on antigen-induced high molecular weight glycoconjugate secretion in allergic guinea pigs.
TLDR
Morphometric analysis of Alcian blue -stained airway sections showed a decline in stored mucosubstances following the antigen exposure, supporting the notion that the allergic guinea pig model exhibits a mucosecretory component. Expand
Evaluation of bronchoconstriction induced by neurokinins and its inhibition by selective nonpeptide antagonists in conscious guinea pigs, using a double-chamber plethysmograph technique.
TLDR
The response to NKA was not inhibited by mepyramine, indomethacin, or MK-571 but was significantly reduced by atropine and hexamethonium, suggesting the involvement of a cholinergic mechanism. Expand
Neurokinin receptors subserving plasma extravasation in guinea pig airways.
TLDR
Results from these studies demonstrate conclusively that only NK1 receptors subserve plasma extravasation in the trachea and large airways of the guinea pig is mediated by both NK1 and NK2 receptors. Expand
2-heterosubstituted-3-(4-methylsulfonyl)phenyl-5-trifluoromethyl pyridines as selective and orally active cyclooxygenase-2 inhibitors.
A series of novel 2-alkoxy, 2-thioalkoxy and 2-amino-3-(4-methylsulfonyl)phenylpyridines has been synthesized and shown to be highly potent and selective cyclooxygenase-2 (COX-2) inhibitors.Expand
...
1
2
...