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The role of 5-HT1A and 5-HT1B receptors in antidepressant drug actions in the mouse forced swimming test.
TLDR
The anti-immobility effects of the selective serotonin reuptake inhibitors in the forced swimming test seem to be mediated by presynaptic 5-HT1A receptors as well as postsynaptic 5 -HT1B receptors. Expand
Characterization of the V1a antagonist, JNJ-17308616, in rodent models of anxiety-like behavior
TLDR
These results demonstrate the potential for V1a receptor antagonists as novel anxiolytics as well as in vivo efficacy of JNJ-17308616 in animal models of anxiety-like behavior. Expand
Effect of the Glucocorticoid Receptor Antagonist Org 34850 on Basal and Stress‐Induced Corticosterone Secretion
TLDR
The data suggest that a prolonged blockade of GRs is required to increase basal HPA axis activity and Org 34850 could be a potential treatment for mood disorders. Expand
Blockade of the V(1b) receptor reduces ACTH, but not corticosterone secretion induced by stress without affecting basal hypothalamic-pituitary-adrenal axis activity.
TLDR
The results confirm that this compound is an antagonist of the V(1b)R in the rat, and that its ability to reduce stress-induced ACTH responses is stressor dependent with differential modulation of pituitary and adrenal responses. Expand
Effect of vasopressin 1b receptor blockade on the hypothalamic-pituitary-adrenal response of chronically stressed rats to a heterotypic stressor.
TLDR
Both repeated and single episodes of restraint induced the sensitization of the ACTH, but not corticosterone response to acute noise, and Pretreatment with Org reduced the exaggerated ACTH response to noise after both single and repeated exposure to restraint. Expand
Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists.
TLDR
Optimised compound 16 shows a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction and high selectivity with respect to related receptors V(1a), V(2) and OT. Expand
The discovery of novel 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamides as vasopressin V1A receptor antagonists.
The discovery of a novel series of 8-azabicyclo[3.2.1]octan-3-yl)-3-(4-chlorophenyl) propanamide antagonists of the vasopressin V(1A) receptor is disclosed. Compounds 47 and 48 were found to be highExpand
Characterization of a novel and selective V1B receptor antagonist.
TLDR
A V(1B) antagonist has been developed which has significant selectivity for the human V( 1B) receptor over the other members of the vasopressin receptor sub-family and does not modulate the activity of the HPA axis under normal basal conditions. Expand
Effect of the glucocorticoid receptor antagonist Org 34850 on fast and delayed feedback of corticosterone release.
TLDR
The data suggest an involvement of GR in modulating delayed, but not fast, inhibition induced by MPL on basal corticosterone secretion, and that blockade of GR with Org 34850 prevented delayed inhibition of MPL in response to the synthetic glucocorticoid methylprednisolone. Expand
Assessment of seizure liability of Org 306039, a 5-HT2c agonist, using hippocampal brain slice and rodent EEG telemetry.
TLDR
In vitro and in vivo models complement each other in the characterization of the seizure potential of CNS-targeted compounds such as the 5-HT2c agonist Org 306039, indicating seizure-genic potential. Expand
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