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5-HT2A receptor antagonism potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and inhibits that in the nucleus accumbens in a dose-dependent manner
Combined serotonin (5-HT)2A and dopamine (DA) D2 blockade has been shown to contribute to the ability of atypical antipsychotic drugs (APDs) to increase DA release in rat medial prefrontal cortex…
5-HT(2A) receptor antagonism potentiates haloperidol-induced dopamine release in rat medial prefrontal cortex and inhibits that in the nucleus accumbens in a dose-dependent manner.
The results suggest that the relatively higher ratio of 5- HT(2A) to D(2) antagonism may contribute to the potentiation of haloperidol-induced mPFC DA release, whereas 5-HT( 2A) antagonisms can diminish haloperIDol- induced NAC DA release.
Nitric oxide: A new messenger in the brain
- J. Bruhwyler, E. Chleide, J. Liégeois, F. Carreer
- Medicine, PsychologyNeuroscience & Biobehavioral Reviews
- 1 December 1993
The aim of this paper is to review and to integrate the most recent advances in the understanding of the roles of NO in the brain.
Modulation of small conductance calcium-activated potassium (SK) channels: a new challenge in medicinal chemistry.
- J. Liégeois, F. Mercier, A. Graulich, F. Graulich-Lorge, J. Scuvée-Moreau, V. Seutin
- Chemistry, MedicineCurrent medicinal chemistry
- 31 March 2003
Small conductance calcium-activated potassium (SK) channels are found in many types of neurons as well as in some other cell types, and are heavily expressed in the basal ganglia and in the limbic system, suggesting that they may modulate motricity and emotional behaviour.
Allosteric Block of KCa2 Channels by Apamin*
- Cédric Lamy, S. Goodchild, +4 authors N. Marrion
- Chemistry, MedicineThe Journal of Biological Chemistry
- 18 June 2010
This multidisciplinary approach suggested that apamin does not behave as a classical pore blocker but blocks using an allosteric mechanism that is consistent with observed differences between binding affinity and potency of block.
SK channels control the firing pattern of midbrain dopaminergic neurons in vivo
- O. Waroux, L. Massotte, +5 authors V. Seutin
- Chemistry, MedicineThe European journal of neuroscience
- 1 December 2005
The first demonstration of a major role of SK channels in the control of the switch between tonic and burst firing of dopaminergic neurons in physiological conditions is provided, which suggests a new strategy to develop modulators of the dopamine (DA) system.
JL13, a pyridobenzoxazepine compound with potential atypical antipsychotic activity: a review of its behavioural properties.
- J. Bruhwyler, J. Liégeois, +6 authors J. Géczy
- Chemistry, MedicinePharmacological research
- 1 October 1997
In a complex temporal regulation schedule in the dog, JL13 showed a high resemblance with clozapine without inducing sialorrhea, palpebral ptosis or any significant motor side effects.
The inflammatory reaction induced by formalin in the rat paw
It is concluded that formalin administered at a low dose induces an oedema which mainly results from a neurogenic inflammation mediated by neuropeptides such as substance P, prostanoids, 5-hydroxytryptamine and histamine.
Crucial role of a shared extracellular loop in apamin sensitivity and maintenance of pore shape of small-conductance calcium-activated potassium (SK) channels
- Kate L. Weatherall, V. Seutin, J. Liégeois, N. Marrion
- Biology, MedicineProceedings of the National Academy of Sciences
- 24 October 2011
It is shown that the S3–S4 loop of one subunit overlaps the outer pore of the adjacent subunit, with apamin interacting with both regions, which provides a unique binding site for each combination of SK subunits within a coassembled channel that may be targeted to produce blockers specific for heteromeric SK channels.
Novel inhibitors of the sodium-calcium exchanger: benzene ring analogues of N-guanidino substituted amiloride derivatives.
- F. Rogister, D. Laeckmann, +8 authors B. Masereel
- Chemistry, MedicineEuropean journal of medicinal chemistry
- 1 August 2001
A series of N-guanidino substituted 2,4-diamino-5-carbonylguanidine molecules related to amiloride were synthesised and evaluated for their ability to inhibit the sodium-calcium exchanger in rat…