Comparative pharmacology of antipsychotics possessing combined dopamine D2 and serotonin 5-HT1A receptor propertiesAdrian Newman-Tancredi
NeuroAct Communication, Castres, France
Psychopharmacology (Berl) 216:451-73. 2011
..Such a strategy reduces side-effects such as the extrapyramidal syndrome (EPS), weight gain, and autonomic disturbance liability...
The importance of 5-HT1A receptor agonism in antipsychotic drug action: rationale and perspectivesAdrian Newman-Tancredi
NeuroAct Communication, 25 rue des Généraux Ricard, Castres, France
Curr Opin Investig Drugs 11:802-12. 2010
..The balance of 5-HT1A/D2 receptor properties should therefore be considered when selecting compounds as antipsychotic development candidates...
- Actions of novel antipsychotic agents on apomorphine-induced PPI disruption: influence of combined serotonin 5-HT1A receptor activation and dopamine D2 receptor blockade
Agnès L Auclair
Division of Neurobiology 2, Centre de Recherche Pierre Fabre, Castres, France
Neuropsychopharmacology 31:1900-9. 2006
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- F15599, a highly selective post-synaptic 5-HT(1A) receptor agonist: in-vivo profile in behavioural models of antidepressant and serotonergic activity
Marie Bernadette Assié
Neurobiology II Division, Centre de Recherche Pierre Fabre, Castres, France
Int J Neuropsychopharmacol 13:1285-98. 2010
..The distinctive pharmacological profile of F15599 suggests that preferential targeting of post-synaptic 5-HT(1A)Rs constitutes a promising strategy for improved antidepressant therapy...
- Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia
Adrian Newman-Tancredi
Division of Neurobiology 2, Centre de Recherche Pierre Fabre, Castres, France
Int J Neuropsychopharmacol 8:341-56. 2005
..Thus, the contribution of 5-HT1A receptor activation to the pharmacological profile of action of the antipsychotics will depend on the relative 5-HT1A/D2 affinities and on 5-HT1A agonist efficacy of the drugs...
- Antipsychotic-like vs cataleptogenic actions in mice of novel antipsychotics having D2 antagonist and 5-HT1A agonist properties
Laurent Bardin
Division of Neurobiology 2, Centre de Recherche Pierre Fabre, Castres, France
Neuropsychopharmacology 31:1869-79. 2006
..Further, they indicate that the balance of affinity and/or efficacy between D2 and 5-HT1A receptors profoundly influences their pharmacological activities, and will likely impact their therapeutic profiles...
- The central serotonin 2B receptor: a new pharmacological target to modulate the mesoaccumbens dopaminergic pathway activity
Agnès L Auclair
Division of Neurobiology 2, Centre de Recherche Pierre Fabre, Castres, France
J Neurochem 114:1323-32. 2010
..63 mg/kg). These findings demonstrate that 5-HT(2B)Rs exert a facilitatory control on mesoaccumbens DA pathway activity, and suggest that they may constitute a new target for improved treatment of DA-related neuropsychiatric disorders...
- Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors disrupt basal PPI of the startle reflex in rats
Agnès L Auclair
Division of Neurobiology 2, Centre de Recherche Pierre Fabre, 17, avenue Jean Moulin, 81106, Castres, France
Psychopharmacology (Berl) 193:45-54. 2007
..A novel class of potential antipsychotics (SSR181507, bifeprunox, and SLV313) possess partial agonist/antagonist properties at D(2) receptors and various levels of 5-HT(1A) activation...
- Pharmacological profiles in rats of novel antipsychotics with combined dopamine D2/serotonin 5-HT1A activity: comparison with typical and atypical conventional antipsychotics
Laurent Bardin
Division of Neurobiology, Pierre Fabre Research Centre, Castres, France
Behav Pharmacol 18:103-18. 2007
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- Agonist and antagonist properties of antipsychotics at human dopamine D4.4 receptors: G-protein activation and K+ channel modulation in transfected cells
Adrian Newman-Tancredi
Division of Neurobiology 2, Centre de Recherche Pierre Fabre, Castres, France
Int J Neuropsychopharmacol 11:293-307. 2008
..These data indicate that, unlike conventional or 'atypical' antipsychotics, several 'third generation' agents display D4 receptor partial agonism that may be sufficient to influence physiological D4 receptor activity in vivo...
- Penile erection and yawning induced by dopamine D2-like receptor agonists in rats: influence of strain and contribution of dopamine D2, but not D3 and D4 receptors
Ronan Depoortere
Division of Neurobiology 2, Centre de Recherche Pierre Fabre, Castres, France
Behav Pharmacol 20:303-11. 2009
..5 mg/kg). The present data do not support a major implication of either DA D3 or D4 receptors in the control of PE and YA in rats, but indicate a preponderant role of DA D2 receptors...
