Aim: Targeting 5-HT 1A receptor (5-HT 1A R) as a strategy for CNS disorders and pain control. Methodology: A series of 1,3-dioxolane-based 2-heteroaryl-phenoxyethylamines was synthesized by a convergent approach and evaluated at α 1 -adrenoceptors and 5-HT 1A R by binding and functional experiments. Absorption, distribution, metabolism, excretion and toxicity prediction studies were performed to explore the drug-likeness of the compounds. Results & conclusion: The most promising compound, the pyridin-4-yl derivative, emerged as a potent and selective 5-HT 1A R agonist (pKi = 9.2; pD2 = 8.83; 5-HT 1A /α1 = 135). In vitro it was able to permeate by passive diffusion MDCKII-MDR1 monolayer mimicking the blood-brain barrier and showed promis...
The analogues 2-5 of the potent 5-HT1A receptor agonist and α1d-adrenoceptor (α1d-AR) antagonist 1 ...
International audienceBased on the definition of a 5-HT(4) receptor antagonist pharmacophore, a seri...
Among the large number of serotoninergic receptors the 5-HT1A subtype has grown into a considerable ...
Aim: Targeting 5-HT 1A receptor (5-HT 1A R) as a strategy for CNS disorders and pain control. Method...
AIM: Targeting 5-HT1A receptor (5-HT1AR) as a strategy for CNS disorders and pain control. METHODOLO...
Our research group has long been involved in the development of new 5-HT1A selective ligands and 1,3...
A series of compounds generated by ring expansion/opening and molecular elongation/simplification of...
International audienceA novel pyridine derivative, 8-4-[(6-methoxy-2,3-dihydro-[1,4]dioxino[2,3-b]py...
New arylpiperazine derivatives were prepared to identify highly selective and potent ligands for the...
Serotonin (5-hydroxytryptamine, 5-HT) is a relevant neurotransmitter both in the central nervous sys...
The serotonin receptor subtype 1A (5-HT<sub>1A</sub>R) has been implicated in several neurological c...
The medications in use for treating migraine are directed either towards inhibiting the characterist...
New arylpiperazine derivatives were prepared to identify highly selective and potent ligands for the...
The analogues 2-5 of the potent 5-HT1A receptor agonist and α1d-adrenoceptor (α1d-AR) antagonist 1 ...
International audienceBased on the definition of a 5-HT(4) receptor antagonist pharmacophore, a seri...
Among the large number of serotoninergic receptors the 5-HT1A subtype has grown into a considerable ...
Aim: Targeting 5-HT 1A receptor (5-HT 1A R) as a strategy for CNS disorders and pain control. Method...
AIM: Targeting 5-HT1A receptor (5-HT1AR) as a strategy for CNS disorders and pain control. METHODOLO...
Our research group has long been involved in the development of new 5-HT1A selective ligands and 1,3...
A series of compounds generated by ring expansion/opening and molecular elongation/simplification of...
International audienceA novel pyridine derivative, 8-4-[(6-methoxy-2,3-dihydro-[1,4]dioxino[2,3-b]py...
New arylpiperazine derivatives were prepared to identify highly selective and potent ligands for the...
Serotonin (5-hydroxytryptamine, 5-HT) is a relevant neurotransmitter both in the central nervous sys...
The serotonin receptor subtype 1A (5-HT<sub>1A</sub>R) has been implicated in several neurological c...
The medications in use for treating migraine are directed either towards inhibiting the characterist...
New arylpiperazine derivatives were prepared to identify highly selective and potent ligands for the...
The analogues 2-5 of the potent 5-HT1A receptor agonist and α1d-adrenoceptor (α1d-AR) antagonist 1 ...
International audienceBased on the definition of a 5-HT(4) receptor antagonist pharmacophore, a seri...
Among the large number of serotoninergic receptors the 5-HT1A subtype has grown into a considerable ...