Fananserin (RP-62203) is a drug which acts as a potent antagonist at both the 5HT 2A receptor, [1] and the Dopamine D 4 receptor, [2] but without blocking other dopamine receptors such as D 2. [3] It has sedative [ 4 ] and antipsychotic effects, and has been researched for the treatment of schizophrenia , [ 5 ] although efficacy was less than ...

Design, synthesis and molecular modelling of new bulky Fananserin derivatives with altered pharmacological profile as potential antidepressants

Fananserin | C23H24FN3O2S | CID 60785 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.

1996年10月24日 · Fananserin, thus, offers an original in vitro profile of monoamine receptor binding, high affinity for D4 and 5-HT2A receptors and low affinity for dopamine D2 recep- tors. It provides an opportunity to assess the role of dopamine D4 receptors in the central nervous system, and their potential as a therapeutic target in innovative treat- ments ...

Objective: The authors' objective was to assess the potential efficacy of fananserin (RP62203), a potent antagonist at the D4 and serotonin2A (5-HT2A) receptors, on symptoms of schizophrenia. Method: A double-blind, placebo-controlled study was conducted in 97 patients. Doses of fananserin reached 250 mg b.i.d. over 28 days, starting with an 8 ...

Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT 2) receptor antagonist, with a K i of 0.37 nM for the rat 5-HT 2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a K i of …

2019年8月1日 · The aim of the study was to synthesize a bulky derivatives of Fananserin, with an altered pharmacological profile. We have focused on the search for multifunctional ligands for the 5-HT 1A /5-HT 7 /D 2 receptors.

1996年10月24日 · This report describe the affinity of the 5-HT2A receptor antagonist RP 62203 (fananserin) for the human dopamine D4 receptor. Fananserin displaces [3H]spiperone binding to recombinant human dopamine D4 receptors with a Ki of 2.93 nM.

法南色林是由赛诺菲研发的一种小分子药物，是一种drd4拮抗剂和5-ht2a拮抗剂。目前该药物最高研发阶段为无进展，用于治疗重度抑郁症、焦虑和精神分裂症。