F-15,063 is an orally active potential antipsychotic, and an antagonist at the D2/D3 receptors, partial agonist at the D4 receptor, and agonist at the 5-HT1A receptors. It has greater efficacy at the 5-HT1A receptors than other antipsychotics, such as clozapine, aripiprazole, and ziprasidone. This greater efficacy may lead to enhanced antipsychotic properties, as antipsychotics that lack 5-HT1A affinity are associated with increased risk of extrapyramidal symptoms, and lack of activity against the negative symptoms of schizophrenia.[1]
As expression of immediate-early gene (IEG) in certain brain regions may represent markers of anti-psychotic activity, expression of immediate-early gene mRNA in the prefrontal cortex and striatum was measured. Treatment with F-15,063 resulted in induction of c-fos and fosB mRNA expression in the prefrontal cortex. In the striatum, F-15,063 treatment resulted in induction of all
IEGs studied (c-fos, fosB, zif268, c-jun, junB, nor1, nur77, arc).[2]
F-15,063 was tested in several animal models that predict antipsychotic activity to help determine the behavioral profile. Administration of F-15,063 blocked amphetamine and ketamine induced hyperlocomotion, but did not affect baseline, spontaneous locomotor activity. In addition, F-15,063 did not produce catalepsy, a side effect of other antipsychotics, such as haloperidol. This inhibition of catalepsy is 5-HT1A receptor mediated, as pretreatment with the 5-HT1A antagonist WAY-100635 reinstated catalepsy. The level of catalepsy did not increase with chronic dosing, and there was no evidence for serotonin syndrome at clinically relevant doses.[3]
Plasma levels of F-15,063 decreased seven-fold 4 hours after oral administration, and 25-fold after 8 hours. Despite this, there was still a high (65%) level of central D2 occupancy at 4 hours, and it retained its full antipsychotic potential at this time point. Even after 8 hours, F-15,063 still demonstrated some central D2 occupancy, and retained some antipsychotic activity.[4]
^Bruins Slot, LA (October 2009). "F15063, a potential antipsychotic with dopamine D(2)/D(3) receptor antagonist and 5-HT(1A) receptor agonist properties: influence on immediate-early gene expression in rat prefrontal cortex and striatum". European Journal of Pharmacology. 620 (1–3): 27–35. doi:10.1016/j.ejphar.2009.08.019. PMID19695244.
Well, that’s interesting to know that Psilotum nudum are known as whisk ferns. Psilotum nudum is the commoner species of the two. While the P. flaccidum is a rare species and is found in the tropical islands. Both the species are usually epiphytic in habit and grow upon tree ferns. These species may also be terrestrial and grow in humus or in the crevices of the rocks.
View the detailed Guide of Psilotum nudum: Detailed Study Of Psilotum Nudum (Whisk Fern), Classification, Anatomy, Reproduction
Well, that’s interesting to know that Psilotum nudum are known as whisk ferns. Psilotum nudum is the commoner species of the two. While the P. flaccidum is a rare species and is found in the tropical islands. Both the species are usually epiphytic in habit and grow upon tree ferns. These species may also be terrestrial and grow in humus or in the crevices of the rocks.
View the detailed Guide of Psilotum nudum: Detailed Study Of Psilotum Nudum (Whisk Fern), Classification, Anatomy, Reproduction