Pharmacology of flibanserin
Flibanserin has best affection for serotonin 5-HT(1A), dopamine D(4k), and serotonin 5-HT(2A) receptors. In vitro and in microiontophoresis, flibanserin behaves as a 5-HT(1A) agonist, a actual anemic fractional agonist on dopamine D(4) receptors, and a 5-HT(2A) antagonist. In vivo flibanserin binds appropriately to 5-HT(1A) and 5-HT(2A) receptors. However, beneath college levels of academician 5-HT (i.e., beneath stress), flibanserin may absorb 5-HT(2A) receptors in college admeasurement than 5-HT(1A) receptors. The furnishings of flibanserin on adenylyl cyclase are altered from those of buspirone and 8-OH-DPAT, two added declared 5-HT(1A) receptor agonists.
Flibanserin reduces neuronal battlefront amount in beef of the after a rape, hippocampus, and case with the CA1 arena getting the a lot of acute in the brain. Flibanserin-induced abridgment in battlefront amount in the case seems to be advised through dispatch of postsynaptic 5-HT(1A) receptors, admitting the abridgement of the amount of alive beef seems to be advised through dopamine D(4) receptor stimulation. Flibanserin bound desensitizes actual 5-HT autoreceptors in the after raphe and enhances analeptic activation of postsynaptic 5-HT(1A) receptors in the CA3 region. Flibanserin preferentially reduces amalgam and extracellular levels of 5-HT in the cortex, area it enhances extracellular levels of NE and DA.
Flibanserin displays antidepressant-like action in a lot of beastly models acute to antidepressants. Such activity, however, seems qualitatively altered from that exerted by added antidepressants. Flibanserin seems to act via absolute or aberrant dispatch of 5-HT(1A), DA, and opioid receptors in those beastly models. Flibanserin does not affectation constant furnishings in beastly models of all-overs and seems to apply abeyant antipsychotic effects. Flibanserin may abet some balance but does not abet appreciable baneful furnishings at pharmacologically accordant doses.
Flibanserin acts as a full agonist in the frontal cortex and the raphe dorsalis, but only as a partial agonist in the CA3 region of the hippocampus of the 5-HT1A receptor (Ki = 1 nM in CHO cells, but only 15–50 nM in cortex, hippocampus and dorsal raphe) and, with lower affinity, as an antagonist of the 5-HT2A receptor (Ki = 49 nM) and antagonist or very weak partial agonist of the D 4 receptor (K i = 4–24 nM).
Send inquiry online For more product information and prices
(Pharmaceutical Ingredients Manufacturer & Supplier & Exporter.)
After sending the online inquiry, we will reply you as soon as possible, if not get any response on time please contact us by Tel or Email. —— Green Stone SwissEmail: [email protected]
Tel: +86 592 5365887
WhatsApp: +86 189 6515 7632
Send inquiry online: