Flibanserin seems like a very promising candidate for helping with POIS symptoms…
ChatGPT 3.5Q: What 5-HT receptor subtypes are present on human mast cells?Human mast cells express various subtypes of serotonin (5-HT) receptors, and the activation of these receptors can influence mast cell function and mediator release. The specific subtypes of serotonin receptors found on mast cells include:5-HT1 Receptors:Subtypes: 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, and 5-HT1F.Function: Activation of 5-HT1 receptors on mast cells may inhibit the release of histamine and other inflammatory mediators.5-HT2 Receptors:Subtypes: 5-HT2A, 5-HT2B, and 5-HT2C.Function: Activation of 5-HT2 receptors on mast cells can enhance the release of histamine and other proinflammatory mediators.5-HT3 Receptors:Subtypes: 5-HT3A and 5-HT3B.Function: 5-HT3 receptors are ligand-gated ion channels. Activation of these receptors on mast cells may contribute to the release of histamine and other mediators, and their blockade is associated with antiemetic effects.5-HT4 Receptors:Subtypes: 5-HT4A and 5-HT4B.Function: Activation of 5-HT4 receptors on mast cells may influence the release of various mediators, including histamine.5-HT6 Receptors:Subtype: 5-HT6.Function: 5-HT6 receptors are primarily found in the central nervous system, and their role on mast cells is not as well-characterized.5-HT7 Receptors:Subtype: 5-HT7.Function: Activation of 5-HT7 receptors on mast cells may influence the release of histamine and other inflammatory mediators.The functional outcomes of serotonin receptor activation on mast cells can vary depending on the specific receptor subtype and the context of the immune response. For example, some receptor subtypes may promote the release of histamine and other proinflammatory mediators, while others may have inhibitory effects.The modulation of serotonin receptors on mast cells is an active area of research, particularly in the context of allergic and inflammatory conditions. Understanding the specific roles of serotonin receptor subtypes on mast cells may contribute to the development of targeted therapies for conditions associated with mast cell activation, such as allergic diseases and mastocytosis.Q: What is the potential effect of flibanserin with 5-HT receptors on mast cells?The specific effects of flibanserin on mast cells would depend on several factors, including the distribution of serotonin receptor subtypes on mast cells, the concentration of flibanserin reaching peripheral tissues, and the overall pharmacological profile of the drug.In general, the potential effects of flibanserin on mast cells could include:5-HT1A Receptor Activation: Flibanserin acts as a 5-HT1A receptor agonist. Activation of 5-HT1A receptors on mast cells may have inhibitory effects, potentially reducing the release of histamine and other inflammatory mediators.5-HT2A Receptor Antagonism: Flibanserin acts as a 5-HT2A receptor antagonist. Antagonism of 5-HT2A receptors may counteract some proinflammatory effects associated with serotonin receptor activation.
Quote from: Muon on December 28, 2023, 11:16:39 AM(236) Flibanserin for Post-Orgasmic Illness Syndrome: A Case Reporthttps://academic.oup.com/jsm/article/20/Supplement_1/qdad060.222/7164839Very interesting, Muon. This would be top of my list of potential anti-POIS drugs to try because of its novel mechanism of action:Quoteflibanserin has been described as a norepinephrine–dopamine disinhibitor (NDDI)https://en.wikipedia.org/wiki/FlibanserinQuoteNorepinephrine and dopamine disinhibitors (NDDIs) are a class of drugs which act at specific sites to disinhibit downstream norepinephrine and dopamine release in the brainhttps://en.wikipedia.org/wiki/Norepinephrine%E2%80%93dopamine_disinhibitorIt's a drug designed to increase libido (for women!), you would expect it to have some kind of effect on male sexual function too. It worked for the one person in the case study, obviously that's no guarantee that it would work long-term or for a larger number of people, but it's still a starting point. I wonder if anyone else has attempted to copy the study?
(236) Flibanserin for Post-Orgasmic Illness Syndrome: A Case Reporthttps://academic.oup.com/jsm/article/20/Supplement_1/qdad060.222/7164839
flibanserin has been described as a norepinephrine–dopamine disinhibitor (NDDI)
Norepinephrine and dopamine disinhibitors (NDDIs) are a class of drugs which act at specific sites to disinhibit downstream norepinephrine and dopamine release in the brain