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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
The primary target is the vomeronasal organ (VON/VNO), a chemosensory organ that detects pheromones. Fasedienol acts as a neurochemical stimulator of the VNO, which projects to the amygdala. By activating this pathway, it modulates the olfactory-amygdala circuitry of fear and anxiety, reducing symptoms of anxiety and PMS without requiring systemic absorption or binding to traditional CNS neurotransmitter receptors.
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| ln Vitro |
In vitro, Fasedienol significantly increases intracellular calcium (Ca2+) levels in cells of the vomeronasal organ, indicating activation of the VNO. It does not directly bind to GABA-A, serotonin, or dopamine receptors, distinguishing it from traditional anxiolytics. Its activity is measured by calcium imaging studies using VNO neurons in culture.
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| ln Vivo |
In vivo, Fasedienol is administered as a nasal spray. In clinical studies, it rapidly alleviates symptoms of social anxiety disorder and premenstrual syndrome. It modulates the olfactory-amygdala circuitry of fear and anxiety without requiring systemic absorption. It has also shown effects on autonomic nervous system activity in healthy adult volunteers.
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| Enzyme Assay |
A non-cellular binding assay is not typically applicable as the target is a chemosensory organ requiring intact tissue structure. However, receptor binding studies can be performed on olfactory bulb or amygdala membranes using radiolabeled steroids to confirm the absence of binding to classical neurotransmitter receptors (GABA, serotonin, dopamine). No specific binding has been observed.
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| Cell Assay |
Cellular activation of the VNO is measured by calcium imaging. Vomeronasal organ tissue or isolated VNO neurons are dissected from rats or mice and loaded with a calcium-sensitive dye (e.g., Fura-2 or Fluo-4). Fasedienol (PH94B) is applied at concentrations of 0.1-100 uM, and changes in intracellular calcium fluorescence are monitored by microscopy. A rapid increase in fluorescence indicates activation of the VNO chemosensory signaling pathway.
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| Animal Protocol |
Fasedienol is evaluated in animal models of anxiety, such as the elevated plus maze (EPM) or light-dark box test in rats. Fasedienol is administered intranasally at doses of 0.1-10 ug per animal. After 15-30 minutes, the animals are placed in the EPM apparatus, and the time spent in the open arms (a measure of reduced anxiety) is recorded. Increased time in the open arms compared to vehicle control indicates anxiolytic-like activity. For human clinical trials, patients with SAD receive Fasedienol nasal spray (e.g., 3.2 mg) before a public speaking challenge, and anxiety is assessed by the Subjective Units of Distress Scale (SUDS) and clinician ratings.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Absorbed after nasal administration. Fasedienol has an unusual pharmacokinetic profile. As a nasal spray that acts locally on the vomeronasal organ, it is designed to have minimal systemic absorption. It acts directly on the VNO without requiring entry into the systemic circulation, thus avoiding first-pass metabolism and reducing systemic side effects. Plasma levels of Fasedienol after intranasal administration are extremely low to undetectable, as the compound does not need to cross the blood-brain barrier to exert its effect. |
| Toxicity/Toxicokinetics |
Toxicity of Fasedienol has been evaluated in preclinical and clinical studies. In animal studies, intranasal administration was well-tolerated. In human clinical trials, Fasedienol has been reported to be safe and well-tolerated, with no significant treatment-emergent adverse events or sedation, distinguishing it from benzodiazepines. Local nasal irritation is mild and transient. No systemic toxicity has been reported.
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| References |
[1]. Clive L. Jennings-White, et al. Steroids as neurochemical stimulators of the vno to alleviate symptoms of anxiety. Patent WO1998014194A1.
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| Additional Infomation |
PH94B, developed by Phern Pharmaceuticals, Inc., is used to treat social phobia (generalized anxiety disorder). It belongs to a new class of drug compounds called vomeronasal agents. Drug Indications For the acute treatment of social phobia. Mechanism of Action Information on the mechanism of action of vomeronasal agents is currently limited. These compounds are administered nasally and bind to chemoreceptors, thereby affecting the hypothalamus and limbic system. Pharmacodynamics Vomeronasal agents can be delivered directly to the nasal cavity via metered-dose nasal sprays or metered-dose nasal aerosols. Because the chemoreceptors are located within the nasal cavity and directly connected to the hypothalamus and limbic system, and because our compounds act locally, vomeronasal proteins do not require systemic absorption and distribution. This offers a significant therapeutic advantage over traditional therapies targeting the hypothalamus and limbic system, which require systemic circulation and crossing the blood-brain barrier to be absorbed by the brain to exert their effects.
Fasedienol is a neuroactive steroid (C19H28O, MW: 272.43) and is the first-in-class pherine (nasal spray) for anxiety disorders. As of the latest data, it has completed Phase 3 clinical trials (e.g., PALISADE-2 trial) for social anxiety disorder. It has not yet received FDA approval. An FDA New Drug Application (NDA) for SAD has been submitted and accepted. It is also under investigation for PMS and postpartum anxiety. The compound was developed by VistaGen Therapeutics. |
| Molecular Formula |
C19H28O
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|---|---|
| Molecular Weight |
272.43
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| Exact Mass |
272.214
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| CAS # |
23062-06-8
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| PubChem CID |
9925482
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4.476
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
20
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| Complexity |
476
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| Defined Atom Stereocenter Count |
6
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| SMILES |
O([H])C1([H])C([H])=C2C([H])([H])C([H])([H])[C@]3([H])[C@@]4([H])C([H])([H])C([H])=C([H])[C@@]4(C([H])([H])[H])C([H])([H])C([H])([H])[C@]3([H])[C@@]2(C([H])([H])[H])C([H])([H])C1([H])[H]
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| InChi Key |
NYVFCEPOUVGTNP-DYKIIFRCSA-N
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| InChi Code |
InChI=1S/C19H28O/c1-18-9-3-4-16(18)15-6-5-13-12-14(20)7-11-19(13,2)17(15)8-10-18/h3,9,12,14-17,20H,4-8,10-11H2,1-2H3/t14-,15-,16-,17-,18-,19-/m0/s1
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| Chemical Name |
(3S,8S,9S,10R,13R,14S)-10,13-dimethyl-2,3,6,7,8,9,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-3-ol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25 mg/mL (91.77 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6707 mL | 18.3533 mL | 36.7067 mL | |
| 5 mM | 0.7341 mL | 3.6707 mL | 7.3413 mL | |
| 10 mM | 0.3671 mL | 1.8353 mL | 3.6707 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT06615557
Conditions:Social Anxiety Disorder (SAD)Link: https://clinicaltrials.gov/ct2/show/NCT06809179
Conditions:Social Anxiety DisorderLink: https://clinicaltrials.gov/ct2/show/NCT04404192
Conditions:Adjustment Disorder With Anxious Mood
Title:Fasedienol Nasal Spray for the Acute Treatment of Anxiety in Adults With Social Anxiety Disorder (PALISADE-3)
Status:Active, not recruiting
updateDate:2025-11-26
Ctid:NCT06358651
Link: https://clinicaltrials.gov/ct2/show/NCT06358651
Conditions:Social Anxiety DisorderLink: https://clinicaltrials.gov/ct2/show/NCT05011396
Conditions:Social Anxiety DisorderLink: https://clinicaltrials.gov/ct2/show/NCT05030350
Conditions:Social Anxiety DisorderLink: https://clinicaltrials.gov/ct2/show/NCT04754802
Conditions:Social Anxiety DisorderLink: https://clinicaltrials.gov/ct2/show/NCT02622958
Conditions:Social Anxiety DisorderProducts are for research use only; We do not sell to patients
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