| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
Spiroxatrine targets serotonin 5-HT1A receptors and α2-adrenergic receptors. It is a selective antagonist of 5-HT1A with a Ki of 3.94 nM, demonstrating high affinity and selectivity for 5-HT1A over 5-HT1B (Ki = 224000 nM) and 5-HT2 (Ki = 118.5 nM). Spiroxatrine is also a potent α2C adrenergic receptor antagonist.
|
|---|---|
| ln Vitro |
In α2A/D-initiin receptor knockout mice, Spirosatin (0.01-0.1 μM, 15 minutes) increases vas deferens tissue contraction [2].
Spiroxatrine is a selective, dual antagonist of 5-HT1A and α2-adrenergic receptors. It exhibits Ki values of 3.94 nM for 5-HT1A, 224000 nM for 5-HT1B, and 118.5 nM for 5-HT2 receptors. The compound's high affinity for 5-HT1A and α2-adrenergic receptors distinguishes it from other serotonergic compounds. |
| ln Vivo |
In the hind paw, carrageenan-induced signal withdrawal latency and nerve damage are both increased by 1-to 25-ug intraperitoneal injection over a 5-day period of time [3]. The efficacy of fluoxetine in decreasing selective proliferative alcoholophilic P-lineage-dependent vitamin A recovery is enhanced by spiroxatrine (4 mg/kg/day, i.p., 5 minutes) [4].
Spiroxatrine exhibits sedative effects in vivo. It has demonstrated anxiolytic effects when used in combination with buspirone. As a 5-HT1A and α2-adrenergic receptor antagonist, it modulates serotonin and noradrenaline signaling in the central nervous system. Specific animal model data are not extensively detailed. |
| Enzyme Assay |
Spiroxatrine's binding affinity to 5-HT1A, 5-HT1B, 5-HT2, and α2-adrenergic receptors can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant receptors. Competition binding experiments are performed with increasing concentrations of spiroxatrine against a fixed concentration of a radiolabeled receptor-specific ligand. Ki values are calculated from competition curves.
|
| Cell Assay |
The functional activity of spiroxatrine at 5-HT1A and α2-adrenergic receptors is evaluated in cell-based assays. Cells expressing recombinant 5-HT1A or α2-adrenergic receptors are treated with increasing concentrations of spiroxatrine. Receptor-mediated signaling pathways (e.g., cAMP modulation or calcium mobilization) are measured. Antagonist activity is assessed by the compound's ability to block agonist-induced signaling.
|
| Animal Protocol |
Animal/Disease Models: nerve injury rat model and carrageenan-induced rat inflammation model [3] Usage and
Doses: 1, 10, 25 ug, 5 days Route of Administration: intraperitoneal (ip) injection Experimental Results: Increased hind paw response to heat and Withdrawal latency to mechanical stimulation. Animal/Disease Models: Fluoxetine induces a decrease in P-line ethanol intake in rats [4] Doses: 4 mg/kg/day, 5 minutes Route of Administration: intraperitoneal (ip) injection Experimental Results:Selectively increases fluoxetine-induced voluntariness Oral ethanol intake produces alcohol-preferring P-strain rats. Spiroxatrine is administered orally or intraperitoneally in animal models of anxiety or sedation. In rodent models (e.g., elevated plus maze, open field test, or sedative assays), spiroxatrine is given at various doses. Behavioral responses are assessed to evaluate anxiolytic and sedative effects. |
| ADME/Pharmacokinetics |
Spiroxatrine has a molecular formula of C22H25N3O3 and a molecular weight of 379.45 g/mol. It is soluble in DMSO. Its exact mass is 379.1896. Specific pharmacokinetic parameters such as half-life and bioavailability are not extensively detailed.
|
| Toxicity/Toxicokinetics |
The toxicity profile of spiroxatrine is not extensively documented. As a 5-HT1A and α2-adrenergic receptor antagonist, potential adverse effects may include sedation and cardiovascular effects. Specific LD50 values and organ-specific toxicity data are not readily available.
|
| References |
|
| Additional Infomation |
8-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1-phenyl-1,3,8-triazaspiro[4.5]decane-4-one is a member of the imidazolide family of compounds.
Spiroxatrine (CAS# 1054-88-2) is also known as R 5188. It is a selective dual antagonist of 5-HT1A (Ki = 3.94 nM) and α2-adrenergic receptors. Spiroxatrine exhibits sedative effects and has been studied for anxiolytic properties in combination with buspirone. |
| Molecular Formula |
C22H25N3O3
|
|---|---|
| Molecular Weight |
379.46
|
| Exact Mass |
379.19
|
| CAS # |
1054-88-2
|
| PubChem CID |
5268
|
| Appearance |
White to off-white solid powder
|
| Density |
1.32g/cm3
|
| Boiling Point |
602.8ºC at 760mmHg
|
| Flash Point |
318.4ºC
|
| Vapour Pressure |
1.74E-14mmHg at 25°C
|
| Index of Refraction |
1.665
|
| LogP |
2.586
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
28
|
| Complexity |
557
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JVGBTTIJPBFLTE-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C22H25N3O3/c26-21-22(25(16-23-21)17-6-2-1-3-7-17)10-12-24(13-11-22)14-18-15-27-19-8-4-5-9-20(19)28-18/h1-9,18H,10-16H2,(H,23,26)
|
| Chemical Name |
8-(2,3-dihydro-1,4-benzodioxin-3-ylmethyl)-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
|
| Synonyms |
R 5188; Espiroxatrina; Spiroxatrine
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~1.92 mg/mL (~5.06 mM)
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6353 mL | 13.1766 mL | 26.3532 mL | |
| 5 mM | 0.5271 mL | 2.6353 mL | 5.2706 mL | |
| 10 mM | 0.2635 mL | 1.3177 mL | 2.6353 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
