| Size | Price | Stock | Qty |
|---|---|---|---|
| 5g |
|
||
| Other Sizes |
| Targets |
Azacyclonol acts primarily as a dopamine receptor antagonist with additional antihistaminic activity. It is a ganglionic blocker that reduces perceptual disturbances induced by hallucinogens such as LSD. It also has affinity for the histamine H1 receptor with a Ki of 6.18.
|
|---|---|
| ln Vitro |
Azacyclidol is produced in rat liver from terfenadine [2].
In vitro, azacyclonol has been characterized as a central nervous system depressant and a ganglionic blocker. Its ability to antagonize the effects of psychostimulants such as amphetamine, morphine, and cocaine has been demonstrated in animal models. It has potential anxiolytic and antidepressant activities. |
| ln Vivo |
In rats and mice, azacyclidol inhibits activity [3]. Azacyclonol prolongs hexobarbital hypnosis and counteracts the increase in coordinated activity in mice brought on by piperamidol, amphetamine, morphine, and cocaine [3].
In vivo, azacyclonol causes depressed activity in mice and rats. It antagonizes increased coordination activity in mice induced by pipradrol, amphetamine, morphine, and cocaine, and prolongs hexobarbital hypnosis. It has been studied for the treatment of schizophrenia and drug-induced psychosis but showed limited efficacy compared with newer antipsychotics. |
| Enzyme Assay |
The activity of azacyclonol can be assessed using receptor binding assays. Membranes prepared from brain tissue are incubated with radiolabeled ligands for dopamine receptors or histamine H1 receptors and varying concentrations of azacyclonol. The displacement of the radioligand is measured to determine the affinity of azacyclonol for these receptors.
|
| Cell Assay |
To evaluate the cellular effects of azacyclonol, neuronal cell cultures are treated with the compound, and the effects on neuronal activity and neurotransmitter release are measured. The compound's ability to inhibit dopamine or histamine receptor-mediated signaling can be assessed using second messenger assays.
|
| Animal Protocol |
In vivo studies with azacyclonol typically involve administration to rodents via oral or intraperitoneal routes. Behavioral tests such as the open field test, elevated plus maze, and conditioned place preference are used to assess the compound's effects on activity, anxiety, and reward. The compound's ability to antagonize the effects of psychostimulants is also evaluated.
|
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Azacycloheptanol is a known human metabolite of terfenadine. Azacyclonol has a molecular formula of C18H21NO and a molecular weight of 267.37. Its CAS number is 115-46-8. It is a central nervous system depressant and a ganglionic blocker. It is a metabolite of terfenadine. The compound is soluble in organic solvents. |
| Toxicity/Toxicokinetics |
Specific toxicology data for azacyclonol are not detailed in the available literature. However, as a central nervous system depressant, it can cause sedation and drowsiness. At high doses, it may cause more severe central nervous system depression. The compound's use has been limited due to its modest efficacy and side effect profile.
|
| References | |
| Additional Infomation |
Diphenyl(4-piperidinyl)methanol is a diarylmethane.
Azacyclonol (MER 17) is a drug used to diminish hallucinations in psychotic individuals. It is a metabolite of terfenadine and acts as a central nervous system depressant and ganglionic blocker. It has been studied for the treatment of schizophrenia and drug-induced psychosis. It is not a commonly used drug in modern clinical practice. |
| Molecular Formula |
C18H21NO
|
|---|---|
| Molecular Weight |
267.3654
|
| Exact Mass |
267.162
|
| CAS # |
115-46-8
|
| Related CAS # |
1798-50-1 (hydrochloride)
|
| PubChem CID |
15723
|
| Appearance |
White to off-white solid powder
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
445.5±40.0 °C at 760 mmHg
|
| Melting Point |
160-163 °C
|
| Flash Point |
142.0±18.0 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.584
|
| LogP |
3.25
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
20
|
| Complexity |
268
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
ZMISODWVFHHWNR-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C18H21NO/c20-18(15-7-3-1-4-8-15,16-9-5-2-6-10-16)17-11-13-19-14-12-17/h1-10,17,19-20H,11-14H2
|
| Chemical Name |
diphenyl(piperidin-4-yl)methanol
|
| 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 : ~100 mg/mL (~374.01 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.35 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.35 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (9.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7401 mL | 18.7007 mL | 37.4014 mL | |
| 5 mM | 0.7480 mL | 3.7401 mL | 7.4803 mL | |
| 10 mM | 0.3740 mL | 1.8701 mL | 3.7401 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
