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Azacyclonol

CAS# 115-46-8

Azacyclonol

2D Structure

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Azacyclonol

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Chemical Properties of Azacyclonol

Cas No. 115-46-8 SDF Download SDF
PubChem ID 15723 Appearance Powder
Formula C18H21NO M.Wt 267.37
Type of Compound N/A Storage Desiccate at -20°C
Synonyms γ-pipradol
Solubility DMSO : 100 mg/mL (374.01 mM; Need ultrasonic)
Chemical Name diphenyl(piperidin-4-yl)methanol
SMILES C1CNCCC1C(C2=CC=CC=C2)(C3=CC=CC=C3)O
Standard InChIKey ZMISODWVFHHWNR-UHFFFAOYSA-N
Standard InChI 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
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Azacyclonol

DescriptionAzacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals. Target: Others Azacyclonol is a drug which is a so-called ataractive, or agent which diminishes hallucinations in psychotic individuals. The formation of Azacyclonol in human intestinal microsomes is linear with respect to time up to 60 min. The rates of formation of Azacyclonol increases linearly with microsomal protein concentration up to 2 mg/mL. The apparent Km and Vmax values of Azacyclonol are 0.82 μM and 60 pmol/min/mg protein in microsomes from human liver [1]. The formation of Azacyclonol and terfenadine alcohol from terfenadine is confirmed to be catalyzed predominantly by CYP3A(4) isozyme, and the ratio of the rate of terfenadine alcohol formation to that of Azacyclonol is 3:1 [2]. The amount of Azacyclonol eliminated renally increases on average 2-fold after rifampin dosing [3].

References:
[1]. Raeissi, S.D., et al., Comparison of CYP3A activities in a subclone of Caco-2 cells (TC7) and human intestine. Pharm Res, 1997. 14(8): p. 1019-25. [2]. Ling, K.H., et al., Metabolism of terfenadine associated with CYP3A(4) activity in human hepatic microsomes. Drug Metab Dispos, 1995. 23(6): p. 631-6. [3]. Brown, D.A. and J.P. Quilliam, The effects of some centrally acting drugs on ganglionic transmission in the cat. Br J Pharmacol Chemother, 1964. 23(2): p. 241-56.

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Preparing Stock Solutions of Azacyclonol

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.7401 mL 18.7007 mL 37.4014 mL 74.8027 mL 93.5034 mL
5 mM 0.748 mL 3.7401 mL 7.4803 mL 14.9605 mL 18.7007 mL
10 mM 0.374 mL 1.8701 mL 3.7401 mL 7.4803 mL 9.3503 mL
50 mM 0.0748 mL 0.374 mL 0.748 mL 1.4961 mL 1.8701 mL
100 mM 0.0374 mL 0.187 mL 0.374 mL 0.748 mL 0.935 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Azacyclonol

Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.

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References on Azacyclonol

Determination of the terfenadine metabolite azacyclonol in human serum using gas chromatography-mass spectrometry.[Pubmed:8738042]

J Chromatogr B Biomed Appl. 1996 Apr 12;678(2):349-53.

In this work, a method for the determination of Azacyclonol, a primary metabolite of terfenadine, in human serum is described. Sample preparation is carried out by liquid-liquid extraction under basic conditions. For an efficient clean up, the analytes are back-extracted into diluted hydrochloric acid and, after alkalinization, are once again extracted into the organic phase. No derivatisation step is performed. The samples are measured by gas chromatography-mass spectrometry with good selectivity. The limit of detection is 2 ng/ml. The coefficients of variation are 12.6% at 10 ng/ml and 6.44% at 200 ng/ml in the day-to-day control measurements.

Measurement of azacyclonol in urine and serum of humans following terfenadine (Seldane) administration using gas chromatography-mass spectrometry.[Pubmed:1400799]

J Chromatogr. 1992 Jul 24;578(2):207-13.

A gas chromatographic-mass spectrometric (GC-MS) method is presented for the analysis of Azacyclonol (AZA), a metabolite of terfenadine in serum and urine specimens. Following an alkaline extraction, AZA and an internal standard were derivatized using heptafluorobutyric anhydride. Fourier transform infrared spectrometry suggested that two sites on the AZA molecule were derivatized. GC-MS of the extracts had a limit of quantitation (LOQ) of 1 ng/ml and linear range of 1-1000 ng/ml in urine. Four volunteers were administered a therapeutic regimen of terfenadine followed by urine and serum specimen collection(s) during the next seven days. The results indicated that following a 60-mg dose of terfenadine each 12 h for five days, (1) AZA appears in urine within 2 h, (2) urine AZA concentrations were above the LOQ 72 h following the last dose, (3) peak urine concentrations were as high as 19,000 ng/ml, and (4) mean serum concentration following the ninth dose was 59 ng/ml.

Description

Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.

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