Piperonyl alcohol does not have a specific pharmacological target. As a benzodioxole derivative, it is primarily used as a chemical intermediate and scaffold in medicinal chemistry. The benzodioxole moiety is a common structural motif in various bioactive compounds, including insecticides, pharmaceuticals, and natural products. Piperonyl alcohol itself is not a therapeutic agent but serves as a building block for the synthesis of more complex molecules.

Piperonyl alcohol has no reported in vitro pharmacological activity. It is not a bioactive compound but rather a chemical reagent and synthetic intermediate. In vitro studies involving piperonyl alcohol would typically focus on its chemical properties, such as reactivity, stability, and solubility, rather than biological activity. It may be used as a control compound or as a starting material for the synthesis of biologically active derivatives.

Piperonyl alcohol has no reported in vivo pharmacological activity. It is not used as a therapeutic agent and has no approved clinical indications. As a chemical reagent, it is not intended for in vivo administration. If administered in vivo, it would likely be metabolized and excreted without exerting specific pharmacological effects.

In vitro enzyme/receptor binding assays are not applicable for piperonyl alcohol, as the compound is not biologically active. It is used as a chemical reagent and synthetic intermediate, not as a bioactive molecule. If used in biochemical assays, it would serve as a negative control or as a reference compound for method development, but it does not interact with enzymes or receptors in a specific manner.

In vitro cell-based assays are not applicable for piperonyl alcohol. The compound is not used in cell culture experiments for biological activity assessment. If used in cell-based systems, it would be as a solvent control or as a precursor for the synthesis of cell-permeable compounds, not for studying cellular responses. Cytotoxicity assays are not relevant for this compound as a primary endpoint.

In vivo animal studies are not conducted for piperonyl alcohol as a test compound. The compound is used as a chemical reagent and synthetic intermediate, not as a pharmacological agent. If used in animal studies, it would be as a component of test formulations for other compounds or as a reference material, but no specific studies have been reported.

Absorption, Distribution and Excretion
Thirteen carbon-14 labeled MDP compounds, such as topiramate, piperonal, piperidine, piperic acid, safrole, dihydrosafrole, or piperidine, were injected into male Swiss Webster mice, Sprague-Dowley rats, or hamsters. Urine, feces, and exhaled gases were collected for 48 hours for carbon-14 assays. Carbon-14 activity in the intestine, liver, and carcass was determined. Carbon dioxide is not a major metabolic pathway for piperidine, piperonal, piperic acid, and topiramate. Their metabolites are primarily excreted in urine. Metabolism/Metabolites The metabolism of methylenedioxyphenyl (MDP) compounds in mammals was investigated. This study aimed to explore the demethylation mechanisms of MDPs and their analogues and their relationship to the metabolism and modes of action of commercial potentiators such as piperidine and topiramate. Male Swiss-Webster mice, Sprague-Dawley rats, and hamsters were administered 13 carbon-14 labeled MDP compounds, including topiramate, piperonal, piperidine, piperic acid, safrole, dihydrosafrole, and piperidine. Carbon-14 content was measured in urine, feces, and exhaled gases over 48 hours. Carbon-14 activity in the intestine, liver, and carcass was measured. Metabolites in urine samples were analyzed. Results showed that compounds such as dihydrosafrole, safrole, myristole, and piperidine were primarily metabolized via the oxidative metabolism of the methylene groups in MDP, generating radiolabeled carbon dioxide. The radiolabeled compounds, ultimately appearing as carbon dioxide, were first released as radioformates. Carbon dioxide was not the primary elimination pathway for piperidine, piperonal, piperic acid, and topiramate. Their metabolites were mainly excreted in urine. No significant species differences were observed in the distribution of carbon-14 in tissues after administration of topiramate and piperidine. Oxidation or conjugation of the side chain is the major metabolic pathway for topiramate, piperaldehyde, piperyl alcohol, and piperic acid. Urinary metabolites of piperyl butyl ether include many compounds lacking the MDP moiety, as well as small amounts of 6-propyl piperic acid and its glycine conjugate. Urinary metabolites of topiramate include glycine and glucuronic acid conjugates of piperic acid. In an in vitro experiment, radiolabeled piperyl butyl ether, topiramate, safrole, and other MDP compounds were incubated with mouse liver microsomes, and their metabolites were detected. Metabolites such as formic acid and catechol were detected. The authors concluded that demethylation of the MDP moiety is the major metabolic pathway following administration of piperyl butyl ether, safrole, dihydrosafrole, and myristole to mammals.
After oral administration of piperine (170 mg/kg) to rats, metabolites in bile and urine were detected using thin-layer chromatography, high-performance liquid chromatography, and gas chromatography-mass spectrometry. Four piperine metabolites, namely piperic acid, piperidine, piperaldehyde, and vanillic acid, were identified in urine from 0 to 96 hours, while piperic acid was detected only in bile from 0 to 6 hours. …
Neolignan Brunner is a natural compound that reduces urinary excretion in kissing bug larvae (Rhodnius prolixus, the vector of Chagas disease), but it is rapidly degraded in the insect's hemolymph. Studies have shown that the main product accumulating in this tissue is piperidine. Other metabolites have been identified by gas chromatography-mass spectrometry analysis.

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The pharmacokinetic properties of piperonyl alcohol have not been characterized, as the compound is not intended for in vivo administration. As a small molecule with a molecular weight of 152.15 and a benzodioxole structure, it would be expected to be absorbed if administered orally and metabolized in the liver. However, no specific PK data are available.

Toxicity Summary
Identification and Uses: Piperanol is a benzodioxane derivative. It is biocompatible and can be used as an initiator in chemical synthesis. Human Studies: No data available. Animal Studies: In mice, rats, or hamsters, the main metabolic pathway of piperinol is the oxidation or conjugation of its side chain.

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The toxicity profile of piperonyl alcohol has not been systematically evaluated. As a benzodioxole derivative, it may have low toxicity, but this has not been confirmed in controlled toxicology studies. Standard safety precautions for handling organic chemicals should be observed. No specific toxicity data are available.

[1]. Lima GDS, et al. Long-term bonding efficacy of adhesives containing benzodioxioles as alternative co-initiators. Braz Oral Res. 2018;32:e104. Published 2018 Oct 11.

Piperonol belongs to the benzodioxane class of compounds.

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Piperonyl alcohol is a benzodioxole derivative used as a chemical reagent, synthetic intermediate, and fragment molecule for drug design. It has the molecular formula C8H8O3 and a molecular weight of 152.15. The compound is biocompatible and can be used as an initiator in chemical synthesis. Piperonyl alcohol is not a therapeutic agent and is not approved for clinical use. It is available only for research purposes.

C8H8O3

152.15

152.047

495-76-1

10322

Needles from petroleum ether
White to yellow powder, crystals or chunks

1.3±0.1 g/cm3

282.2±9.0 °C at 760 mmHg

50-54 °C(lit.)

124.5±18.7 °C

0.0±0.6 mmHg at 25°C

1.595

0.9

1

3

1

11

137

0

O1C([H])([H])OC2C([H])=C([H])C(C([H])([H])O[H])=C([H])C1=2

BHUIUXNAPJIDOG-UHFFFAOYSA-N

InChI=1S/C8H8O3/c9-4-6-1-2-7-8(3-6)11-5-10-7/h1-3,9H,4-5H2

1,3-benzodioxol-5-ylmethanol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO: 100 mg/mL (657.25 mM）

Solubility in Formulation 1: ≥ 2.5 mg/mL (16.43 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.

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Solubility in Formulation 2: 2.5 mg/mL (16.43 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
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.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (16.43 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)