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  3. Puberulin

Puberulin is a coumarin compound and an orally effective analgesic. Puberulin is present in Choisya ternata var. Sundance. Puberulin exerts analgesic activity against chemical and heat-induced pain agents in mouse models, and this activity does not involve opioid receptors or muscarinic receptors. Puberulin can be used in the research of neuropathic pain.

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Puberulin

Puberulin Chemical Structure

CAS No. : 57419-60-0

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Description

Puberulin is a coumarin compound and an orally effective analgesic. Puberulin is present in Choisya ternata var. Sundance. Puberulin exerts analgesic activity against chemical and heat-induced pain agents in mouse models, and this activity does not involve opioid receptors or muscarinic receptors. Puberulin can be used in the research of neuropathic pain[1].

In Vitro

Puberulin (25-300 μg/mL) exhibits good linearity in HPLC quantification, as demonstrated by a regression coefficient greater than 0.99[1].
Puberulin is successfully isolated as a colourless crystalline solid from Choisya ternata var. Sundance ethanol extract using countercurrent chromatography, with purity confirmed by HPLC[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Puberulin (0.3-10 mg/kg; p.o.; single dose) exhibits dose-dependent antinociceptive activity against formalin-induced neurogenic pain in male Swiss Webster mice, with a maximum 68% reduction in paw-licking duration at the 10 mg/kg oral dose[1].
Puberulin (0.3-10 mg/kg; p.o.; single dose) exerts antinociceptive activity against glutamate (HY-14608)-induced pain in male Swiss Webster mice at oral doses of 0.3 mg/kg and 1 mg/kg, but not at 10 mg/kg[1].
Puberulin (10 mg/kg; p.o.; single dose) does not exhibit antinociceptive activity against capsaicin-induced pain in male Swiss Webster mice at the 10 mg/kg oral dose[1].
Puberulin (0.3-10 mg/kg; p.o.; single dose) exhibits central antinociceptive activity in male Swiss Webster mice across oral doses of 0.3 mg/kg, 1 mg/kg, and 10 mg/kg, significantly increasing hot plate nociception thresholds[1].
Puberulin (1 mg/kg; p.o.; single dose) exhibits central antinociceptive activity in male Swiss Webster mice at the 1 mg/kg oral dose that is not mediated by opioid receptors, as naloxone does not inhibit its effect[1].
Puberulin (1 mg/kg; p.o.; single dose) exhibits central antinociceptive activity in male Swiss Webster mice at the 1 mg/kg oral dose that is not mediated by muscarinic receptors, as atropine does not inhibit its effect[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Swiss Webster (male, 2 months old, 20-25 g, formalin-induced acute pain model)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Reduced formalin-induced neurogenic nociception by 62% at 0.3 mg/kg, 53% at 1 mg/kg, and 68% at 10 mg/kg.
Did not affect the inflammatory pain phase (15-30 minutes post-formalin injection).
Animal Model: Swiss Webster (male, 2 months old, 20-25 g, glutamate-induced nociception model)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Inhibited glutamate-induced nociception at 0.3 mg/kg and 1 mg/kg.
Showed no effect at 10 mg/kg.
Animal Model: Swiss Webster (male, 2 months old, 20-25 g, hot plate thermal nociception model)[1]
Dosage: 0.3 mg/kg; 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Significantly increased the nociception threshold, as shown by elevated AUC values relative to vehicle control at 0.3 mg/kg, 1 mg/kg, and 10 mg/kg.
Animal Model: Swiss Webster (male, 2 months old, 20-25 g, hot plate thermal nociception model, muscarinic receptor mechanism assessment)[1]
Dosage: 1 mg/kg
Administration: p.o.; single dose
Result: Atropine (muscarinic receptor antagonist) did not interfere with the antinociceptive effect, as shown by no significant difference in AUC between puberulin-only and puberulin+atropine groups.
Molecular Weight

290.31

Formula

C16H18O5

CAS No.
SMILES

O=C1OC2=C(C=C1)C=C(OC)C(OC/C=C(C)/C)=C2OC

Structure Classification
Initial Source
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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Puberulin
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