Zolantidine
Zolantidine (SKF 95282) is a potent, selective and cross the blood-brain barrier histamine H2 antagonist. Zolantidine induces antinociception.
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- CAS No.: 104076-38-2
- Formule: C22H27N3OS
- Masse moléculaire:381.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
H2 Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
76 μM
Compound: Zolantidine
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Cytotoxicity activity against human HepG2 cells after 24 hrs
Cytotoxicity activity against human HepG2 cells after 24 hrs
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[PMID: 20547797] |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:200-250 g, male Wistar rats (cholestatic rats)[2]
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Dosage:5, 10, 20, 40 mg/kg
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Administration:S.c.
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Result:Significantly increased tail-flick latencies and induced antinociception.
Chemical Information
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CAS No. 104076-38-2
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Masse moléculaire 381.53
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Formule C22H27N3OS
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SMILES
C1(NCCCOC2=CC=CC(CN3CCCCC3)=C2)=NC4=CC=CC=C4S1
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Synonyms
SK&F 95282
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Formalin-Induced Paw Inflammation/Nociceptive Inflammation
The formalin-induced paw inflammation/nociceptive test is a chemical persistent pain model in rodents in which subcutaneous injection of formalin into the hind paw produces spontaneous nocifensive behaviors such as flinching and licking. The response is classically biphasic, consisting of an early acute phase (Phase I) reflecting direct activation of peripheral nociceptors (particularly C-fiber afferents), followed by a later prolonged phase (Phase II) associated with central sensitization in the spinal dorsal horn driven by sustained afferent input and inflammatory signaling. This model is widely used to evaluate analgesic and anti-inflammatory interventions because it captures both peripheral nociception and central sensitization processes within a single assay system.
Pureté et documentation
Références
[1]. Calcutt CR, et al. Zolantidine (SK&F 95282) is a potent selective brain-penetrating histamine H2-receptor antagonist. Br J Pharmacol. 1988 Jan;93(1):69-78. [Content Brief]
[2]. Hasanein P. Two histamine H2 receptor antagonists, zolantidine and cimetidine, modulate nociception in cholestatic rats. J Psychopharmacol. 2011 Feb;25(2):281-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Zolantidine Related Classifications
HY-101373 Related Classifications
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