Quisultidine
Quisultidine (LM 24056) is an orally active phenothiazine derivative with both calmodulin (Calmodulin) inhibitory activity (with a IC50 of 55 μM against porcine calmodulin) and muscarinic acetylcholine receptor (mAChR) ligand activity (with a IC50 of 400 nM). It inhibits gastric acid and pepsin secretion, reduces circulating gastrin levels, and blocks histamine-stimulated gastric acid secretion. Quisultidine can be used in the research of duodenal ulcer.
For research use only. We do not sell to patients.
- CAS No.: 64099-44-1
- Formula: C21H25N3O2S2
- Molecular Weight:415.57
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
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Calmodulin 55 μM (IC50) |
mAChR 400 nM (IC50) |
In Vitro
Quisultidine (LM 24056) inhibits basal prolactin secretion from anterior pituitary cells isolated from adult male Sprague-Dawley rats, with a mean IC50 of 57 μM[7].
Quisultidine (15 min) inhibits the activity of calmodulin-activated cyclic GMP phosphodiesterase in porcine brain, with a mean IC50 of 55 μM[7].
Quisultidine displaces the binding of [3H] QNB to muscarinic receptors in rat striatal membranes, with an IC50 of 400 nM[5].
Quisultidine exhibits rare irreversible electrooxidation behavior and does not form stable cation radicals. Its oxidation process generates the metabolite 2-(N,N-dimethylsulfamoyl) phenothiazine, which is capable of forming stable cation radicals[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Quisultidin (0.6-10 mg/kg; p.o.; single administration) inhibits gastrin-induced gastric acid secretion in Heidenhain pouch hybrid dogs, with an oral ED50 of 1 mg/kg[5].
Quisultidin (2.5 mg/kg; p.o.; 30 to 50 min before feeding) inhibits feeding-stimulated gastric acid secretion in Heidenhain pouch hybrid dogs, with a duration of action of at least 3 h[5].
Quisultidin (2.5 mg/kg; p.o.; single administration) exhibits long-acting inhibitory effect on gastrin-induced gastric acid secretion in Heidenhain pouch hybrid dogs, with an inhibition rate of 66% still maintained 20 h after dosing[5].
Quisultidin (up to 300 mg/kg; p.o.; single administration) exhibits no mydriatic activity in mice[5].
Quisultidin (100 mg/kg; p.o.; single administration) induces mydriasis in rats, with an oral ED50 of 100 mg/kg[5].
Quisultidin (1-25 mg/kg; i.p.; single administration) exhibits weak or no inhibitory effect on [3H]QNB binding to muscarinic receptors in the heart (peripheral) and striatum (central) in mice [5].
Quisultidin (30-60 mg per dog; p.o.; single administration 2 h before meal) is an effective gastric acid secretion inhibitor in Beagle dogs, in which the oral dose of 60 mg/dog completely eliminates food-induced gastric acid and pepsin secretion, and in all tested gastric stimulation models, both 30 mg/dog and 60 mg/dog doses reduce gastrin levels in a dose-dependent manner without altering histamine concentrations[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Charles River CD (female, 200-220 g, pylorus-ligated with pentagastrin stimulation)[5]
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Dosage:3 mg/kg; 10 mg/kg; 30 mg/kg
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Administration:p.o.; single dose; 1 hour prior to pylorus ligation
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Result:Inhibited pentagastrin-induced gastric acid secretion via reduction of secretory volume (with no change in titratable acidity).
Achieved an ED50 of ~3.7 mg/kg p.o. for inhibition of pentagastrin-induced hypersecretion.
Inhibited basal gastric acid secretion via reduction of secretory volume (with no change in titratable acidity).
Achieved an ED50 of ~30 mg/kg p.o. for inhibition of basal secretion.
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Animal Model:Mongrel (15-20 kg, chronic Heidenhain pouch, gastrin stimulation)[5]
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Dosage:0.6 mg/kg; 1.25 mg/kg; 2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:p.o.; single dose
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Result:Inhibited gastrin-induced gastric acid secretion via reduction of secretory volume (with no change in titratable acidity).
Achieved an ED50 of 1 mg/kg p.o. for inhibition of gastrin-induced secretion.
Caused subtotal inhibition of acid response starting 30 minutes after administration at 5 mg/kg.
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Animal Model:Mongrel (15-20 kg, chronic Heidenhain pouch, meal stimulation)[5]
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Dosage:2.5 mg/kg
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Administration:p.o.; single dose; 30 to 50 minutes before feeding
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Result:Suppressed meal-stimulated gastric acid secretion to 3-3.5% of control in the first hour, 2.4-2.6% of control in the second hour, and 4.6-5.3% of control in the third hour.
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Animal Model:Mongrel (15-20 kg, chronic Heidenhain pouch, gastrin stimulation for duration of action assessment)[5]
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Dosage:2.5 mg/kg
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Administration:p.o.; single dose
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Result:Inhibited gastrin-induced acid secretion by 90% when given 4 or 11 hours pre-infusion, 73% when given 16 hours pre-infusion, 66% when given 20 hours pre-infusion, and showed reduced inhibition when given 24 hours pre-infusion.
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Animal Model:Beagle (10-12 kg, fasted 18 hours before experiments; Heidenhain denervated pouch-equipped)[6]
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Dosage:30 mg/dog; 60 mg/dog
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Administration:p.o.; single dose 2 hours before meal
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Result:Completely eliminated food-induced gastric acid and pepsin secretion in the oral dose of 60 mg/dog, and in all tested gastric stimulation models, both 30 mg/dog and 60 mg/dog doses reduce gastrin levels in a dose-dependent manner without altering histamine concentrations.
Chemical Information
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CAS No. 64099-44-1
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Molecular Weight 415.57
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Formula C21H25N3O2S2
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SMILES
O=S(C1=CC=C(SC2=C3C=CC=C2)C(N3C4CN5CCC4CC5)=C1)(N(C)C)=O
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Synonyms
LM 24056
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Purity & Documentation
References
[2]. Wilson JA, et al. Inhibition of pentagastrin-stimulated and overnight gastric secretion by mianserin. British journal of clinical pharmacology. 1983;15 Suppl 2(Suppl 2):329S-333S. [Content Brief]
[4]. Kauffmann JM, et al. Unusual electrochemical behaviour of a new phenothiazine. Analyst. 1985 Apr;110(4):349-51. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Quisultidine Related Classifications
HY-124203 Related Classifications
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