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.
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- CAS. Nr.: 64099-44-1
- Formel: C21H25N3O2S2
- Molecular Weight:415.57
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
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Calmodulin 55 μM (IC50) |
mAChR 400 nM (IC50) |
In Vitro
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.
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. Nr. 64099-44-1
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Molecular Weight 415.57
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Quisultidine Related Classifications
HY-124203 Related Classifications
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