Nizatidine

Catalog No.S1890

Nizatidine Chemical Structure

Molecular Weight(MW): 331.46

Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.

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Biological Activity

Description Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
Targets
Histamine H2 receptor [1] AChE [2]
0.9 nM 6.7 μM
In vitro

Nizatidine, a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion, with IC50 of 0.9 nM. [1] Nizatidine also reversibly inhibits acetylcholinesterase (AChE), with IC50 of 6.7 μM, and the inhibition is noncompetitive, with a Ki value of 7.4 μM. [2]

In vivo Nizatidine exhibits maximal inhibition of gastric acid in rats within the first hour of drug administration, with EC50 of 1.383 μmol/kg. [1] Nizatidine (0.3-3 mg/kg, i.v.) significantly increases the motor index of gastrointestinal (GI) motility in a dose-dependent manner. Nizatidine inhibits gastric acid secretion with ED50 and ED90 of 0.18 and 3.22 mg/kg in dogs, and 2.94 and 19.6 mg/kg in rats, respectively. [2]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Rat
  • Formulation: saline
  • Dosages: 0.5-10 μmol/kg
  • Administration: s.c
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 66 mg/mL (199.11 mM)
Water 28 mg/mL (84.47 mM)
Ethanol 18 mg/mL (54.3 mM)
In vivo Add solvents to the product individually and in order:
Saline
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 331.46
Formula

C12H21N5O2S2

CAS No. 76963-41-2
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02232308 Completed Gastroparesis Adil Bharucha|National Center for Research Resources (NCRR)|National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK)|Mayo Clinic July 2014 Phase 1
NCT01409395 Completed Healthy University of California, San Francisco|National Institute of General Medical Sciences (NIGMS) September 2011 Phase 1
NCT02555852 Completed Gastroesophageal Reflux Disease (GERD)|Community-acquired Pneumonia Canadian Network for Observational Drug Effect Studies, CNODES|Drug Safety and Effectiveness Network, Canada|Canadian Institutes of Health Research (CIHR) September 2011 --
NCT00373334 Completed Gastroesophageal Reflux Disease|GERD|Heartburn Braintree Laboratories August 2006 Phase 3
NCT01161940 Completed Healthy Dr. Reddys Laboratories Limited July 2004 Phase 1
NCT01161927 Completed Healthy Dr. Reddys Laboratories Limited July 2004 Phase 1

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Histamine Receptor Signaling Pathway Map

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