Nizatidine is a histamine type 2 receptor antagonist (H2 blocker) which is widely used for treatment of acid-peptic disease and heartburn. Nizatidine has been linked to rare instances of clinically apparent acute liver injury[3]. In rat and dog models, species in which the absorption, plasma half-life and routes of metabolism are similar to that of humans, nizatidine was three- to four-fold more active than cimetidine and was of similar potency to ranitidine. Nizatidine was well-tolerated in animals after both intravenous and oral administration and following single or repeated administration[4]. Nizatidine administration significantly improved both gastric emptying and clinical symptoms in FD (functional dyspepsia) patients with impaired gastric emptying[5]. Intravenous administration of nizatidine (0.3 - 3 mg/kg) enhanced the motility of the gastric antrum and duodenum during the digestive state. Gastric emptying of a solid test meal was accelerated by intraperitoneal administration of nizatidine (1 - 10 mg/kg) to the same extent as cisapride (0.1 - 1 mg/kg). Furthermore, nizatidine improved clonidine-induced delayed gastric emptying[6].
Nizatidine/尼扎替丁 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HuH-7
10 μM
48 hours
Nizatidine downregulated cccDNA levels
Biomolecules. 2023 Sep 24;13(10):1438.
THP1-derived macrophages
20 µM
48 hours
Decreased pro-inflammatory cytokine expression
Nat Commun. 2021 Sep 17;12(1):5525.
Huh7.5.1dif cells
10 µM
48 hours
Reversed the HCV-induced poor-prognosis PLS status
Nat Commun. 2021 Sep 17;12(1):5525.
Caco-2 cells
0.05–10 mM
120 minutes
To investigate the intestinal epithelial cell efflux transport mechanisms of nizatidine, it was found that nizatidine exhibited 7.7-fold higher BL–AP than AP–BL Caco-2 permeability, indicative of net mucosal secretion. All P-gp inhibitors displayed concentration-dependent inhibition.
AAPS J. 2009 Jun;11(2):205-13.
Caco-2 cells
3.13, 6.25, 12.5 μg/mL
24 hours
To evaluate the biocompatibility of nanofibers and the removal of unreacted glutaraldehyde. Results showed that the viability of Caco-2 cells was 86.87 ± 6.86%, indicating good biocompatibility of the nanofibers.
Drug Deliv. 2021 Aug 24;28(1):1795-1809.
Rat erythrocytes
1.4×10^-6M
To determine the inhibitory activity of nizatidine on acetylcholinesterase (AChE)
World J Gastroenterol. 2000 Oct;6(5):651-658.
RAW264.7 cell line
6 μg/ml
48 hours
To evaluate the effect of Nizatidine on APC activation, results showed upregulated expression levels of MHC II, CD40, and CD80
Hum Vaccin Immunother. 2014;10(2):461-8.
DC2.4 cell line
6 μg/ml
48 hours
To evaluate the effect of Nizatidine on APC activation, results showed increased expression levels of MHC II and CD40
Hum Vaccin Immunother. 2014;10(2):461-8.
RAW264.7 cell line
6 μg/ml
48 hours
To evaluate the effect of Nizatidine on APC activation, results showed upregulation of MHC II, CD40, and CD80
Hum Vaccin Immunother. 2014;10(2):461-8.
DC2.4 cell line
6 μg/ml
48 hours
To evaluate the effect of Nizatidine on APC activation, results showed increased levels of MHC II and CD40
Hum Vaccin Immunother. 2014;10(2):461-8.
Nizatidine/尼扎替丁 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Rat
DEN-induced fibrosis and HCC model
Oral gavage
15 mg/kg
Daily for 9 weeks
Reduced liver fibrosis and HCC development
Nat Commun. 2021 Sep 17;12(1):5525.
Rats
Ethanol-induced gastric injury model
Oral
30 mg/kg
5 consecutive days
To evaluate the gastroprotective effect of nizatidine nanofibers against ethanol-induced gastric injury. Results showed that crosslinked nanofibers significantly enhanced the gastroprotective activity of nizatidine and preserved the gastric wall architecture, COX-2 expression, and oxidative stress markers levels of the normal rats.
Drug Deliv. 2021 Aug 24;28(1):1795-1809.
Rats
Duodenal HCO3- secretion model
Intravenous injection
3-30mg/kg
Single dose, observed for 2 hours
To investigate the stimulatory effect of nizatidine on duodenal HCO3- secretion in rats and its mechanism
World J Gastroenterol. 2000 Oct;6(5):651-658.
C57BL/6 mice
H5N1 killed viral antigen immunization model
Intramuscular injection
0.62 mg/mice
Single immunization
To evaluate the adjuvant effect of Nizatidine on H5N1 vaccine, results showed significant improvement in animal survival and reduction in viral loads in lung tissues
Brazil
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United States, Minnesota
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Mayo Clinic in Rochester
Rochester, Minnesota, United States, 55905
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