Nizatidine

Modify Date: 2024-01-03 01:51:31

Nizatidine Structure
Nizatidine structure
 Common Name Nizatidine
CAS Number 76963-41-2 Molecular Weight 331.457
Density 1.2±0.1 g/cm3 Boiling Point 478.2±45.0 °C at 760 mmHg
Molecular Formula C12H21N5O2S2 Melting Point 130-132ºC
MSDS Chinese USA Flash Point 243.0±28.7 °C
Symbol GHS07
GHS07		 Signal Word Warning

 Use of Nizatidine


Nizatidine is a histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion.Target: Histamine H2 ReceptorNizatidine, a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion, with IC50 of 0.9 nM. 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 also reversibly inhibits acetylcholinesterase (AChE), with IC50 of 6.7 μM, and the inhibition is noncompetitive, with a Ki value of 7.4 μM. 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].

 Names

Name nizatidine
Synonym More Synonyms

 Nizatidine Biological Activity

Description Nizatidine is a histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion.Target: Histamine H2 ReceptorNizatidine, a selective histamine H2-receptor antagonist, is a potent inhibitor of gastric acid secretion, with IC50 of 0.9 nM. 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 also reversibly inhibits acetylcholinesterase (AChE), with IC50 of 6.7 μM, and the inhibition is noncompetitive, with a Ki value of 7.4 μM. 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].
Related Catalog
References

[1]. Lin, T.M., et al., Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs. J Pharmacol Exp Ther, 1986. 239(2): p. 406-10.

[2]. Ueki, S., et al., Gastroprokinetic activity of nizatidine, a new H2-receptor antagonist, and its possible mechanism of action in dogs and rats. J Pharmacol Exp Ther, 1993. 264(1): p. 152-7.

 Chemical & Physical Properties

Density 1.2±0.1 g/cm3
Boiling Point 478.2±45.0 °C at 760 mmHg
Melting Point 130-132ºC
Molecular Formula C12H21N5O2S2
Molecular Weight 331.457
Flash Point 243.0±28.7 °C
Exact Mass 331.113678
PSA 139.55000
LogP 1.18
Vapour Pressure 0.0±1.2 mmHg at 25°C
Index of Refraction 1.592
Storage condition -20?C Freezer

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
KM6565000
CHEMICAL NAME :
1,1-Ethenediamine, N-(2-(((2-((dimethylamino)methyl)-4-thiazolyl)methyl) thio)ethyl)-N'- methyl-2-nitro-
CAS REGISTRY NUMBER :
76963-41-2
LAST UPDATED :
199806
DATA ITEMS CITED :
18
MOLECULAR FORMULA :
C12-H21-N5-O2-S2
MOLECULAR WEIGHT :
331.50

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1653 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,920,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>2 gm/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - coma Gastrointestinal - hypermotility, diarrhea
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
301 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - coma Gastrointestinal - hypermotility, diarrhea
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1630 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,920,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1082 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - coma Gastrointestinal - hypermotility, diarrhea
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
232 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,920,1995
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>800 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) Gastrointestinal - nausea or vomiting
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>75 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - nausea or vomiting
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>225 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - tetany Gastrointestinal - nausea or vomiting
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>1200 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Primate - monkey
DOSE/DURATION :
>200 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - tremor Gastrointestinal - nausea or vomiting
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
51415 mg/kg/13W-I
TOXIC EFFECTS :
Endocrine - changes in thymus weight Blood - change in clotting factors Blood - pigmented or nucleated red blood cells
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,525,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
91 gm/kg/26W-C
TOXIC EFFECTS :
Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
146 gm/kg/1Y-C
TOXIC EFFECTS :
Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
164 gm/kg/91D-C
TOXIC EFFECTS :
Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
73 gm/kg/91D-I
TOXIC EFFECTS :
Liver - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
146 gm/kg/1Y-I
TOXIC EFFECTS :
Liver - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes
REFERENCE :
FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
16500 mg/kg
SEX/DURATION :
female 7-17 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - sex ratio
REFERENCE :
YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,547,1989

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Precautionary Statements P301 + P312 + P330
Hazard Codes Xn
Risk Phrases R22
Safety Phrases S36
RIDADR NONH for all modes of transport
WGK Germany 3
RTECS KM6565000
HS Code 2934999090

 Synthetic Route

A9LS0UV4E3 structure

A9LS0UV4E3

CAS#:102721-76-6

2-(((2-((Dimethylamino)methyl)thiazol-4-yl)methyl)thio)ethanamine structure

2-(((2-((Dimeth...

CAS#:78441-62-0

~78%

Nizatidine Structure

Nizatidine

CAS#:76963-41-2

Literature: KUMAR, Dinesh, R. Patent: WO2004/69817 A1, 2004 ; Location in patent: Page 8,9 ;

 Precursor & DownStream

Precursor  1

DownStream  0

 Customs

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Articles32

More Articles
Impact of sleep disorders in Japanese patients with functional dyspepsia (FD): nizatidine improves clinical symptoms, gastric emptying and sleep disorders in FD patients.

J. Gastroenterol. Hepatol. 28(8) , 1314-20, (2013)

The association between functional dyspepsia (FD) and sleep disorders has yet to be studied in detail. The aim of this study is to evaluate the risk factors associated with sleep disorders and the cli...

[Nizatidine].

Medicina (Firenze.) 9(1) , 93-6, (1989)

Nizatidine is a new H2-receptor antagonist, as potent as ranitidine. It does not interfere with hepatic metabolism and it lacks anti-androgenic effects. An evening dose of 300 mg suppresses nocturnal ...

Nizatidine improves clinical symptoms and gastric emptying in patients with functional dyspepsia accompanied by impaired gastric emptying.

Digestion 86(2) , 114-21, (2012)

In this crossover study, we investigated whether nizatidine, a H(2)-receptor antagonist, can alleviate clinical symptoms and gastric emptying in patients with Rome III-based functional dyspepsia (FD) ...

 Synonyms

Tazac
N-{2-[({2-[(Dimethylamino)methyl]-1,3-thiazol-4-yl}methyl)sulfanyl]ethyl}-N'-methyl-2-nitroethene-1,1-diamine
Acinon
(E)-1-N'-[2-[[2-[(dimethylamino)methyl]-1,3-thiazol-4-yl]methylsulfanyl]ethyl]-1-N-methyl-2-nitroethene-1,1-diamine
Nizax
N-[2[[[2-[(dimethylamino)methyl]-4-thiazolyl]methyl]thio]ethyl]-N'-methyl-2-nitro-1,1-ethenediamine
Cronizat
Axid
N-{2-[({2-[(Dimethylamino)methyl]-1,3-thiazol-4-yl}methyl)sulfanyl]ethyl}-N'-methyl-2-nitro-1,1-ethenediamine
MFCD00865660
Galitidin
Distaxid
1,1-Ethenediamine, N-[2-[[[2-[(dimethylamino)methyl]-4-thiazolyl]methyl]thio]ethyl]-N'-methyl-2-nitro-
Nizatidine
Zanizal
Calmaxid
1,1-Ethenediamine, N-(2-(((2-((dimethylamino)methyl)-4-thiazolyl)methyl)thio)ethyl)-N'-methyl-2-nitro-
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Nizatidine Sulfoxide
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Desmethyl Nizatidine
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DES(N'-METHYL-2-NITRO-1,1-ETHENEDIAMINO) N'-METHYLUREIDO NIZATIDINE
82586-81-0
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930439-75-1
4,5,6,7-Tetrahydrobenzo[d]isoxazole-3-carbaldehyde
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3-Cyano-6-methoxyindole-1-carboxylic acid tert-butyl ester
876743-01-0
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1375289-11-4
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