| Identification | More | [Name]
Roxatidine | [CAS]
78273-80-0 | [Synonyms]
n-{3-[3-(1-piperidinylmethyl)phenoxy]propyl}hydroxyacetamide
ROXATIDINE
ROXATIDINE ENTERPRISE STANDARD
RoxatidineAcetateHclBase
ROXATIDINE(SUBJECTTOPATENTFREE)
desacetyl-TZU-0460
2-Hydroxy-N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]acetamide
2-Hydroxy-N-[3-[m-(piperidinomethyl)phenoxy]propyl]acetamide | [Molecular Formula]
C17H26N2O3 | [MDL Number]
MFCD00871807 | [Molecular Weight]
306.4 | [MOL File]
78273-80-0.mol |
| Chemical Properties | Back Directory | [Melting point ]
59-60 °C | [Boiling point ]
524.3±45.0 °C(Predicted) | [density ]
1.137±0.06 g/cm3(Predicted) | [storage temp. ]
-20° | [solubility ]
Soluble in DMSO (up to 25 mg/ml). | [form ]
oil | [pka]
13.34±0.10(Predicted) | [color ]
Colorless to pale yellow | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. | [CAS DataBase Reference]
78273-80-0(CAS DataBase Reference) |
| Hazard Information | Back Directory | [Description]
Roxatidine (78273-80-0) is a novel histamine H2 receptor antagonist.1?Suppresses inflammatory responses via inhibition of NFκB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages.2?Clinically useful agent for prevention and healing of gastric and duodenal ulcers and bleeding.3?Attenuates degradation of extracellular matrix in osteoarthritis models by inactivating the NFkB pathway.4 | [Uses]
Anti-ulcerative. | [in vivo]
Roxatidine (20 mg/kg, p.o., a single dose for 1h before Compound 48/80 injection) ameliorates Compound 48/80 (HY-115768) (8mg/kg, i.p., a single dose for 1h)-induced allergic hypersensitivity and suppresses Compound 48/80-induced allergic inflammation in anaphylactic animal model[1].
| Animal Model: | Compound 48/80-induced anaphylactic shock mouse model[1] | | Dosage: | 20 mg/kg | | Administration: | p.o., a single dose for 1h before Compound 48/80 injection | | Result: | Increased the survival rate to 20% at 60 min after compound 48/80 injection. |
| [IC 50]
H2 Receptor | [storage]
-20°C | [References]
1) Mills and Wood (1989),?The pharmacology of histamine H2-receptor antagonists; Methods Find. Exp. Clin. Pharmacol., 11 Suppl. 1?87
2) Cho?et al. (2011), Roxatidine suppresses inflammatory responses via inhibition of NF-κB and p38 MAPK activation in LPS-induced RAW 264.7 macrophages; J. Cell. Biochem.,?112?3648
3) Imaeda?et al.?(2011),?Effect of lansoprazole versus roxatidine on prevention of bleeding and promotion of ulcer healing after endoscopic submucosal dissection for superficial gastric neoplasia; J. Gastroenterol.,?46?1267
4) Ze?et al. (2017),?Roxatidine Attenuates Degradation of Extracellular Matrix;?Biomed. Pharmacother.,?95?1156 |
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