Detail of "118288-08-7"

CAS Number:
118288-08-7
Name:
Lafutidine
Molecular Structure:
Formula:
C₂₂H₂₉N₃O₄S
Molecular Weight:
431.54836 [g/mol]
Deleted CAS:
143375-16-0
Synonyms:
Acetamide,2-[(2-furanylmethyl)sulfinyl]-N-[(2Z)-4-[[4-(1-piperidinylmethyl)-2-pyridinyl]oxy]-2-butenyl]-,(+)- (9CI);Acetamide,2-[(2-furanylmethyl)sulfinyl]-N-[4-[[4-(1-piperidinylmethyl)-2-pyridinyl]oxy]-2-butenyl]-,(Z)-(+)-;(+)-2-(Furfurylsulfinyl)-N-[(Z)-4-[[4-(piperidinomethyl)-2-pyridyl]oxy]-2-butenyl]acetamide;(+)-Lafutidine;FRG 8813;Protecadin;Stogar;
Density:
1.252 g/cm³
Boiling Point:
704.2 °C at 760 mmHg
Flash Point:
379.7 °C

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Reference

Effect of omeprazole 10 mg on intragastric pH in three different CYP2C19 genotypes, compared with omeprazole 20 mg and lafutidine 20 mg, a new H2-receptor antagonist: Effect of omeprazole 10 mg on intragastric pH in three different CYP2C19 genotypes, compared with omeprazole 20 mg and lafutidine 20 mg, a new H2-receptor antagonist. Shimatani, T.; Inoue, M.; Kuroiwa, T.; Horikawa, Y.; Mieno, H.; Nakamura, M. (Department of General Medicine, Hiroshima University Hospital, Hiroshima, Japan). Alimentary Pharmacology and Therapeutics, 18(11/12), 1149-1157 (English) 2003 Blackwell Publishing Ltd. CODEN: APTHEN. 330589-90-7 and 118288-08-7 which are cas registry numbers are also used here. ISSN: 0269-2813. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Omeprazole 10 mg is used as maintenance therapy for gastro-esophageal reflux disease, but previous reports have not mentioned the potency of its acid suppression. The aim of this study was to evaluate the potency of acid suppression with omeprazole 10 mg, in relation to CYP2C19 genotypes. Eighteen healthy subjects without Helicobacter pylori participated. After a 7-day regimen of omeprazole 10 mg, 20 mg, lafutidine 20 mg (a novel H2-receptor antagonist) or water only (baseline data), intragastric pH was measured for 24 h. With omeprazole 10 mg, greater differences were obsd. than 20 mg in median pH values and pH > 4 holding time ratios between poor metabolizers (PMs, n = 6) and the others [homozygous extensive metabolizers (homo-EMs, n = 6) and heterozygous extensive metabolizers (hetero-EMs, n = 6)]. With lafutidine 20 mg, these parameters were not influenced by the genotype. The potency of acid suppression was: omeprazole 20 mg u lafutidine 20 mg > omeprazole 10 mg in homo-EMs, omeprazole 20 mg > omeprazole 10 mg u lafutidine 20 mg in hetero-EMs, and omeprazole 20 mg u omeprazole 10 mg > lafutidine 20 mg in PMs. Omeprazole 10 mg strongly suppresses acid secretion, but depending on the CYP2C19 genotypes shows greater interindividual variations in suppression than 20 mg. .

Protective effect of lafutidine, a novel H2-receptor antagonist, on reflux esophagitis in rats through capsaicin-sensitive afferent neurons: Protective effect of lafutidine, a novel H2-receptor antagonist, on reflux esophagitis in rats through capsaicin-sensitive afferent neurons. Nagahama, Kenji; Yamato, Masanori; Kato, Shinichi; Takeuchi, Koji ( Department of Pharmacology and Experimental Therapeutics, Kyoto Pharmaceutical University, Kyoto 607-8414, Japan). Journal of Pharmacological Sciences (Tokyo, Japan), 93(1), 55-61 (English) 2003 Japanese Pharmacological Society. CODEN: JPSTGJ. ISSN: 1347-8613. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) We examd. the effect of lafutidine, a novel histamine H2-receptor antagonist, on acid reflux esophagitis in rats in relation to capsaicin-sensitive afferent neurons. The esophagitis was induced in rats by ligating both the pylorus and forestomach for 4 h. Lafutidine (1-30 mg/kg) and cimetidine (100 mg/kg) were administered either intragastrically or intraduodenally, while capsaicin (1-30 mg/kg) was administered intragastrically after the dual ligation. Intragastrical administered lafutidine at > 3 mg/kg significantly prevented the hemorrhagic esophageal damage induced by the dual ligation, and this effect was mimicked by neither capsaicin nor cimetidine given intragastrically, but totally abolished by sensory deafferentation. 404-86-4 and 118288-08-7 are cas registry numbers of chemicals which are used as reagents here. In contrast, lafutidine and cimetidine given intraduodenally were both protective against the esophageal damage in a sensory deafferentation-resistant manner. The acid secretion in pylorus-ligated stomachs was significantly inhibited by these agents given intraduodenally, but not intragastrically. Vanilloid receptor subtype 1 (VR1) was expressed abundantly in the stomach, but very weakly expressed in the esophagus as assessed by Western blotting. These results suggest that lafutidine is effective against the esophageal lesions induced by acid reflux through inhibition of acid secretion and capsaicin-sensitive afferent neurons. The latter mechanism, not shared by cimetidine, may be due to the interaction of lafutidine with unidentified sites on sensory neurons other than VR1. .

Detail of "118288-08-7"

Lafutidine

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Reference