Detail of "103177-37-3"

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CAS Number:
103177-37-3
Name:
Benzamide,N-[4-oxo-2-(2H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)-
Superlist Name:
Pranlukast
Molecular Structure:
Formula:
C₂₇H₂₃N₅O₄
Molecular Weight:
481.50
Synonyms:
Benzamide,N-[4-oxo-2-(1H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)- (9CI);4-Oxo-8-[4-(4-phenylbutoxy)benzoylamino]-2-(tetrazol-5-yl)-4H-1-benzopyran;8-[4-(4-Phenylbutoxy)benzoyl]amino-2-(5-tetrazolyl)-4-oxo-4H-1-benzopyran;Azlaire;CCN 00401;ONO 1078;ONO-RS 411;Onon;RS 411;SB 205312;
EINECS:
201-616-4
Density:
1.374 g/cm³
Melting Point:
236-238 °C
Appearance:
off-white solid
Hazard Symbols:
F, C
Risk Codes:
11-34
Safety:
16-26-36/37/39-45 Details

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Reference

Effect of leukotrienes antagonist on LTD4-induced coronary spasm: Effect of leukotrienes antagonist on LTD4-induced coronary spasm. Honye, Junko (Sch. Med., Nihon Univ., Japan). 73836-78-9 and 103177-37-3 are also occured in this study. Kokyu to Junkan, 34(12), 1343-8 (Japanese) 1986. CODEN: KOJUA9. ISSN: 0452-3458. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 14 The action of Leukotriene D4 (LTE4) [73836-78-9] on coronary circulation and the effect of LT antagonist RS-411 (I) [103177-37-3] on LTD4-induced coronary spasm were evaluated in anesthetized dogs. After administering LTD4 (0.33 mg) into the left anterior descending artery(LAD), the hemodynamic parameters as well as epicardial ECG were recorded. Following pretreatment with intracoronary administration of RS-411 50 mg/kg, LTD4 (0.33 mg) was given and the same parameters were recorded. In 4 dogs, coronary angiog. (CAG) was performed to study the effect of RS-411 on LTD4-induced coronary spasm. LTD4 caused a redn. in coronary blood flow and an increase in coronary vascular resistance with a marked ST elevation on epicardial ECG. An increase in left ventricular end-diastolic pressure and a transient decrease in aortic pressure, mean coronary arterial pressure, and aortic flow were obsd. with no effect on heart rate. No change in hemodynamic parameters were shown after pretreatment with RS-411, and the duration of ST elevation was shortened. CAGs documented the total occlusion of LAD in all dogs after intracoronary administration of LTD4, but the degrees of coronary spasm were attenuated by RS-411 in each dog. These data suggest that RS-411 is effective against LTD4-induced coronary spasm. It is also indicated that LTD4 has direct coronary vasoconstrictory action and might play an important role in pathogenesis and deterioration of myocardial ischemia. .

Purification and characterization of pranlukast hydrolase from rat liver microsomes: the hydrolase is identical to carboxylesterase pI 6: Purification and characterization of pranlukast hydrolase from rat liver microsomes: the hydrolase is identical to carboxylesterase pI 6.2. Luan, Libiao; Sugiyama, Tadashi; Takai, Satomi; Usami, Yoshiko; Adachi, Tetsuo; Katagiri, Yoshihiro; Hirano, Kazuyuki (Department of Pharmaceutics, Gifu Pharmaceutical University, Gifu 502, Japan). Biological & Pharmaceutical Bulletin, 20(1), 71-75 (English) 1997 Pharmaceutical Society of Japan. CODEN: BPBLEO. ISSN: 0918-6158. DOCUMENT TYPE: Journal CA Section: 7 (Enzymes) Section cross-reference(s): 1 Two carboxylesterases with pI 6.0 and 6.2 derived from rat liver microsomes were purified. The 2 isoenzymes were markedly different in substrate specificity, but they had equal enzymic activity for a-naphthyl acetate and were inhibited equally by phenylmethylsulfonyl fluoride (PMSF) and bis-(4-nitrophenyl) phosphate (BNPP). Carboxylesterases pI 6.0 and 6.2 were found to be identical to the enzymes referred to as hydrolases A and B, resp., from the results of amino acid sequence analyses.Several substances with their cas registry numbers 9016-18-6 and 103177-37-3 may be metioned in this study. Pranlukast was effectively hydrolyzed by carboxylesterase pI 6.2, but not by the pI 6.0 enzyme, and the difference in pranlukast metab. between the human and the rat could be explained by the substrate specificity of carboxylesterase. Furthermore, prodrugs of angiotensin-converting enzyme inhibitors were found to be converted to the active drugs after hydrolysis by carboxylesterases pI 6.0 and 6.2. Carboxylesterases generally catalyzed the hydrolysis of ester-type drugs preferentially rather than amide-type drugs. .

Detail of "103177-37-3"

Benzamide,N-[4-oxo-2-(2H-tetrazol-5-yl)-4H-1-benzopyran-8-yl]-4-(4-phenylbutoxy)-

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Reference