88107-10-2 Usage
Description
LY-171883 (88107-10-2) is a selective and orally active leukotriene D4 (LTD4) antagonist (Ki = 0.63 μM).1 It is also an activator of peroxisome proliferator-activated receptors (PPARs).2,3
Uses
LY 171883 is a selective leukotriene D4 antagonist.
Definition
ChEBI: A member of the class of acetophenones that is 1-phenylethanone substituted at position 2 by a hydroxy group, a propyl group at position 3 and a 4-(1H-tetrazol-5-yl)butoxy group at position 4. A leukotriene antagonist, it exhibits anti
asthmatic activity.
Biological Activity
Selective, orally active leukotriene D 4 (LTD 4 ) antagonist; inhibits binding of [ 3 H]-LTD 4 to guinea pig lung membranes (K i = 0.63 μ M).? Acts as an agonist at peroxisome proliferator-activated receptors (PPARs).
in vitro
in gh(3) cells, ly-171883 was able to reversibly increase the amplitude of ca(2+)-activated k(+) current concentration-dependently with an ec(50) value of 15 μm. moreover, the treatment of ly-171883 to cytosolic face did not affect single channel conductance of large-conductance ca(2+)-activated k(+) channels in excised inside-out patches recorded from gh(3) cells, however, ly-171883 did increase the channel activity. in addition, the ly-171883-stimulated activity of bk(ca) channels was dependent on membrane potential [1].
in vivo
the effect of ly-171883 on the respiratory and cardiovascular changes in endotoxemia was studied in unanesthetized sheep. in group one, ly-171883 at 4 mg/kg was i.v. injected. in group two, escherichia coli endotoxin (1 μg/kg) was infused, and in group three, ly-171883 at 4 mg/kg was administered before and after the same dose of endotoxin. results showed that infusion of ly-171883 in group one did not alter baseline ventilatory and cardiovascular measurements. in group two, a two-phase pulmonary response was found. an early pulmonary hypertension phase with a fall in cardiac index was observed in group three [2].
References
1) Fleisch et al. (1985), LY171883, 1-less than 2-hydroxy-3-propyl-4-less than 4-(1H-tetrazol-5-yl)butoxy greater than phenyl greater than ethanone, an orally active leukotriene D4 antagonist; J. Pharmacol. Exp. Ther., 233 148
2) Foxworthy and Eacho (1991) Effect of the peroxisome proliferator LY171883 on triglyceride accumulation in rats fed a fat-free diet; Biochem. Pharmacol. 42 1487
3) Kliewer et al. (1994) Differential expression and activation of a family of murine peroxisome proliferator-activated receptors; Proc. Natl. Acad. Sci .USA 91 7355
Check Digit Verification of cas no
The CAS Registry Mumber 88107-10-2 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 8,8,1,0 and 7 respectively; the second part has 2 digits, 1 and 0 respectively.
Calculate Digit Verification of CAS Registry Number 88107-10:
(7*8)+(6*8)+(5*1)+(4*0)+(3*7)+(2*1)+(1*0)=132
132 % 10 = 2
So 88107-10-2 is a valid CAS Registry Number.
InChI:InChI=1/C16H22N4O3/c1-3-6-13-14(9-8-12(11(2)21)16(13)22)23-10-5-4-7-15-17-19-20-18-15/h8-9,22H,3-7,10H2,1-2H3,(H,17,18,19,20)
88107-10-2Relevant articles and documents
Disubstituted tetrazole leukotriene antagonists and methods for their use thereas
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, (2008/06/13)
The instant invention provides disubstituted tetrazoles that antagonizes the effect of leukotrienes C4, D4 or E4 or any combination thereof in selected tissues. The disubstituted tetrazoles are used in pharmaceutical formulations and methods of treatment of conditions caused by excessive release or production of leukotrienes C4, D4 or E4 or any combination thereof. Such conditions include an immediate hypersensitivity reaction of the type represented by asthma, or by shock or other adverse cardiovascular effects.
Improved conditions for the formation of tetrazoles
Bernstein,Vacek
, p. 1133 - 1134 (2007/10/02)
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