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SC 41930
leukotriene B4 receptor antagonist; structure in first source
Also Known As:
2H-1-Benzopyran-2-carboxylic acid, 7-(3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy)-3,4-dihydro-8-propyl-; 7-(3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy)-3,4-dihydro-8-propyl-2H-1-benzopyran-2-carboxylic acid; SC-41930
Networked:
17
relevant articles (
2
outcomes,
2
trials/studies)
Relationship Network
Bio-Agent Context: Research Results
Heterocyclic Compounds: 198
1-Ring Heterocyclic Compounds
Pyrans: 130
Benzopyrans: 195
SC 41930: 17
Fused-Ring Heterocyclic Compounds
2-Ring Heterocyclic Compounds
Benzopyrans: 195
SC 41930: 17
Related Diseases
1.
Inflammation (Inflammations)
11/01/1990 - "
These data indicate that SC-41930 is effective locally to prevent acute colonic inflammation.
"
12/01/1990 - "
The PMA-induced skin inflammation model also was assessed histologically and revealed acanthosis, edema, PMNL infiltration, and rete ridge prominence as long as 96 h after a single application that was completely inhibited by SC-41930 topical coapplication.
"
12/01/1990 - "
When coapplied topically with A23187 or PMA, SC-41930 significantly inhibited epidermal inflammation with ED50 values of 0.6 and 4 mg, respectively.
"
11/01/1990 - "
Effect of the leukotriene B4 receptor antagonist SC-41930 on colonic inflammation in rat, guinea pig and rabbit.
"
06/01/1989 - "
The effect of leukotriene-B4 receptor antagonist, SC-41930, on acetic acid-induced colonic inflammation.
"
2.
Colitis
01/01/1993 - "
However, SC-41930 produced histological evidence (reduced numbers of polymorphonuclear cells) of anti-colitic efficacy over an eight-week treatment period in CTTs with persistent active colitis.
"
01/01/1993 - "
To evaluate anti-colitic efficacy, eight cotton-top tamarins (CTTs) with histologically confirmed persistent active colitis were given the anti-inflammatory agent SC-41930 (10 mg/kg BW by gavage BID) for eight weeks.
"
01/01/1993 - "
Reduced LTB4 (PMN degranulation and chemotaxis) and increased PGE2 (mucosal-protective effect) may, in part, explain the observed efficacy of SC-41930 in active tamarin colitis.
"
01/01/1993 - "
To evaluate anti-colitic efficacy, the leukotriene B4 receptor antagonist and anti-inflammatory agent, SC-41930, was administered (10 mg/kg BW by gavage BID) for 8 weeks to CTTs with histologically confirmed persistent and defined active colitis.
"
04/01/1992 - "
Mucin purified from additional animals with hapten-induced colitis but treated with the oral leukotriene B4-receptor antagonist SC-41930 showed intermediate inhibition of RDEC-1 binding (35.6% +/- 14.3%).
"
3.
Psoriasis (Pustulosis Palmaris et Plantaris)
12/01/1990 - "
These models possess many of the characteristics of human psoriasis, and agents such as SC-41930 that demonstrate activity in these models may well have therapeutic utility in the treatment of human psoriasis.
"
12/01/1989 - "
SC-41930, 7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)-propoxy]- 3,4-dihydro-8-propyl-2H-1-benzopyran-2-carboxylic acid, given intragastrically inhibited 12(R)-HETE-induced neutrophil infiltration of the cavine dermis with an ED50 value of 13.5 mg/kg. Compounds such as SC-41930 may well have utility for treating human psoriasis.
"
01/01/1993 - "
SC-41930, 7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4- dihydro-8-propyl-2H-1-benzopyran-2-carboxylic acid, is a selective, orally active, LTB4 receptor antagonist currently in clinical trials for psoriasis and ulcerative colitis.
"
04/01/1995 - "
SC-41930 (7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxyl]-3,4-dihy dro-8-propyl-2H - 1-benzopyran-2-carboxylic acid), a first-generation LTB4 receptor antagonist, inhibited the chemotactic actions of LTB4 when given orally with an ED50 value of 1.7 mg/kg. The second-generation LTB4 receptor antagonist, SC-53228 [(+)-(S)-7-(3-(2-(cyclopropylmethyl)-3-methoxy-4- [(methylamino)carbonyl]phenoxy)propoxy)-3,4-dihydro-8-propyl-2H-1- benzopyran-2-propanoic acid], inhibited LTB4-induced chemotaxis when given intragastrically with an ED50 value of 0.07 mg/kg. Furthermore, SC-53228 inhibited 12(R)-HETE-induced granulocyte chemotaxis with an oral ED50 value of 5.8 mg/kg. When dosed orally over a range of 0.03-100 mg/kg, SC-53228 gave Cmax plasma concentrations of 0.015-41.1 micrograms/ml. SC-53228 inhibited LTB4-primed membrane depolarization of human neutrophils with an IC50 value of 34 nM. As a potent LTB4 receptor antagonist, SC-53228 may well have application in the medical management of disease states such as asthma, rheumatoid arthritis, inflammatory bowel disease, contact dermatitis, and psoriasis, in which LTB4 and/or 12(R)-HETE are implicated as inflammatory mediators.
"
4.
Ulcerative Colitis
01/01/1993 - "
SC-41930, 7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4- dihydro-8-propyl-2H-1-benzopyran-2-carboxylic acid, is a selective, orally active, LTB4 receptor antagonist currently in clinical trials for psoriasis and ulcerative colitis.
"
5.
Edema (Dropsy)
09/01/1994 - "
Topically applied SC-41930 attenuated TPA-induced edema and neutrophil influx in a dose-related manner.
"
12/01/1990 - "
The PMA-induced skin inflammation model also was assessed histologically and revealed acanthosis, edema, PMNL infiltration, and rete ridge prominence as long as 96 h after a single application that was completely inhibited by SC-41930 topical coapplication.
"
Related Drugs and Biologics
1.
Leukotriene B4
2.
Leukotriene B4 Receptors (Leukotriene B4 Receptor)
3.
Dinoprostone (PGE2)
4.
Acids
5.
Carboxylic Acids
6.
Benzopyrans
7.
Anti-Inflammatory Agents (Anti-Inflammatories)
8.
7- (3- (2- (cyclopropylmethyl)- 3- methoxy- 4- ((methylamino)carbonyl)phenoxy)propoxy)- 3,4- dihydro- 8- propyl- 2H- 1- benzopyran- 2- propanoic acid
9.
Calcium Ionophores
10.
Mesalamine (Mesalazine)