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N-acetyldesloratadine
dual antagonist of platelet-activating factor and histamine
Also Known As:
1-acetyl-4-(8-chloro-5,6-dihydro-11H-benzo(5,6)cycloheptal(1,2-b)pyridin-11-ylidine)piperidine; SCH-37370; Sch 37370
Networked:
4
relevant articles (
2
outcomes,
1
trials/studies)
Relationship Network
Bio-Agent Context: Research Results
Organic Chemicals: 133
Hydrocarbons: 1713
Cyclic Hydrocarbons: 97
Aromatic Hydrocarbons: 291
Polycyclic Aromatic Hydrocarbons: 2020
Benzocycloheptenes
Dibenzocycloheptenes
Cyproheptadine: 709
Loratadine: 463
N-acetyldesloratadine: 4
Heterocyclic Compounds: 198
1-Ring Heterocyclic Compounds
Piperidines: 17
Cyproheptadine: 709
Loratadine: 463
N-acetyldesloratadine: 4
Polycyclic Compounds: 6
Polycyclic Aromatic Hydrocarbons: 2020
Benzocycloheptenes
Dibenzocycloheptenes
Cyproheptadine: 709
Loratadine: 463
N-acetyldesloratadine: 4
Related Diseases
1.
Bronchial Spasm
12/01/1991 - "
Sch 37370 selectively inhibits PAF-induced aggregation of human platelets in vitro (IC50 = 0.6 microM), and in vivo inhibits PAF- and histamine-induced bronchospasm in guinea pigs with ED50 values of 6.0 and 2.4 mg/kg p.o., respectively.
"
03/01/1990 - "
Administered i.v. to guinea pigs, Sch 37370 is an equipotent antagonist of PAF and histamine-induced bronchospasm (ED50 = 0.6-0.7 mg/kg).
"
01/01/1991 - "
In addition, Sch 37370 blocks bronchospasm induced by either antigen in sensitized guinea pigs or hyperventilation in nonsensitized guinea pigs.
"
03/01/1990 - "
Orally in guinea pigs, Sch 37370 is somewhat more effective against bronchospasms to histamine (ED50 = 2.4 mg/kg) than against PAF (ED50 = 4.1-6.0 mg/kg) or serotonin (ED50 = 9.6 mg/kg).
"
01/01/1991 - "
In guinea pigs, orally administered Sch 37370 is effective against bronchospasm to histamine (ED50 = 2.4 mg/kg), PAF (ED50 = 6.0 mg/kg) or serotonin (ED50 = 9.6 mg/kg).
"
2.
Asthma (Bronchial Asthma)
12/01/1991 - "
Sch 37370 is expected to be more efficacious than single mediator antagonists in allergic diseases, such as asthma.
"
08/01/1992 - "
Preclinical studies have established that Sch 37370 (1-acetyl-4-(8-chloro-5,6-dihydro-11H-benzo[5,6]-cyclohepta [1,2-b]pyridin-11-ylidene)piperidine) is an orally active antagonist of platelet-activating factor (PAF) and histamine H1-receptors with potential therapeutic use in the treatment of asthma.
"
3.
Hypotension (Low Blood Pressure)
03/01/1990 - "
Sch 37370 blocks hypotension in rats and a cutaneous reaction in monkeys induced by either PAF or histamine, as well as PAF-induced lethality in mice.(ABSTRACT TRUNCATED AT 250 WORDS)
"
01/01/1991 - "
Sch 37370 blocks hypotension in rats and a cutaneous reaction in monkeys induced by either PAF or histamine, as well as PAF-induced edema in the rat pleural cavity.
"
4.
Hyperventilation
01/01/1991 - "
In addition, Sch 37370 blocks bronchospasm induced by either antigen in sensitized guinea pigs or hyperventilation in nonsensitized guinea pigs.
"
5.
Eosinophilia
01/01/1991 - "
Sch 37370 also inhibits antigen-induced lung eosinophilia in sensitized guinea pigs and a reverse passive Arthus reaction in rats.
"
Related Drugs and Biologics
1.
Histamine (Histamine Dihydrochloride)
2.
Serotonin (5 Hydroxytryptamine)
3.
Therapeutic Uses
4.
Platelet Activating Factor
5.
piperidine
6.
Leukotriene C4
7.
Methacholine Chloride (Methacholine)
8.
Substance P
9.
Antigens