Details
Stereochemistry | ACHIRAL |
Molecular Formula | C25H29ClN2O3.2ClH |
Molecular Weight | 513.884 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.Cl.CC1=C(C)C2=C(OC1=O)C=C(OCCCN3CCN(CC4=CC=C(Cl)C=C4)CC3)C=C2
InChI
InChIKey=AMHVERUFVROLJA-UHFFFAOYSA-N
InChI=1S/C25H29ClN2O3.2ClH/c1-18-19(2)25(29)31-24-16-22(8-9-23(18)24)30-15-3-10-27-11-13-28(14-12-27)17-20-4-6-21(26)7-5-20;;/h4-9,16H,3,10-15,17H2,1-2H3;2*1H
Molecular Formula | C25H29ClN2O3 |
Molecular Weight | 440.962 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Picumast is a prophylactically active anti-allergic compound which combines inhibition of mediator release and action. The activity profile of picumast differs clearly from that of known prophylactic anti-allergic drugs such as DSCG and ketotifen. Other inhibitory actions of picumast in addition to its Histamine H1 receptor -antagonism (and that of its metabolites M2 and M1) may be the cause of the suppression of immediate and late phase allergic reactions in animals as well as allergic rhinitis and bronchial responsiveness and symptom scores in asthmatic patients. In the rat, picumast inhibited carrageenin edema but was inactive against other types of inflammation. Picumast dihydrochloride cannot be considered as an anti-inflammatory drug in general, since it was inactive against adjuvant arthritis in rats and did not inhibit cotton pellet granulomas.
Originator
Approval Year
PubMed
Title | Date | PubMed |
---|---|---|
Acceptability, safety and efficacy of picumast dihydrochloride on long-term use in patients with perennial bronchial asthma. | 1989 Oct |
|
A one-year double-blind clinical study of the efficacy and tolerability of picumast dihydrochloride versus ketotifen in patients with bronchial asthma. | 1989 Oct |
|
Efficacy and tolerability of picumast dihydrochloride in comparison with placebo in asthmatic patients. | 1989 Oct |
|
A placebo-controlled comparison of the efficacy and tolerability of picumast dihydrochloride and terfenadine in patients with seasonal allergic rhinitis. | 1989 Oct |
|
Study of potential kinetic interactions of picumast dihydrochloride and theophylline in vitro and after oral administration in man. | 1989 Oct |
|
Picumast dihydrochloride (Auteral), a new anti-allergic inhibitor of mediator release and action. | 1991 |
|
High performance liquid chromatographic determination of Picumast and two active metabolites in plasma using on-line sample preparation. | 1991 Jan |
|
Effect of picumast on histamine release from rat cardiac and peritoneal mast cells. | 1991 May |
|
The effects of picumast on human eosinophil and neutrophil activation. | 1991 May |
|
Picumast and mast cell function. | 1991 May |
|
Therapeutic options in ocular allergic disease. | 1995 Aug |
Patents
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 08:03:40 GMT 2023
by
admin
on
Sat Dec 16 08:03:40 GMT 2023
|
Record UNII |
71G4MG44OQ
|
Record Status |
Validated (UNII)
|
Record Version |
|
-
Download
Name | Type | Language | ||
---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Code | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Brand Name | English | ||
|
Code | English |
Code System | Code | Type | Description | ||
---|---|---|---|---|---|
|
298894
Created by
admin on Sat Dec 16 08:03:40 GMT 2023 , Edited by admin on Sat Dec 16 08:03:40 GMT 2023
|
PRIMARY | |||
|
39577-20-3
Created by
admin on Sat Dec 16 08:03:40 GMT 2023 , Edited by admin on Sat Dec 16 08:03:40 GMT 2023
|
PRIMARY | |||
|
6917863
Created by
admin on Sat Dec 16 08:03:40 GMT 2023 , Edited by admin on Sat Dec 16 08:03:40 GMT 2023
|
PRIMARY | |||
|
71G4MG44OQ
Created by
admin on Sat Dec 16 08:03:40 GMT 2023 , Edited by admin on Sat Dec 16 08:03:40 GMT 2023
|
PRIMARY | |||
|
DTXSID60960191
Created by
admin on Sat Dec 16 08:03:40 GMT 2023 , Edited by admin on Sat Dec 16 08:03:40 GMT 2023
|
PRIMARY | |||
|
m8800
Created by
admin on Sat Dec 16 08:03:40 GMT 2023 , Edited by admin on Sat Dec 16 08:03:40 GMT 2023
|
PRIMARY | Merck Index |
Related Record | Type | Details | ||
---|---|---|---|---|
|
PARENT -> SALT/SOLVATE |
Related Record | Type | Details | ||
---|---|---|---|---|
|
ACTIVE MOIETY |