Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C25H29ClN2O3 |
| Molecular Weight | 440.962 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
CC1=C(C)C2=C(OC1=O)C=C(OCCCN3CCN(CC4=CC=C(Cl)C=C4)CC3)C=C2
InChI
InChIKey=USCSJAIWXWYTEH-UHFFFAOYSA-N
InChI=1S/C25H29ClN2O3/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
| 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 |
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 |
|---|---|---|
| Therapeutic options in ocular allergic disease. | 1995-08 |
|
| Effect of picumast on histamine release from rat cardiac and peritoneal mast cells. | 1991-05 |
|
| The effects of picumast on human eosinophil and neutrophil activation. | 1991-05 |
|
| Picumast and mast cell function. | 1991-05 |
|
| High performance liquid chromatographic determination of Picumast and two active metabolites in plasma using on-line sample preparation. | 1991-01 |
|
| Pharmacokinetic interactions between theophylline and other medication (Part I). | 1991-01 |
|
| Picumast dihydrochloride (Auteral), a new anti-allergic inhibitor of mediator release and action. | 1991 |
|
| Lens safety study with Picumast dihydrochloride--a double masked study using the Scheimpflug method. | 1990 |
|
| Acceptability, safety and efficacy of picumast dihydrochloride on long-term use in patients with perennial bronchial asthma. | 1989-10 |
|
| A one-year double-blind clinical study of the efficacy and tolerability of picumast dihydrochloride versus ketotifen in patients with bronchial asthma. | 1989-10 |
|
| Efficacy and tolerability of picumast dihydrochloride in comparison with placebo in asthmatic patients. | 1989-10 |
|
| Double-blind multicenter controlled clinical study comparing the efficacy of picumast dihydrochloride versus astemizole and placebo in patients with seasonal allergic rhinitis. | 1989-10 |
|
| A placebo-controlled comparison of the efficacy and tolerability of picumast dihydrochloride and terfenadine in patients with seasonal allergic rhinitis. | 1989-10 |
|
| Double-blind controlled crossover study comparing the protective effect of picumast dihydrochloride versus placebo following nasal allergen challenge. | 1989-10 |
|
| Double-blind study on the influence of picumast dihydrochloride on safety-related performance. | 1989-10 |
|
| Pharmacokinetics of picumast dihydrochloride in patients with liver cirrhosis. | 1989-10 |
|
| Study of potential kinetic interactions of picumast dihydrochloride and theophylline in vitro and after oral administration in man. | 1989-10 |
|
| Pharmacokinetics of picumast dihydrochloride and its active metabolites M1 and M2 in humans. | 1989-10 |
|
| Effect of picumast dihydrochloride on antigen-induced early and late airway responses in allergic sheep. | 1989-10 |
|
| Pharmacokinetics of picumast after administration of 14C-picumast dihydrochloride in dogs, rats, rabbits and monkeys. | 1989-10 |
Patents
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:27:36 GMT 2025
by
admin
on
Mon Mar 31 18:27:36 GMT 2025
|
| Record UNII |
125267OAUF
|
| Record Status |
Validated (UNII)
|
| Record Version |
|
-
Download
| Name | Type | Language | ||
|---|---|---|---|---|
|
Preferred Name | English | ||
|
Official Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English |
| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
|
NCI_THESAURUS |
C29712
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
m8800
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | Merck Index | ||
|
DTXSID20192693
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | |||
|
C75140
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | |||
|
SUB09821MIG
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | |||
|
100000081942
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | |||
|
5164
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | |||
|
125267OAUF
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | |||
|
CHEMBL2106970
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | |||
|
431850
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | |||
|
C013373
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY | |||
|
39577-19-0
Created by
admin on Mon Mar 31 18:27:36 GMT 2025 , Edited by admin on Mon Mar 31 18:27:36 GMT 2025
|
PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
SALT/SOLVATE -> PARENT |
| Related Record | Type | Details | ||
|---|---|---|---|---|
|
|
ACTIVE MOIETY |
