U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C6H8N6
Molecular Weight 164.1679
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of DAMETRALAST

SMILES

CC1=NN2C(=C1)N=C(N)N=C2N

InChI

InChIKey=CDMRMPWJHYFXJJ-UHFFFAOYSA-N
InChI=1S/C6H8N6/c1-3-2-4-9-5(7)10-6(8)12(4)11-3/h2H,1H3,(H4,7,8,9,10)

HIDE SMILES / InChI

Molecular Formula C6H8N6
Molecular Weight 164.1679
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Dametralast is disclosed in patent application US4183930A as example 2

Dametralast is an antihistamine agent. Bronchodilator action of dametralast was demonstrated on the isolated trachea of guinea pigs. Dametralast prevents bronchospasm in anesthetized guinea-pigs, protects mice from anaphylactic shock induced by injection of bovine albumin, and has a protective effect in passive cutaneous anaphylaxis test in rats. Investigations into the mechanism of action have shown that the drug was ineffective on the synthesis of cyclooxygenase products from arachidonic acid. Dametralast inhibited cAMP phosphodiesterase (PDE) but this inhibition does not seem to be involved in their anti-inflammatory activity. In clinical tests dametralast was well tolerated; functional respiratory exploration determinations provided the same bronchodilator effect found in animals. A favorable effect was noted in asthmatic subjects and in subjects suffering from respiratory insufficiency.

Approval Year

PubMed

PubMed

TitleDatePubMed
Bronchodilator and antiallergic properties of LA 2851 (2-4-diamino-7-methyl-pyrazolo (1,5-a) 1,3,5-triazine).
1981 Aug
Anti-inflammatory effect of LA 2851 and reference drugs on some models of inflammation. Investigation of the mechanism of action.
1982 Oct
Patents
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:35:53 GMT 2023
Edited
by admin
on Fri Dec 15 16:35:53 GMT 2023
Record UNII
16992A3UUS
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DAMETRALAST
INN  
INN  
Official Name English
dametralast [INN]
Common Name English
2,4-DIAMINO-7-METHYLPYRAZOLO(1,5-A)-S-TRIAZINE
Systematic Name English
Classification Tree Code System Code
NCI_THESAURUS C29712
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
Code System Code Type Description
INN
5816
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
PRIMARY
EVMPD
SUB06895MIG
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
PRIMARY
NCI_THESAURUS
C74271
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
PRIMARY
SMS_ID
100000083435
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
PRIMARY
PUBCHEM
68910
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
PRIMARY
EPA CompTox
DTXSID00868026
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
PRIMARY
FDA UNII
16992A3UUS
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
PRIMARY
CAS
71680-63-2
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
PRIMARY
ChEMBL
CHEMBL2104205
Created by admin on Fri Dec 15 16:35:54 GMT 2023 , Edited by admin on Fri Dec 15 16:35:54 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY