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Details

Stereochemistry ACHIRAL
Molecular Formula C17H13ClN2O2
Molecular Weight 312.75
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of LONAZOLAC

SMILES

OC(=O)CC1=CN(N=C1C2=CC=C(Cl)C=C2)C3=CC=CC=C3

InChI

InChIKey=XVUQHFRQHBLHQD-UHFFFAOYSA-N
InChI=1S/C17H13ClN2O2/c18-14-8-6-12(7-9-14)17-13(10-16(21)22)11-20(19-17)15-4-2-1-3-5-15/h1-9,11H,10H2,(H,21,22)

HIDE SMILES / InChI
Lonazolac is a nonsteroidal anti-inflammatory drug. The mononuclear cell response to a synovial stimulus can be abolished by very low concentrations of lonazolac. This blockade can be completely released by the addition of prostaglandin E2. Lonazolac appears therefore as an agent able in addition to modulate the immune response. The release of histamine from human basophils was significantly decreased after preincubation of the cells with lonazolac Ca. Preincubation of human polymorphonuclear leukocytes with lonazolac Ca led to an inhibition of leukotriene generation induced by either the Ca ionophore or opsonized zymosan. Lonazolac Ca affected different enzymes of the platelet activating factor metabolism. After pre- and post-treatment with lonazolac-Ca, the numbers of animals with lung metastases and the score of metastases significantly decreased. Lonazolac-Ca is indicated for the treatment of painful inflammatory rheumatic diseases of the joints and the spine. Acute irritation in osteoarthritis and spondylosis. Soft tissue rheumatism. Post-traumatic and postoperative pain and swelling states.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Irritren

Approved Use

Unknown
Palliative
Irritren

Approved Use

Indicated for the treatment of painful inflammatory rheumatic diseases of the joints and the spine. Acute irritation in osteoarthritis and spondylosis. Soft tissue rheumatism. Post-traumatic and postoperative pain and swelling states.
Palliative
Irritren

Approved Use

Indicated for the treatment of painful inflammatory rheumatic diseases of the joints and the spine. Acute irritation in osteoarthritis and spondylosis. Soft tissue rheumatism. Post-traumatic and postoperative pain and swelling states.
PubMed

PubMed

TitleDatePubMed
[Synthesis and physico-chemical properties of lonazolac-Ca, a new antiphlogistic/antirheumatic agent].
1981
[Lonazolac-Ca = Calcium [3-(p-chlorophenyl)-1-phenylpyrazole-4[ -acetate 1 Pharmacological properties of a new antiinflammatory/antirheumatic drug (author's transl)].
1981
[Lonazolac - a new non-steroidal antirheumatic agent. Report of a double-blind crossover clinical study].
1983 Jun
Blocking of mononuclear cell activation by lonazolac.
1985
A double-blind parallel group comparative study of lonazolac-calcium and diclofenac in patients with rheumatoid arthritis.
1988 Dec
Reductive effect of lonazolac on lung metastasis formation in mice.
1990
Pharmacokinetics of small unilamellar liposomes and incorporated lonazolac after i.m. administration.
1990 Jan-Mar
Effects of the nonsteroidal anti-inflammatory compounds Lonazolac Ca, indomethacin and NDGA on inflammatory mediator generation and release from various cells.
1990 Mar-Apr
The H+, K(+)-ATPase inhibitor pantoprazole (BY1023/SK&F96022) interacts less with cytochrome P450 than omeprazole and lansoprazole.
1991 Jul 5
Different drug metabolizing capacities in cultured periportal and pericentral hepatocytes.
1994 Aug 17
[Gastroduodenal tolerance and clinical effectiveness of therapy with lonazolac-calcium in rheumatic diseases].
1996
Perifusion of co-cultured hepatocytes: optimization of studies on drug metabolism and cytotoxicity in vitro.
1996 Apr
Transsynovial kinetics of lonazolac and its hydroxy metabolite in synovitis patients.
1998 Aug
Screening procedure for detection of non-steroidal anti-inflammatory drugs and their metabolites in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons by gas chromatography-mass spectrometry after extractive methylation.
2001 May-Jun
Determination of lonazolac and its hydroxy and O-sulfated metabolites by on-line sample preparation liquid chromatography with fluorescence detection.
2002 Jan 25
Patents

Sample Use Guides

300 mg taken twice daily
Route of Administration: Oral
In Vitro Use Guide
Unknown
Name Type Language
LONAZOLAC
INN   MI   WHO-DD  
INN  
Official Name English
NSC-319772
Code English
3-(P-CHLOROPHENYL)-1-PHENYLPYRAZOLE-4-ACETIC ACID
Common Name English
lonazolac [INN]
Common Name English
Lonazolac [WHO-DD]
Common Name English
LONAZOLAC CALCIUM SALT
Common Name English
LONAZOLAC [MI]
Common Name English
Classification Tree Code System Code
WHO-VATC QM01AB09
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
WHO-ATC M01AB09
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
NCI_THESAURUS C257
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
Code System Code Type Description
WIKIPEDIA
LONAZOLAC
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
PRIMARY
NSC
319772
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EPA CompTox
DTXSID4046151
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ChEMBL
CHEMBL1334692
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PUBCHEM
68706
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
PRIMARY
ECHA (EC/EINECS)
258-791-5
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PRIMARY
MESH
C017472
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
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FDA UNII
13097143QI
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CAS
53808-88-1
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PRIMARY
DRUG BANK
DB13432
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PRIMARY
CHEBI
76164
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PRIMARY
SMS_ID
100000082006
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
PRIMARY
DRUG CENTRAL
1597
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
PRIMARY
INN
3829
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CHEBI
76167
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
PRIMARY
EVMPD
SUB08570MIG
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
PRIMARY
NCI_THESAURUS
C66031
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
PRIMARY
RXCUI
28876
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
PRIMARY
RXCUI
52162
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
ALTERNATIVE
MERCK INDEX
m6893
Created by admin on Fri Dec 15 15:47:22 UTC 2023 , Edited by admin on Fri Dec 15 15:47:22 UTC 2023
PRIMARY Merck Index