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
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)
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
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL3335 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1650212 |
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Target ID: CHEMBL3509602 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1650212 |
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Target ID: CHEMBL5978 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1650212 |
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Target ID: GO:0002391 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1693604 |
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Target ID: GO:0035490 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1693604 |
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Target ID: GO:0002349 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1693604 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Palliative | Irritren Approved UseUnknown |
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Palliative | Irritren Approved UseIndicated 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. |
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Palliative | Irritren Approved UseIndicated 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
Title | Date | PubMed |
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[Synthesis and physico-chemical properties of lonazolac-Ca, a new antiphlogistic/antirheumatic agent]. | 1981 |
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[Lonazolac-Ca = Calcium [3-(p-chlorophenyl)-1-phenylpyrazole-4[ -acetate 1 Pharmacological properties of a new antiinflammatory/antirheumatic drug (author's transl)]. | 1981 |
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[Lonazolac - a new non-steroidal antirheumatic agent. Report of a double-blind crossover clinical study]. | 1983 Jun |
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Blocking of mononuclear cell activation by lonazolac. | 1985 |
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A double-blind parallel group comparative study of lonazolac-calcium and diclofenac in patients with rheumatoid arthritis. | 1988 Dec |
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Reductive effect of lonazolac on lung metastasis formation in mice. | 1990 |
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Pharmacokinetics of small unilamellar liposomes and incorporated lonazolac after i.m. administration. | 1990 Jan-Mar |
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Effects of the nonsteroidal anti-inflammatory compounds Lonazolac Ca, indomethacin and NDGA on inflammatory mediator generation and release from various cells. | 1990 Mar-Apr |
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The H+, K(+)-ATPase inhibitor pantoprazole (BY1023/SK&F96022) interacts less with cytochrome P450 than omeprazole and lansoprazole. | 1991 Jul 5 |
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Different drug metabolizing capacities in cultured periportal and pericentral hepatocytes. | 1994 Aug 17 |
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[Gastroduodenal tolerance and clinical effectiveness of therapy with lonazolac-calcium in rheumatic diseases]. | 1996 |
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Perifusion of co-cultured hepatocytes: optimization of studies on drug metabolism and cytotoxicity in vitro. | 1996 Apr |
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Transsynovial kinetics of lonazolac and its hydroxy metabolite in synovitis patients. | 1998 Aug |
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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 |
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Determination of lonazolac and its hydroxy and O-sulfated metabolites by on-line sample preparation liquid chromatography with fluorescence detection. | 2002 Jan 25 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/9726694
300 mg taken twice daily
Route of Administration:
Oral
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WHO-VATC |
QM01AB09
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WHO-ATC |
M01AB09
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NCI_THESAURUS |
C257
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LONAZOLAC
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319772
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CHEMBL1334692
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68706
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258-791-5
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C017472
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C66031
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m6893
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PRIMARY | Merck Index |
ACTIVE MOIETY
SALT/SOLVATE (PARENT)