BIOMAT Database Logo BIOMAT Database Logo

Pharmacological profiles of 2-carboxyphenyl-1-(4-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetate and 2-[(2-carboxyphenoxy)-carbonyl]phenyl-1-(4-chlorobenzoyl)-5-meth oxy-2- methylindole-3-acetate, new antiinflammatory agents. 1986

I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka

When the effects of new antiinflammatory drugs, 2-carboxyphenyl-1-(4-chlorobenzoyl)-5-methoxy-2-methyl-indole-3-acetate (TB 219) and 2-[(2-carboxyphenoxy)carbonyl]phenyl-1-(4-chlorobenzoyl)-5- methoxy-2-methylindole-3-acetate (TB 220), were investigated in various experiments, the following results were obtained: 1. TB 219 and TB 220 showed remarkable inhibitory effects on carrageenin edema, ultraviolet erythema and adjuvant arthritis. Although TB 219 displayed almost equipotent or slightly more potent effect than those of indometacin and acemetacin, TB 220 was slightly less effective than these two reference drugs except for the therapeutic effect on adjuvant arthritis. 2. TB 219 and TB 220 inhibited the writhing syndrome induced by acetic acid and inflammatory hyperesthesia, and they provided a significant antipyretic activity. 3. Both drugs elicited almost negligible side effects in the gastrointestinal tract even after the repeated administrations. Especially, ulcerogenic activity of TB 220 was extremely weak. LD50's of both drugs are higher than that of indometacin in rats. 4. Both drugs elicited no appreciable changes in general behavior in mice and rats after oral administration. After intraperitoneal or intravenous injection of these two drugs, no marked changes in spontaneous EEG pattern and the spinal reflex were observed.

UI MeSH Term Description Entries
D007213 Indomethacin A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES. Amuno,Indocid,Indocin,Indomet 140,Indometacin,Indomethacin Hydrochloride,Metindol,Osmosin
D008297 Male Males
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D002199 Capillary Permeability The property of blood capillary ENDOTHELIUM that allows for the selective exchange of substances between the blood and surrounding tissues and through membranous barriers such as the BLOOD-AIR BARRIER; BLOOD-AQUEOUS BARRIER; BLOOD-BRAIN BARRIER; BLOOD-NERVE BARRIER; BLOOD-RETINAL BARRIER; and BLOOD-TESTIS BARRIER. Small lipid-soluble molecules such as carbon dioxide and oxygen move freely by diffusion. Water and water-soluble molecules cannot pass through the endothelial walls and are dependent on microscopic pores. These pores show narrow areas (TIGHT JUNCTIONS) which may limit large molecule movement. Microvascular Permeability,Permeability, Capillary,Permeability, Microvascular,Vascular Permeability,Capillary Permeabilities,Microvascular Permeabilities,Permeabilities, Capillary,Permeabilities, Microvascular,Permeabilities, Vascular,Permeability, Vascular,Vascular Permeabilities
D004064 Digestive System A group of organs stretching from the MOUTH to the ANUS, serving to breakdown foods, assimilate nutrients, and eliminate waste. In humans, the digestive system includes the GASTROINTESTINAL TRACT and the accessory glands (LIVER; BILIARY TRACT; PANCREAS). Ailmentary System,Alimentary System
D004487 Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE. Dropsy,Hydrops,Anasarca
D004644 Emotions Those affective states which can be experienced and have arousing and motivational properties. Feelings,Regret,Emotion,Feeling,Regrets
D004890 Erythema Redness of the skin produced by congestion of the capillaries. This condition may result from a variety of disease processes. Erythemas
D004910 Erythrocyte Membrane The semi-permeable outer structure of a red blood cell. It is known as a red cell 'ghost' after HEMOLYSIS. Erythrocyte Ghost,Red Cell Cytoskeleton,Red Cell Ghost,Erythrocyte Cytoskeleton,Cytoskeleton, Erythrocyte,Cytoskeleton, Red Cell,Erythrocyte Cytoskeletons,Erythrocyte Ghosts,Erythrocyte Membranes,Ghost, Erythrocyte,Ghost, Red Cell,Membrane, Erythrocyte,Red Cell Cytoskeletons,Red Cell Ghosts
D005106 Exploratory Behavior The tendency to explore or investigate a novel environment. It is considered a motivation not clearly distinguishable from curiosity. Curiosity,Novelty-Seeking Behavior,Behavior, Exploratory,Behavior, Novelty-Seeking,Behaviors, Exploratory,Behaviors, Novelty-Seeking,Curiosities,Exploratory Behaviors,Novelty Seeking Behavior,Novelty-Seeking Behaviors

Related Publications

I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
2-Isopropyl-4-meth-oxy-5-methyl-phenyl acetate.
October 2013, Acta crystallographica. Section E, Structure reports online,
I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
(E)-2-Meth-oxy-4-(3-oxobut-1-en-yl)phenyl acetate.
July 2008, Acta crystallographica. Section E, Structure reports online,
I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
Crystal and molecular structure of an antiinflammatory agent, indomethacin, 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid.
February 1972, Journal of the American Chemical Society,
I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
Glycerides as prodrugs. 3. Synthesis and antiinflammatory activity of [1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetyl]glycerides (indomethacin glycerides).
January 1980, Journal of medicinal chemistry,
I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
2-Meth-oxy-4-(prop-2-en-1-yl)phenyl 4-meth-oxy-benzoate.
June 2013, Acta crystallographica. Section E, Structure reports online,
I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
ANTI-INFLAMMATORY AND ANTIPYRETIC ACTIVITIES OF INDOMETHACIN, 1-(P-CHLOROBENZOYL)-5-METHOXY-2-METHYLINDOLE-3-ACETIC ACID.
September 1963, The Journal of pharmacology and experimental therapeutics,
I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
4-(7-Acet-oxy-6-meth-oxy-4-methyl-2-oxo-2H-chromen-3-yl)phenyl acetate.
June 2008, Acta crystallographica. Section E, Structure reports online,
I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
2-Isopropyl-4-meth-oxy-5-methyl-phenyl benzoate.
March 2010, Acta crystallographica. Section E, Structure reports online,
I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
Ethyl (Z)-2-chloro-2-[2-(4-meth-oxy-phenyl)hydrazin-1-yl-idene]acetate.
December 2012, Acta crystallographica. Section E, Structure reports online,
I Tanaka, and H Yoshizumi, and Y Tanaka, and S Takeda, and C Kamei, and N Nakaya, and K Kitazumi, and H Tagami, and K Tasaka
Phenyl 3-meth-oxy-4-phen-oxy-benzoate.
September 2011, Acta crystallographica. Section E, Structure reports online,
Copied contents to your clipboard!