Lornoxicam 是一种新型非甾体抗炎药,是高活性 COX-1 和 COX-2 抑制剂,IC50 分别为 5 和 8 nM。
产品描述
Lornoxicam (chlortenoxicam) is a new nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class with analgesic, anti-inflammatory, and antipyretic properties. Lornoxicam differs from other oxicam compounds in its potent inhibition of prostaglandin biosynthesis, a property that explains the particularly pronounced efficacy of the drug. Lornoxicam is approved for use in Japan.
体外活性
Lornoxicam is as effective as the opioid analgesics morphine, pethidine (meperidine) and tramadol in relieving postoperative pain following gynaecological or orthopaedic surgery, and as effective as other NSAIDs after oral surgery. Lornoxicam is also as effective as other NSAIDs in relieving symptoms of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, acute sciatica and low back pain. [1]
体内活性
Lornoxicam dose relatedly reduces the total number of c-Fos-LI neurons with the strongest effect corresponding to the 75% reduction for the highest dose of 9 mg/kg, and the 45% reduction for the low dose of 0.3 mg/kg. Lornoxicam (0.1, 0.3 mg/kg, 1 mg/kg, 3 mg/kg and 9 mg/kg, i.v.) significantly reduces the number of c-Fos-LI neurons in both superficial (24%, 33%, 53%, 54%, and 63% reduction, respectively) and deep (28%, 48%, 62%, 69% and 79% reduction, respectively) laminae of the dorsal horn of the spinal cord. [2] Lornoxicam reduces hyperalgesia with an effective dose that provides 50% inhibition (ED50) of 0.083 mg/kg, 3.9 mg/kg and 4.3 mg/kg respectively in a chronic rat model of arthritis. Lornoxicam significantly reduces the PGE2 level in paw exudate and the cerebrospinal fluid in rats. Lornoxicam 0.16 mg/kg, celecoxib 4 mg/kg and loxoprofen 2.4 mg/kg significantly reduces hyperalgesia to a similar extent in acute oedematous rats. [3]
Cas No.
70374-39-9
分子式
C13H10ClN3O4S2
分子量
371.81
别名
Chlortenoxicam;氯诺昔康;Ro 13-9297;TS110;Lornoxicam
储存和溶解度
DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years