Tamibarotene
Tamibarotene is an agonist at retinoic acid receptors (RARs) and is selective primarily for RARα/β. Tamibarotene exhibits neuroprotective, cognition enhancing, immunomodulatory, and anticancer chemotherapeutic benefits. Tamibarotene upregulates tropomysin-related kinase B and growth-associated protein 43, inducing neuronal differentiation. In vivo, tamibarotene activates the ADAM10-Notch-Hes5 signaling pathway, inhibiting deterioration of working memory and improving cognitive deficits in dementia and Alzheimer’s disease. Tamibarotene also prevents decreases in acetylcholine and decreases secretion of inflammatory cytokines and anxiety in models of Alzheimer’s disease. Tamibarotene decreases iron-induced oxidative stress in vivo, decreasing blood glucose levels and hepatic iron content. In animal models of vasculitis, this compound inhibits neutrophil migration, ROS production, and phosphorylation of ERK 1/2 and p38. Tamibarotene also exhibits immunomodulatory effects in animal models of graft-versus-host disease (GVHD) and experimental autoimmune encephalitis (EAE), altering Th1 and Th17 responses. Additionally, tamibarotene may inhibit cell growth in leukemia cells and induce partial regression of tumors in animal models of cancer.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18974576
| Cas No. |
94497-51-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C22H25NO3 |
| Formula Wt. |
351.44 |
| IUPAC Name |
4-[(5,5,8,8-tetramethyl-6,7-dihydronaphthalen-2-yl)carbamoyl]benzoicacid |
| Synonym |
Am80 |
| Melting Point |
230-232°C |
| Appearance |
White to off white crystalline powder |
Kitaoka K, Shimizu N, Ono K, et al. The retinoic acid receptor agonist Am80 increases hippocampal ADAM10 in aged SAMP8 mice. Neuropharmacology. 2013 Sep;72:58-65. PMID: 23624141
Yoshikawa O, Ebata Y, Tsuchiya H, et al. A retinoic acid receptor agonist tamibarotene suppresses iron accumulation in the liver. Obesity (Silver Spring). 2013 Jan;21(1):E22-5. PMID: 23404745.
Miyabe C, Miyabe Y, Miura NN, et al. Am80, a retinoic acid receptor agonist, ameliorates murine vasculitis through the suppression of neutrophil migration and activation. Arthritis Rheum. 2013 Feb;65(2):503-12. PMID: 23203767.
Fukasawa H, Nakagomi M, Yamagata N, et al. Tamibarotene: a candidate retinoid drug for Alzheimers disease. Biol Pharm Bull. 2012;35(8):1206-12. PMID: 22863914.
Nishimori H, Maeda Y, Teshima T, et al. Synthetic retinoid Am80 ameliorates chronic graft-versus-host disease by down-regulating Th1 and Th17. Blood. 2012 Jan 5;119(1):285-95. PMID: 22077062.
Shiohira H, Kitaoka A, Shirasawa H, et al. Am80 induces neuronal differentiation in a human neuroblastoma NH-12 cell line. Int J Mol Med. 2010 Sep;26(3):393-9. PMID: 20664956.
Klemann C, Raveney BJ, Klemann AK, et al. Synthetic retinoid AM80 inhibits Th17 cells and ameliorates experimental autoimmune encephalomyelitis. Am J Pathol. 2009 Jun;174(6):2234-45. PMID: 19389933.
