AMG-9810 explained

AMG-9810 is a drug which acts as a potent and selective antagonist for the TRPV1 receptor.^[1] It has analgesic and antiinflammatory effects and is used in scientific research, but has not been developed for medical use. It has high antagonist potency and good bioavailability and pharmacokinetics, and so has been used to study the role of TRPV1 in areas other than pain perception, such as its roles in the brain.^{[2] [3] [4] [5] [6]}

See also

• AMG-517
• SB-705498

Notes and References

1. Doherty EM, Fotsch C, Bo Y, Chakrabarti PP, Chen N, Gavva N, Han N, Kelly MG, Kincaid J, Klionsky L, Liu Q, Ognyanov VI, Tamir R, Wang X, Zhu J, Norman MH, Treanor JJ . 6 . Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides . Journal of Medicinal Chemistry . 48 . 1 . 71–90 . January 2005 . 15634002 . 10.1021/jm049485i .
2. Okun A, DeFelice M, Eyde N, Ren J, Mercado R, King T, Porreca F . Transient inflammation-induced ongoing pain is driven by TRPV1 sensitive afferents . Molecular Pain . 7 . 1744-8069-7-4 . January 2011 . 21219650 . 10.1186/1744-8069-7-4 . 3025866 . free .
3. Shirazi M, Izadi M, Amin M, Rezvani ME, Roohbakhsh A, Shamsizadeh A . Involvement of central TRPV1 receptors in pentylenetetrazole and amygdala-induced kindling in male rats . Neurological Sciences . 35 . 8 . 1235–41 . August 2014 . 24577898 . 10.1007/s10072-014-1689-5 . 24122557 .
4. Amiresmaili S, Shamsizadeh A, Allahtavakoli M, Pourshanazari AA, Roohbakhsh A . The effect of intra-ventral hippocampus administration of TRPV1 agonist and antagonist on spatial learning and memory in male rats . Pharmacological Reports . 66 . 1 . 10–4 . February 2014 . 24905300 . 10.1016/j.pharep.2013.06.002 . 15631269 .
5. Walters ET . Neuroinflammatory contributions to pain after SCI: roles for central glial mechanisms and nociceptor-mediated host defense . Experimental Neurology . 258 . 48–61 . August 2014 . 25017887 . 10.1016/j.expneurol.2014.02.001 . 39671969 .
6. Bannazadeh M, Fatehi F, Fatemi I, Roohbakhsh A, Allahtavakoli M, Nasiri M, Azin M, Shamsizadeh A . 6 . The role of transient receptor potential vanilloid type 1 in unimodal and multimodal object recognition task in rats . Pharmacological Reports . 69 . 3 . 526–531 . May 2017 . 31994094 . 10.1016/j.pharep.2017.01.025 . 210949267 .