- Source: AM-251 (drug)
AM-251 is an inverse agonist at the CB1 cannabinoid receptor. AM-251 is structurally very close to rimonabant; both are biarylpyrazole cannabinoid receptor antagonists. In AM-251, the p-chloro group attached to the phenyl substituent at C-5 of the pyrazole ring is replaced with a p-iodo group. The resulting compound exhibits slightly better binding affinity for the CB1 receptor (with a Ki value of 7.5 nM) than rimonabant, which has a Ki value of 11.5 nM, AM-251 is, however, about two-fold more selective for the CB1 receptor when compared to rimonabant. Like rimonabant, it is additionally a μ-opioid receptor antagonist that attenuates analgesic effects.
AM251 has shown an in vitro antimelanoma activity against pancreatic and colon cancer cells.
See also
Discovery and development of Cannabinoid Receptor 1 Antagonists
References
Kata Kunci Pencarian:
- Raksa
- Bakteri
- Mitomisin
- Ras manusia
- Meningitis
- Skizofrenia
- Asam hipoklorit
- Nikotinamida adenina dinukleotida
- AIDS
- Virus dalam sejarah manusia
- AM-251 (drug)
- Cannabis (drug)
- Psychoactive drug
- Recreational drug use
- Lean (drug)
- MDMA
- Psychedelic drug
- Nonsteroidal anti-inflammatory drug
- Orlistat
- Addiction
