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CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider |
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UNII | |
ChEBI | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.162.062 |
Chemical and physical data | |
Formula | C22H21Cl2IN4O |
Molar mass | 555.24 g·mol−1 |
3D model ( JSmol) | |
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(verify) |
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. [1] Like rimonabant, it is additionally a μ-opioid receptor antagonist [2] that attenuates analgesic effects. [3]
AM251 has shown an in vitro antimelanoma activity against pancreatic and colon cancer cells. [4]
Receptor ( ligands) |
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μ-opioid (MOR) |
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δ-opioid (DOR) |
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κ-opioid (KOR) |
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Nociceptin (NOP) |
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Others |
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This cannabinoid related article is a stub. You can help Wikipedia by expanding it. |
Identifiers | |
---|---|
| |
CAS Number | |
PubChem CID | |
IUPHAR/BPS | |
ChemSpider |
|
UNII | |
ChEBI | |
ChEMBL | |
CompTox Dashboard ( EPA) | |
ECHA InfoCard | 100.162.062 |
Chemical and physical data | |
Formula | C22H21Cl2IN4O |
Molar mass | 555.24 g·mol−1 |
3D model ( JSmol) | |
| |
| |
(verify) |
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. [1] Like rimonabant, it is additionally a μ-opioid receptor antagonist [2] that attenuates analgesic effects. [3]
AM251 has shown an in vitro antimelanoma activity against pancreatic and colon cancer cells. [4]
Phytocannabinoids ( comparison) |
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Endocannabinoids |
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Synthetic cannabinoid receptor agonists / neocannabinoids |
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Endocannabinoid enhancers (inactivation inhibitors) |
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Anticannabinoids (antagonists/inverse agonists/antibodies) |
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Receptor ( ligands) |
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Transporter ( modulators) |
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Enzyme ( modulators) |
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Others |
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μ-opioid (MOR) |
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δ-opioid (DOR) |
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κ-opioid (KOR) |
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Nociceptin (NOP) |
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Others |
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This cannabinoid related article is a stub. You can help Wikipedia by expanding it. |