Org 27569 (CAS 868273-06-7)
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Org 27569 is an allosteric modulator of the cannabinoid receptor type 1 (CB1). It binds to a distinct site on the receptor, which is different from the orthosteric binding site where endogenous ligands like anandamide or synthetic cannabinoids bind. By interacting with this allosteric site, Org 27569 enhances the affinity of agonists for the CB1 receptor without directly activating the receptor itself. This modulation can amplify the receptor′s response to endogenous cannabinoids, providing a unique tool to study CB1 receptor functions and signaling pathways. It is particularly useful for investigating the receptor′s role in various physiological and pathological processes, including pain, appetite regulation, and neuroprotection, by providing insights into how allosteric modulation can influence receptor activity and downstream effects. Org 27569 can also help in better understanding the mechanisms of allosteric modulation and its potential therapeutic applications by offering a means to fine-tune receptor activity without the typical effects of direct agonism or antagonism.
Org 27569 (CAS 868273-06-7) References
- Allosteric modulation of the cannabinoid CB1 receptor. | Price, MR., et al. 2005. Mol Pharmacol. 68: 1484-95. PMID: 16113085
- Parameterization of Org27569: an allosteric modulator of the cannabinoid CB1 G protein-coupled receptor. | Iliff, HA., et al. 2011. J Comput Chem. 32: 2119-26. PMID: 21523790
- The inverse agonist effect of rimonabant on G protein activation is not mediated by the cannabinoid CB1 receptor: evidence from postmortem human brain. | Erdozain, AM., et al. 2012. Biochem Pharmacol. 83: 260-8. PMID: 22093909
- Allosteric modulator ORG27569 induces CB1 cannabinoid receptor high affinity agonist binding state, receptor internalization, and Gi protein-independent ERK1/2 kinase activation. | Ahn, KH., et al. 2012. J Biol Chem. 287: 12070-82. PMID: 22343625
- A key agonist-induced conformational change in the cannabinoid receptor CB1 is blocked by the allosteric ligand Org 27569. | Fay, JF. and Farrens, DL. 2012. J Biol Chem. 287: 33873-82. PMID: 22846992
- CB(1) receptor allosteric modulators display both agonist and signaling pathway specificity. | Baillie, GL., et al. 2013. Mol Pharmacol. 83: 322-38. PMID: 23160940
- Distinct roles of β-arrestin 1 and β-arrestin 2 in ORG27569-induced biased signaling and internalization of the cannabinoid receptor 1 (CB1). | Ahn, KH., et al. 2013. J Biol Chem. 288: 9790-9800. PMID: 23449980
- The membrane proximal region of the cannabinoid receptor CB1 N-terminus can allosterically modulate ligand affinity. | Fay, JF. and Farrens, DL. 2013. Biochemistry. 52: 8286-94. PMID: 24206272
- In-vivo pharmacological evaluation of the CB1-receptor allosteric modulator Org-27569. | Gamage, TF., et al. 2014. Behav Pharmacol. 25: 182-5. PMID: 24603340
- Effects of the cannabinoid CB₁ receptor allosteric modulator ORG 27569 on reinstatement of cocaine- and methamphetamine-seeking behavior in rats. | Jing, L., et al. 2014. Drug Alcohol Depend. 143: 251-6. PMID: 25169627
- Behavioral effects of the cannabinoid CB1 receptor allosteric modulator ORG27569 in rats. | Ding, Y., et al. 2014. Pharmacol Res Perspect. 2: e00069. PMID: 25431655
- Structural dynamics and energetics underlying allosteric inactivation of the cannabinoid receptor CB1. | Fay, JF. and Farrens, DL. 2015. Proc Natl Acad Sci U S A. 112: 8469-74. PMID: 26100912
- CB1 allosteric modulator Org27569 is an antagonist/inverse agonist of ERK1/2 signaling. | Gamage, TF., et al. 2016. Cannabis Cannabinoid Res. 1: 272-280. PMID: 28660254
- Rational design of cannabinoid type-1 receptor allosteric modulators: Org27569 and PSNCBAM-1 hybrids. | Nguyen, T., et al. 2021. Bioorg Med Chem. 41: 116215. PMID: 34015703
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Org 27569, 10 mg | sc-204151 | 10 mg | $164.00 | |||
Org 27569, 50 mg | sc-204151A | 50 mg | $689.00 |