AR-M 1000390
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| File:AR-M 1000390.svg | |
| Clinical data | |
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| Synonyms | ARM-390 |
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| ChemSpider | |
| E number | {{#property:P628}} |
| ECHA InfoCard | {{#property:P2566}} |
| Chemical and physical data | |
| Formula | C23H28N2O |
| Molar mass | 348.490 g·mol−1 |
| 3D model (JSmol) | |
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AR-M 1000390 (ARM-390) is a δ-opioid receptor agonist, known for its selectivity and potency in targeting the delta opioid receptor (DOR). It is a non-peptidic compound, derived from SNC 80, and has been studied for its potential analgesic effects without triggering acute desensitization of the receptor. AR-M 1000390 is a low-internalizing δ-opioid receptor agonist, meaning it does not induce rapid receptor desensitization. Studies suggest it may be brain-penetrant following systemic administration and has been investigated for its ability to reduce hyperalgesia in experimental models. The compound has been studied in preclinical trials for its potential in pain management and opioid receptor modulation. It has demonstrated high selectivity for the δ-opioid receptor, with an EC50 of 7.2±0.9 nM.[1][2][3]
Synthesis
Weinreb ketone synthesis Ethyl isonipecotate [1126-09-6] (1) 1-Boc-4-(methoxy-methyl-carbamoyl)piperidine [139290-70-3] (2) N,N-diethyl-4-iodobenzamide [77350-52-8] (3) Tert-butyl 4-[4-(diethylcarbamoyl)benzoyl]piperidine-1-carboxylate, PC1057236 (4) Tert-butyl 4-[[4-(diethylcarbamoyl)phenyl]-hydroxy-phenylmethyl]piperidine-1-carboxylate, PC10814060 (5)
Dor Agonists
There are many DOR agonists that have been developed. For example, compare for: ADL5747, BW 373U86, JNJ-20788560, PN6047, SB 205607, SB-205588, SNC 121 & UFP-512.
References
- ↑ Wei ZY, Brown W, Takasaki B, Plobeck N, Delorme D, Zhou F, Yang H, Jones P, Gawell L, Gagnon H, Schmidt R, Yue SY, Walpole C, Payza K, St-Onge S, Labarre M, Godbout C, Jakob A, Butterworth J, Kamassah A, Morin PE, Projean D, Ducharme J, Roberts E (October 2000). "N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl)benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues". Journal of Medicinal Chemistry. 43 (21): 3895–905. doi:10.1021/jm000229p. PMID 11052794.
- ↑ Marie N, Landemore G, Debout C, Jauzac P, Allouche S (August 2003). "Pharmacological characterization of AR-M1000390 at human delta opioid receptors". Life Sciences. 73 (13): 1691–704. doi:10.1016/s0024-3205(03)00489-2. PMID 12875901.
- ↑ Pradhan AA, Walwyn W, Nozaki C, Filliol D, Erbs E, Matifas A, Evans C, Kieffer BL (December 2010). "Ligand-directed trafficking of the δ-opioid receptor in vivo: two paths toward analgesic tolerance". The Journal of Neuroscience : The Official Journal of the Society for Neuroscience. 30 (49): 16459–68. doi:10.1523/JNEUROSCI.3748-10.2010. PMC 3086517. PMID 21147985.
- ↑ Daniel Delorme, Edward Roberts, & Zhongyong Wei, WO1998028275 (AstraZeneca Canada Inc).
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