Draft:AR-M 1000390

AR-M 1000390
Clinical data
Other names	ARM-390
Identifiers
CAS Number	209808-01-5 209808-47-9 (HCl);
ChemSpider	8016974;
Chemical and physical data
Formula	C23H28N2O
Molar mass	348.490 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CCN(CC)C(=O)C1=CC=C(C=C1)C(=C2CCNCC2)C3=CC=CC=C3;

Submission declined on 18 December 2024 by SafariScribe (talk).

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Declined by SafariScribe 19 days ago. Last edited by SafariScribe 19 days ago. Reviewer: Inform author.

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AR-M 1000390 is an exceptionally selective, potent δ opioid receptor agonist with an EC50 of 7.2±0.9 nM for δ agonist potency.^[1]^[2]^[3]

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.

[pmid11052794-1] 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.

[pmid12875901-2] 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.

[pmid21147985-3] 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.

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