| Name | delta opioid receptor |
|---|---|
| Synonyms | Delta type opioid receptor; Delta type opioid receptor; OPRD; OPRD 1; OPRD1; delta opioid receptor; delta1 opioid receptor; Delta type opioid receptors… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 11052794 | 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: N,N-Diethyl-4-(phenylpiperidin-4-ylidenemethyl) benzamide: a novel, exceptionally selective, potent delta opioid receptor agonist with oral bioavailability and its analogues. J Med Chem. 2000 Oct 19;43(21):3895-905. These compounds, formally derived from SNC-80 (2) by replacing the piperazine ring with a piperidine ring containing an exocyclic carbon carbon double bond, were found to bind with high affinity and exhibit excellent selectivity for the delta opioid receptor as full agonists. 6a, the simplest structure in the class, exhibited an IC (50) = 0.87 nM for the delta opioid receptors and extremely high selectivity over the mu receptors (mu/delta = 4370) and the kappa receptors (kappa/delta = 8590). |
84(1,1,1,4) | Details |
| 11052793 | Plobeck N, Delorme D, Wei ZY, Yang H, Zhou F, Schwarz P, Gawell L, Gagnon H, Pelcman B, Schmidt R, Yue SY, Walpole C, Brown W, Zhou E, Labarre M, Payza K, St-Onge S, Kamassah A, Morin PE, Projean D, Ducharme J, Roberts E: New diarylmethylpiperazines as potent and selective nonpeptidic delta opioid receptor agonists with increased In vitro metabolic stability. J Med Chem. 2000 Oct 19;43(21):3878-94. Further structural modifications on the basis of 1 confirmed the importance of the N, N-diethylbenzamide group and the piperazine lower basic for delta binding, in agreement with mutagenesis data. |
1(0,0,0,1) | Details |
| 11425550 | Nortey SO, Baxter EW, Codd EE, Zhang SP, Reitz AB: Piperazinyl benzamidines: synthesis and affinity for the delta opioid receptor. Bioorg Med Chem Lett. 2001 Jul 9;11(13):1741-3. The most active compounds had a N,N-diethylcarboxamido group and a N-benzyl piperazine. |
3(0,0,0,3) | Details |
| 19827086 | Holl R, Jung B, Schepmann D, Humpf HU, Grunert R, Bednarski PJ, Englberger W, Wunsch B: Synthesis and pharmacological evaluation of SNC80 analogues with a bridged piperazine ring. ChemMedChem. 2009 Dec;4(12):2111-22. To discover novel delta-opioid receptor ligands derived from SNC80 (1), a series of 6,8-diazabicyclo [3.2.2] nonane derivatives bearing two aromatic moieties was prepared, and the affinity toward delta, mu, and kappa receptors, as well as sigma receptors, was investigated. |
1(0,0,0,1) | Details |
| 11300879 | Thomas JB, Herault XM, Rothman RB, Atkinson RN, Burgess JP, Mascarella SW, Dersch CM, Xu H, Flippen-Anderson JL, George CF, Carroll FI: Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the 4-[(N-substituted-4-piperidinyl) arylamino]-N,N-diethylbenzamides. J Med Chem. 2001 Mar 15;44(6):972-87. It was shown that high-affinity, fully efficacious, and delta opioid receptor-selective compounds can be obtained from this transposition. Additionally, it was discovered that the somewhat lower mu/delta selectivities observed for the piperidine compounds relative to the piperazine-based ligands appear to arise as a consequence of the carbon- transposition which imparts an overall lower delta and higher mu affinity to the piperidine-based ligands. |
1(0,0,0,1) | Details |