| Name | kappa opioid receptor |
|---|---|
| Synonyms | Kappa opioid receptor; KOR 1; KOR1; Kappa type opioid receptor; OPRK; OPRK 1; OPRK1; Opioid receptor kappa 1… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 18674898 | Hilfiker MA, Zhang D, Dowdell SE, Goodman KB, McAtee JJ, Dodson JW, Viet AQ, Wang GZ, Sehon CA, Behm DJ, Wu Z, Carballo LH, Douglas SA, Neeb MJ: Aminomethylpiperazines as selective urotensin antagonists. . Bioorg Med Chem Lett. 2008 Aug 15;18(16):4470-3. Epub 2008 Jul 20. Optimized substitution of the piperazine moiety has provided high affinity urotensin receptor antagonists with greater than 100-fold selectivity over the kappa-opioid receptor. |
82(1,1,1,2) | Details |
| 12393064 | Hiramatsu M, Hoshino T, Kameyama T, Nabeshima T: Involvement of kappa-opioid and sigma receptors in short-term memory in mice. Eur J Pharmacol. 2002 Oct 18;453(1):91-8. Kappa-opioid receptor agonists, trans-(+/-)-3,4-dichloro-N-methyl-N-(2-[1-pyrrolidinyl] cyclohexyl) benzeneacetamide methanesulfonate (U-50,488H) and dynorphin A-(1-13), improve impairments of learning and memory in mice and rats. sigma Receptor agonists, (+)-N-allylnormetazocine ((+)-SKF10,047) and 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl) piperazine dihydrochloride (SA4503), also reverse learning and memory impairment in various animal models. |
31(0,1,1,1) | Details |
| 19576786 | Yongye AB, Appel JR, Giulianotti MA, Dooley CT, Medina-Franco JL, Nefzi A, Houghten RA, Martinez-Mayorga K: Identification, structure-activity relationships and molecular modeling of potent triamine and piperazine opioid ligands. Bioorg Med Chem. 2009 Aug 1;17(15):5583-97. Epub 2009 Jun 21. A highly potent (14 nM) and selective (IC (50 (mu))/IC (50 (kappa))=71; IC (50 (delta))/IC (50 (kappa))=714) triamine for the kappa-opioid receptor was found. |
2(0,0,0,2) | Details |
| 11848227 | Sato S, Komoto T, Kanamaru Y, Kawamoto N, Okada T, Kaiho T, Mogi K, Morimoto S, Umehara N, Koda T, Miyashita A, Sakamoto T, Niino Y, Oka T: New mu-opioid receptor agonists with phenoxyacetic acid moiety. Chem Pharm Bull. 2002 Feb;50(2):292-7. New muq-opioid receptor (MOR) agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Among the synthesized compounds, 12-[1-[3-(N,N-dimethylcarbamoyl)-3,3-diphenylpropyl]-4-hydroxypiperidin-4- yl] phenoxy] (8: SS620) having phenoxyacetic acid and 4-hydroxypiperidine moieties showed the highest agonist potency on the MOR in an isolated guinea-pig ileum preparation, and it also had selectivity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells compared with the same types of delta- and kappa-opioid receptors (DOR and KOR). |
1(0,0,0,1) | Details |