Protein Information

Name Mu opioid receptor
Synonyms MOR 1; MOR1; Mu opiate receptor; Mu opioid receptor; Mu type opioid receptor; OPRM; OPRM 1; OPRM1…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
15158798 Bedurftig S, Wunsch B: Chiral, nonracemic (piperazin-2-yl) methanol derivatives with sigma-receptor affinity. Bioorg Med Chem. 2004 Jun 15;12(12):3299-311.

In this series the p-methoxybenzyl substituted piperazine 3d reveals the highest sigma1-receptor affinity (Ki=12.4 nM) with selectivity toward sigma2-, NMDA-, kappa-opioid, and mu-opioid receptors.
81(1,1,1,1) Details
15742360 D'Antuono M, de Guzman P, Kano T, Avoli M: Ripple activity in the dentate gyrus of dishinibited hippocampus-entorhinal cortex slices. J Neurosci Res. 2005 Apr 1;80(1):92-103.

Ripples, which were also recorded in "minislices" only of the dentate gyrus, were unaffected by application of the mu-opioid receptor agonist (D-Ala2-N-Me-Phe,Gly-ol) enkephalin (10 microM; n = 6) or the N-methyl-D-aspartate (NMDA) receptor antagonist 3-(2-carboxy-piperazine-4-yl)-propyl-l-phosphonate (10 microM; n = 5).
31(0,1,1,1) 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.
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.

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-nitrogen transposition which imparts an overall lower delta and higher mu affinity to the piperidine-based ligands.
This is particularly important since analogues of 1, which show both mu- and delta-type activity, are now recognized as important for their strong analgesia and cross-canceling of many of the side effects found in agonists operating exclusively from either the delta or mu opioid receptor.
1(0,0,0,1) Details
11605661 Komoto T, Okada T, Sato S, Niino Y, Oka T, Sakamoto T: New mu-opioid receptor agonists with piperazine moiety. Chem Pharm Bull. 2001 Oct;49(10):1314-20.
162(2,2,2,2) Details