GR 89696

a potent & selective kappa opioid receptor agonist; RN given refers to (E)-2-butenedioate(1:1); RN for parent cpd not available 11/92; GR 103545 is the (R)-isomer

Also Known As:

1-((3,4-dichlorophenyl)acetyl)-4-acetyl-2-(1-pyrrolidinylmethyl)piperazine; GR 103545; GR 85571; GR 89696, (R)-isomer, (E)-2-butenedioate (1:1); GR-103545; GR-85571; GR-89696; GR103545; GR85571; methyl 4-((3,4-dichlorophenyl)acetyl)-3-(1-pyrrolidinylmethyl)-1-piperazinecarboxylate fumarate; 1-Piperazinecarboxylic acid, 4-((3,4-dichlorophenyl)acetyl)-3-(1-pyrrolidinylmethyl)-, methyl ester, (E)-2-butenedioate (1:1)

Networked: 5 relevant articles (0 outcomes, 0 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Pyrrolidines: 115
    - GR 89696: 5
  - Piperazines: 26
    - GR 89696: 5

Experts

1.	Carson, Richard E: 1 article (11/2021)
2.	Hillmer, Ansel T: 1 article (11/2021)
3.	Mann, J John: 1 article (11/2021)
4.	Miller, Jeffrey M: 1 article (11/2021)
5.	Oquendo, Maria A: 1 article (11/2021)
6.	Smart, Kelly: 1 article (11/2021)
7.	Yttredahl, Ashley: 1 article (11/2021)
8.	Husbands, Stephen M: 1 article (01/2009)
9.	Ko, Mei-Chuan: 1 article (01/2009)
10.	Kolar, F: 1 article (06/2008)

Related Diseases

1.	Coronary Occlusion 06/01/2008 - "Chronic treatment with opioid receptor ligands: nonselective peptide opioid receptor agonist dalargin (intraperitoneally in a dose of 1 mg/kg), selective nonpeptide kappa-receptor agonist GR 89696 (subcutaneously in a dose of 0.03 mg/kg), nonselectrive nonpeptide antagonist quadazocine (subcutaneously in a dose of 3 mg/kg) or naltrexone (subcutaneously in a dose of 10 mg/kg) for 20 day had no effect of the incidence of ischemic ventricular arrhythmias and the size of necrotic zone after coronary occlusion and reperfusion in rats in vivo."
2.	Respiratory Insufficiency (Respiratory Failure) 01/01/2009 - "In addition, pretreatment with effective antiscratching doses of nalfurafine, bremazocine, or GR 89696 did not antagonize systemic morphine-induced antinociception and respiratory depression. " 01/01/2009 - "In particular, previously proposed non-KOR-1 agonists, including nalfurafine [TRK-820, 17-cyclopropylmethyl-3,14 beta-dihydroxy-4,5 alpha-epoxy-6 beta-[N-methyl-trans-3-(3-furyl)acrylamido]morphinan], bremazocine [(+/-)-6-ethyl-1,2,3,4,5,6-hexahydro-3-[(1-hydroxycyclopropy)-methyl]-11,11-dimethyl-2,6-methano-3-benzazocin-8-ol], and GR 89696 [4-[(3,4-dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)-1-piperazinecarboxylic acid methyl ester] were studied in various behavioral assays for measuring itch/scratching, analgesia, and respiratory depression. "
3.	Ischemia 03/01/1999 - "To do this, the actions of the peripherally selective OP2 agonists, EMD-61569 and EMD-61747, have been compared with those of the centrally acting OP2 agonist, GR-89696, in the rat permanent focal ischemia model. "
4.	Hyperalgesia 08/01/1992 - "GR103545 raised the noxious presure threshold in the inflamed and non-inflamed paws at the same doses.8. GR94839 was sedative in the rat rotarod test (ED50: 35 (12-245) mg kg-', s.c.) at doses higher than those required to inhibit the 2nd phase of the formalin response or reverse hyperalgesia in the zymosan-inflamed rat paw. "
5.	Major Depressive Disorder (Major Depressive Disorders) 11/27/2021 - "Here we present results of a secondary analysis of data acquired using positron emission tomography (PET) with the KOR radiotracer [11C]GR103545 in 10 unmedicated, currently depressed individuals with major depressive disorder (MDD; 32.6 ± 6.5 years, 5 women) and 13 healthy volunteers (34.8 ± 10 years, 6 women). "

Related Drugs and Biologics

1.	Opioid Peptides (Opioid Peptide)
2.	kappa Opioid Receptors (kappa Opioid Receptor)
3.	Zymosan
4.	Opioid Receptors (Opioid Receptor)
5.	Naltrexone (ReVia)
6.	Morphine (MS Contin)
7.	Morphinans
8.	Ligands
9.	Hypnotics and Sedatives (Sedatives)
10.	Formaldehyde (Formol)

Related Therapies and Procedures

1.	Analgesia