GR 89696 fumarate - CAS 126766-32-3
Category: Inhibitor
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Molecular Formula:
C19H25Cl2N3O3.C4H4O4
Molecular Weight:
530.4
COA:
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Targets:
Opioid Receptor
Description:
GR 89696 fumarate is a potent and selective κ-opioid agonist (IC50 = 0.04 nM) displaying anti-nociceptive and neuroprotective activity.
Brife Description:
κ-opioid agonist
Purity:
≥99% by HPLC
Related CAS:
126766-31-2 (free base)
Synonyms:
GR 89696 fumarate; GR 89696; GR89696; GR-89696. 4-[(3,4-Dichlorophenyl)acetyl]-3-(1-pyrrolidinylmethyl)-1-piperazinecarboxylic acid methyl ester fumarate
MSDS:
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InChIKey:
ABTNETSDXZBJTE-WLHGVMLRSA-N
InChI:
InChI=1S/C19H25Cl2N3O3.C4H4O4/c1-27-19(26)23-8-9-24(15(13-23)12-22-6-2-3-7-22)18(25)11-14-4-5-16(20)17(21)10-14;5-3(6)1-2-4(7)8/h4-5,10,15H,2-3,6-9,11-13H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
Canonical SMILES:
COC(=O)N1CCN(C(C1)CN2CCCC2)C(=O)CC3=CC(=C(C=C3)Cl)Cl.C(=CC(=O)O)C(=O)O
1.A series of novel, highly potent and selective agonists for the kappa-opioid receptor.
Hayes AG;Birch PJ;Hayward NJ;Sheehan MJ;Rogers H;Tyers MB;Judd DB;Scopes DI;Naylor A Br J Pharmacol. 1990 Dec;101(4):944-8.
1. This paper describes the opioid receptor pharmacology and in vivo activity of several novel benzene-acetamidopiperidine and benzeneacetamidopiperazine analogues. 2. These compounds all showed potent, naloxone-reversible, full agonist activity in the field-stimulated rabbit vas deferens, indicating that they are kappa-opioid agonists; but showed very little activity in the rat or hamster vas deferens, indicating good selectivity with regard to mu- and delta-opioid receptors. 3. They were all potent antinociceptive agents, the most potent compound, GR 103545, having an ED50 value in the mouse abdominal constriction test of 0.25 micrograms kg-1 s.c. The compounds also produced sedation and diuresis, but had little effect on respiration rate or gastrointestinal motility. 4. It is concluded that the seven novel compounds described are all potent and selective agonists for the kappa-opioid receptor.
2.Evaluation of the effects of specific opioid receptor agonists in a rodent model of spinal cord injury.
Aceves M;Mathai BB;Hook MA Spinal Cord. 2016 Oct;54(10):767-777. doi: 10.1038/sc.2016.28. Epub 2016 Mar 1.
OBJECTIVE: ;The current study aimed to evaluate the contribution(s) of specific opioid receptor systems to the analgesic and detrimental effects of morphine, observed after spinal cord injury in prior studies.;STUDY DESIGN: ;We used specific opioid receptor agonists to assess the effects of μ- (DAMGO), δ- (DPDPE) and κ- (GR89696) opioid receptor activation on locomotor (Basso, Beattie and Bresnahan scale, tapered beam and ladder tests) and sensory (girdle, tactile and tail-flick tests) recovery in a rodent contusion model (T12). We also tested the contribution of non-classic opioid binding using [+]- morphine.;METHODS: ;First, a dose-response curve for analgesic efficacy was generated for each opioid agonist. Baseline locomotor and sensory reactivity was assessed 24 h after injury. Subjects were then treated with an intrathecal dose of a specific agonist and re-tested after 30 min. To evaluate the effects on recovery, subjects were treated with a single dose of an agonist and both locomotor and sensory function were monitored for 21 days.;RESULTS: ;All agonists for the classic opioid receptors, but not the [+]- morphine enantiomer, produced antinociception at a concentration equivalent to a dose of morphine previously shown to produce strong analgesic effects (0.
3.Role of dorsal hippocampus κ opioid receptors in contextual aversive memory consolidation in rats.
Vanz F;Bicca MA;Linartevichi VF;Giachero M;Bertoglio LJ;Monteiro de Lima TC Neuropharmacology. 2018 Jun;135:253-267. doi: 10.1016/j.neuropharm.2018.02.029. Epub 2018 Feb 27.
The main κ opioid receptors (κORs) subtypes already described (κ;1;ORs and κ;2;ORs) are expressed in brain regions involved in aversive memory consolidation, including the dorsal hippocampus (DH). However, the role of DH κORs in consolidation of aversive memories with varied intensity and specificity is still uncertain. The present study aimed to investigate this question using pharmacological agents in rats subjected to a weak, moderate or strong contextual aversive conditioning (CAC) protocol. Antagonizing DH κORs with nor-binaltorphimine (nor-BNI), immediately after, but not 6 h later, a moderate CAC leads to intensified freezing behavior in the re-exposure to the paired context. Thus, indicating that DH κORs have an inhibitory role in the consolidation of an aversive memory. Increased DH κORs expression 1 h and 3 h after the moderate CAC was also observed. This up-regulation was absent in animals only exposed to the shock or to the context, indicating that this phenomenon requires a shock-context pairing to occur. Intra-DH nor-BNI infusion induced no changes following a weak CAC, but it was able to potentiate the expression of freezing behavior in novel and unpaired context after a strong CAC, indicating that DH κORs also modulate the consolidation of a more intense and generalized memory.
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CAS 126766-32-3 GR 89696 fumarate

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