GR 89696 fumarate
GR 89696 fumarate结构式
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常用名 | GR 89696 fumarate | 英文名 | GR 89696 fumarate |
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| CAS号 | 126766-32-3 | 分子量 | 530.39800 | |
| 密度 | N/A | 沸点 | 559.2ºC at 760 mmHg | |
| 分子式 | C23H29Cl2N3O7 | 熔点 | N/A | |
| MSDS | 美版 | 闪点 | 292ºC |
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[11C]GR103545: novel one-pot radiosynthesis with high specific activity.
Nucl. Med. Biol. 38(2) , 215-21, (2011) GR103545 is a potent and selective kappa-opioid receptor agonist. Previous studies in non-human primates demonstrated favorable properties of [(11)C]GR103545 as a positron emission tomography tracer for in vivo imaging of cerebral kappa-opioid receptor. Nonet... |
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GR89,696: a potent kappa-opioid agonist with subtype selectivity in rhesus monkeys.
J. Pharmacol. Exp. Ther. 298(3) , 1049-59, (2001) GR89,696 is a synthetic kappa-opioid receptor agonist, recently reported to have an agonist profile consistent with selectivity at the proposed "kappa(2)" subtype. The present studies evaluated the effects of GR89,696 in vitro (i.e., in radioligand binding an... |
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[(11)C]-GR89696, a potent kappa opiate receptor radioligand; in vivo binding of the R and S enantiomers.
Nucl. Med. Biol. 29(1) , 47-53, (2002) The R and S enantiomers of [(11)C]GR89696, [(11)C]-methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)methyl]-1-piperazinecarboxylate, were synthesized from their appropriate chiral precursors and [(11)C]methyl chloroformate. The [(11)C]-labeled R enant... |
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Sensory nerve-mediated relaxation of guinea-pig isolated pulmonary artery: prejunctional modulation by alpha 2-adrenoceptor agonists but not sumatriptan.
Br. J. Pharmacol. 109(1) , 126-30, (1993) 1. Effects of the alpha 2-adrenoceptor agonists, UK14304 and clonidine, the 5-HT1 receptor agonist, sumatriptan and the kappa-opioid receptor agonist, GR103545, on sensory neurotransmission in histamine-contracted guinea-pig isolated pulmonary artery (GPPA) h... |
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Induction of bladder sphincter dyssynergia by kappa-2 opioid receptor agonists in the female rat.
J. Urol. 171(1) , 472-7, (2004) The nonselective kappa opioid receptor agonist ethylketocyclazocine suppresses external urethral sphincter (EUS) reflexes in cats. We examined the role of spinal kappa-opioid receptor subtypes in the control of EUS function in rats using selective kappa-1 (U-... |
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[11C]-methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl)-methyl]-1- piperazinecarboxylate ([11C]GR89696): synthesis and in vivo binding to kappa opiate receptors.
Nucl. Med. Biol. 26(7) , 737-41, (1999) GR89696, racemic methyl 4-[(3,4-dichlorophenyl)acetyl]-3-[(1-pyrrolidinyl) methyl]-1-piperazinecarboxylate, a kappa opioid receptor ligand, was labeled with [11C]methyl chloroformate. The radiochemical yield was 20% with an observed specific radioactivity of ... |
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Opioid regulation of spinal cord plasticity: evidence the kappa-2 opioid receptor agonist GR89696 inhibits learning within the rat spinal cord.
Neurobiol. Learn. Mem. 89(1) , 1-16, (2008) Spinal cord neurons can support a simple form of instrumental learning. In this paradigm, rats completely transected at the second thoracic vertebra learn to minimize shock exposure by maintaining a hindlimb in a flexed position. Prior exposure to uncontrolla... |
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Effects of GR-89696 and the novel peripherally selective OP2 agonists, EMD-61569 and EMD-61747, against focal cerebral ischemia in the rat.
Methods Find. Exp. Clin. Pharmacol. 21(2) , 105-13, (1999) We examined whether increases in blood-brain barrier (BBB) permeability occurring after stroke can be exploited to apply protective substances selectively to ischemic tissue. To do this, the actions of the peripherally selective OP2 agonists, EMD-61569 and EM... |
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The intrathecally administered kappa-2 opioid agonist GR89696 and interleukin-10 attenuate bone cancer-induced pain through synergistic interaction.
Anesth. Analg. 113(4) , 934-40, (2011) Although bone cancer-related pain is one of the most disruptive symptoms in patients with advanced cancer, patients are often refractory to pharmacological treatments; thus, more effective treatments for bone cancer pain are needed. We evaluated the analgesic... |
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Synthesis and stereoselective kappa-receptor binding of methylated analogues of GR-89.696.
Eur. J. Med. Chem. 36(2) , 211-4, (2001) Stereoselective synthesis of all four stereoisomers of methylated analogues 8 of the kappa-receptor agonist GR-89.696 is presented. Starting with orthogonally protected piperazine derivatives (R,R)-4 and (S,S)-4, the reaction sequence involves oxidation, redu... |