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Benzeneacetamides (1):
Recent article
Benzeneacetamides
Abstract
Photoprotein obelin, the enzyme-substrate complex of polypeptide with 2-hydroperoxycoelenterazine, is responsible for bioluminescence of marine hydroid Obelia longissima. Addition of Ca(2+) to the photoprotein triggers the bioluminescent reaction with light emission. The product of the bioluminescen...
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PMID: 20678944
PDF is available here.
PDF is available here.
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Abstract
At Weeks 12 and 16, both the nepafenac and bromfenac groups showed a significant reduction in retinal thickness compared with that in placebo (nepafenac, P = 0.0048, bromfenac, P = 0.0113). A difference, however, between these 2 NSAID groups was observed in that only the nepafenac group was able to...
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PMID: 20175270
PDF is available here.
PDF is available here.
Abstract
These results indicate that ATM is the predominant protein which is active in the phosphorylation of histone H2AX after heating....
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PMID: 20448412
PDF is available here.
PDF is available here.
Abstract
Treatment with an MOR agonist ([D-Ala(2), N-Me-Phe(4), Gly(5)-ol]-enkephalin acetate salt [DAMGO; 1.3 or 6.6 mg/kg]) increased HLWLs (from baseline) at 2 to 8 hours after injection; at the higher dose, the maximum mean increase was 5.6 seconds at 4 hours. Treatment with a DOR agonist ([D-Ala(2), D-L...
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PMID: 19719421
PDF is available here.
PDF is available here.
Abstract
We report a case of sterile ulceration after photorefractive keratectomy surgery, which we believe was caused by frequent postoperative dosing of nepafenac....
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PMID: 19654513
PDF is available here.
PDF is available here.
Prescrire international (18)102 2009
Abstract
Abstract
Incubation of mitochondria with aged Abeta(25-35) inhibited the activities of alpha-ketoglutarate dehydrogenase (alpha-KGDH), pyruvate dehydrogenase (PDH) and respiratory chain complex IV. It also resulted in increased H(2)O(2) and (O2*-) production, and decreased the GSH level in mitochondria. Furt...
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PMID: 19417731
PDF is available here.
PDF is available here.
Psychopharmacology (203)2 2009
Abstract
Salvinorin A and both synthetic derivatives of salvinorin B substituted completely for U69,593. Additionally, cross-generalization was observed between salvinorin A and both KOP agonists. CONCLUSION: These findings support previous reports indicating that the discriminative stimulus effects of salvi...
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PMID: 19153716
PDF is available here.
PDF is available here.
Journal of Neuroscience (29)4 2009
Abstract
We report that morphine increased microglial migration via a novel interaction between mu-opioid and P2X(4) receptors, which is dependent upon PI3K/Akt pathway activation. Morphine at 100 nm enhanced migration of primary microglial cells toward adenosine diphosphate by 257, 247, 301, 394, and 345% f...
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PMID: 19176808
PDF is available here.
PDF is available here.
Abstract
Our article reviews allergist's opinions on a protocol to test for PCN allergy in patients without a history of a life-threatening reaction. This study was performed to determine whether fellows of the American Academy of Allergy, Asthma, and Immunology (AAAAI) would use a two-challenge PCN allergy...
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PMID: 19463208
PDF is available here.
PDF is available here.
Abstract
It is known that bioluminescence of obelin is triggered by Ca2+ the binding of which to the protein induces the decarboxylation of 2-hydroperoxycoelenterazine. The molecular mechanism of fluorescence of obelin, which determines the fluorescence of see hydroid Obelia Longissima, has been investigated...
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PMID: 19795783
PDF is available here.
PDF is available here.
Abstract
Nepafenac ophthalmic suspension 0.1% was well tolerated and effectively resolved ocular inflammation and increased the incidence of ocular pain-free patients following cataract surgery when dosed QD, BID, or TID. By postoperative day 14, all nepafenac posologies significantly reduced the incidence o...
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PMID: 19040348
PDF is available here.
PDF is available here.
Molecular Pharmacology (74)6 2008
Abstract
We used high-throughput screening (HTS) to discover a series of small molecule phenylacetamides as novel and more potent FFA2 agonists. This series is specific for FFA2 over FFA1 (GPR40) and FFA3 (GPR41), and it is able to activate both the Galpha(q) and Galpha(i) pathways in vitro on Chinese hamste...
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PMID: 18818303
PDF is available here.
PDF is available here.
Biological Psychiatry (64)11 2008
Abstract
Activation of KORs reduces the reward-related effects of cocaine. Inasmuch as cocaine-induced behavioral stimulation in rodents may model key aspects of enhanced mood in humans, these findings raise the possibility that KOR agonists might ameliorate symptoms of conditions characterized by increased...
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PMID: 18639235
PDF is available here.
PDF is available here.
Neuroscience Letters (446)2-3 2008
Abstract
Locomotor sensitization induced by the dopamine agonist quinpirole can be potentiated by co-treatment with the synthetic kappa opioid agonist U69593. The identification of salvinorin A, an active component of the psychotropic sage Salvia divinorum, as a structurally different agonist of kappa-opioid...
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PMID: 18824069
PDF is available here.
PDF is available here.
Abstract
Mu opioid receptor agonists are clinically valuable as analgesics; however, their use is limited by high abuse liability. Kappa opioid agonists also produce antinociception, but they do not produce mu agonist-like abuse-related effects, suggesting that they may enhance the antinociceptive effects and...
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PMID: 18837635
PDF is available here.
PDF is available here.
Abstract
The behavioral effects of the kappa-opioid receptor agonist U69593 were examined in lactating rats. On day 5 of lactation, animals were treated with 0.1 mg/kg of U69593 to determine whether it influences general activity and maternal latencies toward pups. Because little attention has been given to...
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PMID: 18514802
PDF is available here.
PDF is available here.
Abstract
Statistical analysis showed no difference between the nepafenac and non-nepafenac groups in delayed epithelialization (P = .61, chi-square test). Neither group had significant corneal haze. CONCLUSION: Nepafenac did not appear to delay corneal epithelial healing or contribute to haze formation after...
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PMID: 18721717
PDF is available here.
PDF is available here.
Journal of Neuroscience (28)36 2008
Abstract
We report that amygdala (AMYG)-projecting VTA DA neurons have brief APs and lack D(2)R agonist (quinpirole; 1 microM) autoinhibition. However, they are hyperpolarized by both the GABA(B) agonist baclofen (1 microM) and the kappa-opioid receptor agonist U69593 [(+)-(5alpha,7alpha,8beta)-N-methyl-N-[7...
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PMID: 18768684
PDF is available here.
PDF is available here.
Abstract
Arthritis & Rheumatism (58)8 2008
Abstract
Antigen challenge in immunized mice induced production of TNFalpha, CXCL1, and CXCL2 and also resulted in neutrophil recruitment, leukocyte rolling and adhesion, and hypernociception. Treatment with reparixin or DF2162 (allosteric inhibitors of CXCR1/CXCR2) decreased neutrophil recruitment, an effec...
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PMID: 18668539
PDF is available here.
PDF is available here.
Abstract
An HPLC method was established and validated for the determination of compound FLZ, a synthetic novel anti-Parkinson's disease candidate drug, in rat plasma. FLZ and the internal standard bicyclol were extracted from plasma by solid-phase extraction method and analyzed on a Restek C18 column (4.6 x...
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PMID: 18384063
PDF is available here.
PDF is available here.
European Journal of Pharmacology (586)1-3 2008
Abstract
Treatment with a kappa-opioid receptor agonist for 5 days decreases locomotor activity and reduces activity in response to a cocaine challenge 3 days later. In addition, chronic cocaine increases kappa-opioid receptor density, striatal dynorphin, and dynorphin gene expression in the striatum. The up...
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PMID: 18395712
PDF is available here.
PDF is available here.
Abstract
DF 2162 inhibited neutrophil chemotaxis induced by CXCR1/2 ligands but had no effect on CXCL8 binding to neutrophils. A single mutation of the allosteric site at CXCR1 abrogated the inhibitory effect of DF 2162 on CXCL-8-induced chemotaxis. Treatment with DF 2162 prevented influx of neutrophils and...
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PMID: 18362895
PDF is available here.
PDF is available here.
Abstract
Treatment with nepafenac 0.1% significantly reduced postoperative pain immediately following surgery and had no significant adverse effect on time to reepithelialization compared to placebo....
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PMID: 18500088
PDF is available here.
PDF is available here.
Abstract
Abstract
Abstract
Kappa-(kappa) opioid receptors are widely distributed in the periphery and activation results in antinociception; however supraspinal acting kappa-agonists result in unwanted side effects. Two novel, all d-amino acid, tetrapeptide kappa-opioid receptor agonists, FE 200665 and FE 200666, were identif...
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PMID: 18282565
PDF is available here.
PDF is available here.
Clinical Cancer Research (14)6 2008
Abstract
We set out to find a means to specifically induce senescent tumor cells to undergo cell death and not to reenter the cell cycle that may have general application in cancer therapy....
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PMID: 18347191
PDF is available here.
PDF is available here.
Abstract
Neuropsychopharmacology (33)4 2008
Acute amphetamine exposure selectively desensitizes kappa-opioid receptors in the nucleus accumbens.
Abstract
We investigated the effects of psychostimulant exposure on kappa-opioid peptide (KOP) receptor signaling in the rat mesolimbic system. A single subcutaneous (s.c.) injection of amphetamine (2.5 mg/kg) reduced the KOP receptor-mediated inhibition of glutamate release in the nucleus accumbens shell, a...
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PMID: 17551543
PDF is available here.
PDF is available here.
Abstract
DF2162 prevented chemotaxis of rat and human neutrophils induced by chemokines acting on CXCR1/2. DF2162 was orally bioavailable and metabolized to two major metabolites. Only metabolite 1 retained CXCR1/2 blocking activity. Treatment with DF2162 (15 mg kg(-1), twice daily) or metabolite 1, but not...
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PMID: 17891165
PDF is available here.
PDF is available here.
Abstract
We report a strategy for narrowly changing the biophysicochemical properties of NPs in a reproducible manner, thereby enabling systematic screening of optimally formulated drug-encapsulated targeted NPs. NPs were formulated by the self-assembly of an amphiphilic triblock copolymer composed of end-to...
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PMID: 18272481
PDF is available here.
PDF is available here.
Behavioral Neuroscience (122)1 2008
Abstract
These results indicate that the acute effects of U-69593 are independent of estradiol treatment. Repeated exposure to U-69593 (0.32 mg/kg) prior to cocaine decreased the development of behavioral sensitization in OVX-EB-implanted rats. This decrease in cocaine-induced hyperlocomotion persisted after...
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PMID: 18298258
PDF is available here.
PDF is available here.
Abstract
We reported the thiourea antagonists 2a and 2b as potent and high affinity TRPV1 antagonists. For further optimization of the lead compounds, a series of their amide and alpha-substituted amide surrogates were investigated and novel chiral N-(2-benzyl-3-pivaloyloxypropyl) 2-[4-(methylsulfonylamino)p...
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PMID: 18072720
PDF is available here.
PDF is available here.
Abstract
Inflammation plays an important role in the pathogenesis of Parkinson's disease (PD) through over-activation of microglia, which consequently causes the excessive production of proinflammatory and neurotoxic factors, and impacts surrounding neurons and eventually induces neurodegener...
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PMID: 18507839
PDF is available here.
PDF is available here.
Abstract
Inflammation plays an important role in the pathogenesis of Parkinson's disease (PD) through over-activation of microglia, which consequently causes the excessive production of proinflammatory and neurotoxic factors, and impacts surrounding neurons and eventually induces neurodegener...
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PMID: 18507839
PDF is available here.
PDF is available here.
Abstract
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 uncontrollable shock (shock independent of leg posit...
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PMID: 17983769
PDF is available here.
PDF is available here.
Abstract
Positive penicillin skin test results for patients with a remote history of non-life-threatening allergic reaction to penicillin were not associated with a greater prevalence of adverse reactions to oral challenge with penicillin than negative results. Because skin testing is considered the gold sta...
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PMID: 18254480
PDF is available here.
PDF is available here.
Abstract
This study evaluated the validity of measuring fentanyl concentrations in equine plasma using radioimmunoassay (RIA) by comparing it to the established technique of liquid chromatography-mass spectrometry (LC-MS). Equine plasma samples were analyzed using a solid-phase Coat-A-Count fentanyl RIA and...
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PMID: 19021930
PDF is available here.
PDF is available here.
Abstract
We compared the in vitro receptor binding selectivity of salvA and four analogs containing an ethyl ether (EE), isopropylamine (IPA), N-methylacetamide (NMA), or N-methylpropionamide (NMP) at C-2. All compounds showed high binding affinity for the KOR (K(i) = 0.11-6.3 nM), although only salvA, EE, a...
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PMID: 17951511
PDF is available here.
PDF is available here.
Abstract
Abstract
The aim of the present study was to access the protective effect of a novel synthesized squamosamide cyclic analogue, compound FLZ, on memory impairment in artificially senescent mice induced by chronic injection of D-galactose and sodium nitrite (NaNO(2)). Artificially senescent mouse model was ind...
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PMID: 17971066
PDF is available here.
PDF is available here.
Abstract
We describe 6 patients with CME and 1 patient with diabetic macular edema (DME), all of whom were treated with nepafenac 0.1%, a novel prodrug NSAID. Three (3) patients with acute CME following cataract surgery were treated for 3-4 weeks with nepafenac 0.1%, with or without concomitant steroids. Bot...
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PMID: 18001248
PDF is available here.
PDF is available here.
Psychopharmacology (194)4 2007
Abstract
Distinct alterations of D2R and DYN mRNA levels in SN and Acb/STR, respectively, strengthen the evidence implicating pre- and postsynaptic changes in augmented locomotor sensitization to U69593/QNP cotreatment. It is suggested that repeated U69593/QNP cotreatment may augment locomotor sensitization...
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PMID: 17619861
PDF is available here.
PDF is available here.
Abstract
Abstract
We sought small organic molecules for lead candidate CYP51 inhibitors. The changes in CYP51 spectral properties following ligand binding make CYP51 a convenient target for high-throughput screening technologies. These changes are characteristic of either substrate binding (type I) or inhibitor bindi...
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PMID: 17846131
PDF is available here.
PDF is available here.
Abstract
We describe a patient with systemic graft-versus-host disease who developed a nonhealing epithelial defect after cataract surgery that healed on cessation of a topical nonsteroidal antiinflammatory drug (NSAID) (ketorolac). The patient developed a central corneal perforation in the fellow eye while...
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PMID: 17964407
PDF is available here.
PDF is available here.
Abstract
The ketorolac group consisted of 94 patients (100 eyes) and the nepafenac group, 89 patients (93 eyes). The between-group differences in visual outcomes and anterior chamber inflammation were not statistically significant (mean P = .33). There was a higher incidence of posterior capsule opacificatio...
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PMID: 17964399
PDF is available here.
PDF is available here.
Abstract
These results suggest that select opioid ligands up-regulate rKOR by enhancing the rate of receptor folding and maturation and by protecting the receptor from degradation, resulting in an increase in the number of rKOR binding sites, immunoreactive protein, and functional receptors....
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PMID: 17720886
PDF is available here.
PDF is available here.
Abstract
Our results demonstrate that UK-201844 represents the prototype for a unique HIV-1 inhibitor class that directly or indirectly interferes with HIV-1 gp160 processing....
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PMID: 17646410
PDF is available here.
PDF is available here.
Behavioral Neuroscience (121)5 2007
Abstract
Repeated injections of the D2/D3 dopamine agonist, quinpirole, induce locomotor sensitization and compulsive checking behavior in rats, a phenomenon that may constitute an animal model of obsessive- compulsive disorder (OCD). Considering that the co-joint treatment with quinpirole and the kappa opio...
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PMID: 17907829
PDF is available here.
PDF is available here.
Biological Psychiatry (62)6 2007
Abstract
In Sprague-Dawley rats, psychotropic drugs with distinct pharmacological profiles produced distinguishable effects in the 5CSRTT. The effects of these classes of drugs under our testing conditions are qualitatively similar to their effects in humans....
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PMID: 17343834
PDF is available here.
PDF is available here.
Abstract
An efficient xanthate-based method for the preparation of azaspirocyclic cyclohexadienones via an ipso oxidative radical cyclization of p-oxygenated N-benzylacetamides and N-phenetylacetamide is described.
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PMID: 17700890
PDF is available here.
PDF is available here.
Carcinogenesis (28)9 2007
Abstract
These results indicate that the topical administration of a COX-2 inhibitor delayed the progression of this malignancy in our animal model. A clinical trail using an anti-COX-2 inhibitor for patients with UM should be considered....
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PMID: 17434930
PDF is available here.
PDF is available here.
Neuropharmacology (53)4 2007
Abstract
Data from clinical and preclinical studies converge implicating the plant-derived hallucinogen salvinorin A as an important pharmacologic tool; this psychoactive compound may expand scientific understandings on mammalian kappa-opioid receptor systems. Human salvinorin A effects, consistent with kapp...
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PMID: 17681558
PDF is available here.
PDF is available here.
Abstract
These results suggest that long-term effect of KOR activation results in facilitation of amphetamine-induced DA extracellular levels in the NAc accompanied by sensitization of amphetamine-induced increase in locomotor activity....
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PMID: 17568430
PDF is available here.
PDF is available here.
Abstract
Postoperatively, 240 patients were treated with prednisolone and 210 patients, with prednisolone-nepafenac. Preoperatively, the 2 groups were demographically and clinically comparable in sex distribution (P = .8400), history of diabetes (P = .7267), hypertension or cardiac disease (P = .8690), and c...
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PMID: 17720068
PDF is available here.
PDF is available here.
Abstract
Seventy-five patients participated in the study. The prodrug nepafenac had the shortest time to peak concentration and the greatest peak aqueous humor concentration (C(max)). The C(max) of nepafenac was significantly higher than that of the other drugs (P<.05), including the higher-concentration ket...
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PMID: 17720067
PDF is available here.
PDF is available here.
Abstract
Topical nonsteroidal anti-inflammatory agents have been associated with corneal ulceration and stromal melts. This is, to our knowledge, the first reported case involving the new agent, Nepafenac....
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PMID: 17721306
PDF is available here.
PDF is available here.