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Sabah Moradi Mohammad Charkhpour Hamed Ghavimi Rasoul Motahari Majid Ghaderi Kambiz Hassanzadeh 《Journal of biomedical science》2013,20(1):77
Background
The exact mechanisms of morphine-induced dependence and withdrawal symptoms remain unclear. In order to identify an agent that can prevent withdrawal syndrome, many studies have been performed. This study was aimed to evaluate the effect of gap junction blockers; carbenoxolone (CBX) or mefloquine (MFQ); on morphine withdrawal symptoms in male rat.Adult male Wistar rats (225 – 275 g) were selected randomly and divided into 10 groups. All groups underwent stereotaxic surgery and in order to induce dependency, morphine was administered subcutaneously) Sc) at an interval of 12 hours for nine continuous days. On the ninth day of the experiment, animals received vehicle or CBX (100, 400, 600 μg/10 μl/rat, icv) or MFQ (50, 100 and 200 μg/10 μl/rat, icv) after the last saline or morphine (Sc) injection. Morphine withdrawal symptoms were precipitated by naloxone hydrochloride 10 min after the treatments. The withdrawal signs including: jumping, rearing, genital grooming, abdomen writhing, wet dog shake and stool weight, were recorded for 60 minutes.Results
Results showed that CBX and MFQ decreased all withdrawal signs; and the analysis indicated that they could attenuate the total withdrawal scores significantly.Conclusion
Taking together it is concluded that gap junction blockers prevented naloxone-precipitated withdrawal symptoms. 相似文献2.
Philip Magnus Bahman Ghavimi Jotham W. Coe 《Bioorganic & medicinal chemistry letters》2013,23(17):4870-4874
(?)-Codeine 1 was converted into previously unknown 7β-methyl-7,8-dihydrocodeine/morphine derivatives such as 13 via classical diaxial opening of α-epoxide 3. Several analogs exhibited dual μ/δ-agonist activity. 相似文献
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Mohammad Charkhpour Hamed Ghavimi Saeed Ghanbarzadeh Bahman Yousefi Arash Khorrami Mehran Mesgari Kambiz Hassanzadeh 《Journal of biomedical science》2015,22(1)
Background
Morphine-induced tolerance is associated with the spinal neuroinflammation. The aim of this study was to explore the effects of oral administration of the pioglitazone, the peroxisome proliferator activated receptor gamma (PPAR-γ) agonist, on the morphine-induced neuroinflammation in the lumbar region of the male Wistar rat spinal cord.Results
Co-administration of the pioglitazone with morphine not only attenuated morphine-induced tolerance, but also prevented the up-regulation of pro-inflammatory cytokines (tumor necrosis factor alpha, interleukin-1beta, and interleukin 6) and nuclear factor-kappa B activity. Administration of the GW-9662 antagonized the above mentioned effects of the pioglitazone.Conclusions
It is concluded that oral administration of the pioglitazone attenuates morphine-induced tolerance and the neuroinflammation in the lumbar region of the rat spinal cord. This action of the pioglitazone may be, at least in part, due to an interaction with the spinal pro-inflammatory cytokine expression and the nuclear factor-kappa B activity. 相似文献4.
P1 Phenethyl peptide boronic acid inhibitors of HCV NS3 protease 总被引:1,自引:0,他引:1
Priestley ES De Lucca I Ghavimi B Erickson-Viitanen S Decicco CP 《Bioorganic & medicinal chemistry letters》2002,12(21):3199-3202
A series of peptide boronic acids containing extended, hydrophobic P1 residues was prepared to probe the shallow, hydrophobic S1 region of HCV NS3 protease. The p-trifluoromethylphenethyl P1 substituent was identified as optimal with respect to inhibitor potency for NS3 and selectivity against elastase and chymotrypsin. 相似文献
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Expression of DC-SIGN by Dendritic Cells of Intestinal and Genital Mucosae in Humans and Rhesus Macaques 总被引:17,自引:0,他引:17 下载免费PDF全文
Brian Jameson Frdric Baribaud Stefan Phlmann Darlene Ghavimi Frank Mortari Robert W. Doms Akiko Iwasaki 《Journal of virology》2002,76(4):1866-1875
To better understand the role of dendritic cells (DCs) in human immunodeficiency virus (HIV) transmission at mucosal surfaces, we examined the expressions of the HIV adhesion molecule, dendritic-cell-specific ICAM-3 grabbing nonintegrin (DC-SIGN), its closely related homologue DC-SIGNR, and HIV coreceptors by distinct DC populations in the intestinal and genital tracts of humans and rhesus macaques. We also developed monoclonal antibodies (MAbs) specific for DC-SIGN or DC-SIGNR. In the Peyer's patches, DC-SIGN expression was detected in the interfollicular regions and in clusters of cells in the subepithelial dome regions. DC-SIGN expression was not found on plasmacytoid DCs. DC-SIGNR expression was restricted to endothelial cells in approximately one-third of the capillaries in the terminal ileum. In the vaginal epithelium, Langerhans' cells did not express DC-SIGN, whereas subepithelial DCs in the lamina propria expressed moderate levels of DC-SIGN. Finally, the rectum contained cells that expressed high levels of DC-SIGN throughout the entire thickness of the mucosa, while solitary lymphoid nodules within the rectum showed very little staining for DC-SIGN. Triple-color analysis of rectal tissue indicated that CCR5(+) CD4(+) DC-SIGN(+) DCs were localized just beneath the luminal epithelium. These findings suggest that DC-SIGN(+) DCs could play a role in the transmission of primate lentiviruses in the ileum and the rectum whereas accessibility to DC-SIGN(+) cells is limited in an intact vaginal mucosa. Finally, we identified a MAb that blocked simian immunodeficiency virus interactions with rhesus macaque DC-SIGN. This and other specific MAbs may be used to assess the relevance of DC-SIGN in virus transmission in vivo. 相似文献
6.
Chen XT Ghavimi B Corbett RL Xue CB Liu RQ Covington MB Qian M Vaddi KG Christ DD Hartman KD Ribadeneira MD Trzaskos JM Newton RC Decicco CP Duan JJ 《Bioorganic & medicinal chemistry letters》2007,17(7):1865-1870
A new P1' group for TACE inhibitors was identified by eliminating the oxygen atom in the linker of the original 4-(2-methylquinolin-4-ylmethoxy)phenyl P1' group. Incorporation of this 4-(2-methylquinolin-4-ylmethyl)phenyl group onto different beta-aminohydroxamic acid cores provided compound 18, which demonstrated potent porcine TACE (p-TACE) and human whole blood activity, excellent PK properties, and good selectivity against a variety of MMPs. 相似文献
7.
Ghasemi Ali Ghavimi Reza Momenzadeh Niloofar Hajian Sobhan Mohammadi Mohsen 《International journal of peptide research and therapeutics》2021,27(4):2391-2401
International Journal of Peptide Research and Therapeutics - Breast cancer is one of the well-known non-cutaneous cancers among women worldwide. In the present study, we have characterized the... 相似文献
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Ghavimi Reza Akbari Vajihe Jahanian-Najafabadi Ali 《International journal of peptide research and therapeutics》2021,27(4):2583-2594
International Journal of Peptide Research and Therapeutics - Interleukin-24 (IL-24) is known to selectively induce apoptosis in cancer cells through endoplasmic reticulum (ER) stress. However, this... 相似文献
9.
Xue CB Chen XT He X Roderick J Corbett RL Ghavimi B Liu RQ Covington MB Qian M Ribadeneira MD Vaddi K Trzaskos J Newton RC Duan JJ Decicco CP 《Bioorganic & medicinal chemistry letters》2004,14(17):4453-4459
Replacement of the amide functionality in IM491 (N-hydroxy-(5S,6S)-1-methyl-6-[[4-(2-methyl-4-quinolinylmethoxy)anilinyl]carbonyl]5-piperidinecarboxamide) with a sulfonyl group led to a new series of alpha,beta-cyclic and beta,beta-cyclic gamma-sulfonyl hydroxamic acids, which were potent TNF-alpha converting enzyme (TACE) inhibitors. Among them, inhibitor 4b (N-hydroxy-(4S,5S)-1-methyl-5-[[4-(2-methyl-4-quinolinylmethoxy)phenyl]sulfonylmethyl]-4-pyrrolidinecarboxamide) exhibited IC50 values of < 1 nM and 180 nM in porcine TACE (pTACE) and cell assays, respectively, with excellent selectivity over MMP-1, -2, -9 and -13 and was orally bioavailable with an F value of 46% in mice. 相似文献
10.
Drugs that block P-glycoprotein-modulated efflux of antiepileptic drugs in the brain, lead to increase their intracellular concentration. Addition of R-verapamil as one enantiomer of verapamil to antiepileptic drugs may facilitate the penetration of drugs to the brain and prevents their efflux from CNS without serious cardiovascular side effects. 相似文献
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