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Marianna Gregova Trencanova et al.
Chemphyschem : a European journal of chemical physics and physical chemistry, 16(11), 2466-2473 (2015-06-03)
The solvation and confinement of coumarin C153 within supramolecular host/guest complexes based on β-cyclodextrin (β-CD) and 6-deoxy-6-thio-β-cyclodextrin (β-CD-SH) in water are studied by fluorescence spectroscopy. For β-CD/C153, the 1:1 complex is proposed, and for β-CD-SH/C153 both the 1:1 and 2:1
Sivalingam Soumya et al.
Chemphyschem : a European journal of chemical physics and physical chemistry, 16(11), 2440-2446 (2015-06-16)
The microenvironments of a leucine-based organogel are probed by monitoring the fluorescence behavior of coumarin 153 (C153) and 4-aminophthalimide (AP). The steady-state data reveals distinctly different locations of the two molecules in the gel. Whereas AP resides close to the
Hayden T Ravert et al.
Nuclear medicine and biology, 29(1), 47-53 (2002-01-12)
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 enantiomer of GR89696, also known as GR103545, demonstrated high affinity in mouse brain with region to cerebellar ratios
H Nishiwaki et al.
Japanese journal of pharmacology, 77(4), 279-286 (1998-09-28)
Relationship between activation of opioid receptors and muscarinic autoinhibition in acetylcholine (ACh) release from the myenteric plexus was studied in longitudinal muscle myenteric plexus (LMMP) preparations of guinea pig ileum. A mu-receptor agonist, [D-Ala2, N-Me-Phe4, Gly5-ol] enkephalin (DAMGO), at a
R H Straub et al.
Journal of neurochemistry, 68(4), 1633-1639 (1997-04-01)
The PNS was anticipated to be involved in the modulation of immune responses. To study aspects of this neuronal-immune communication, a recently developed tissue slice method was used to study the effects of adrenergic and opioidergic transmitters on interleukin 6
Kenjiro Matsumoto et al.
Life sciences, 78(1), 2-7 (2005-09-20)
7-Hydroxymitragynine is a potent opioid analgesic alkaloid isolated from the Thai medicinal herb Mitragyna speciosa. In the present study, we investigated the opioid receptor subtype responsible for the analgesic effect of this compound. In addition, we tested whether development of
D M Hutcheson et al.
European journal of pharmacology, 383(1), 29-37 (1999-11-11)
Evidence suggests that the antinociceptive effects of selective delta-opioid receptor agonists may involve an activation of the mu-receptor in some experimental conditions. The aim of this study was to clarify the receptors involved in the antinociceptive responses of the selective
L Romanelli et al.
British journal of pharmacology, 127(4), 909-918 (1999-08-05)
1. Although cholecystokinin octapeptide sulphate (CCK-8) activates the opioid system of isolated guinea-pig ileum (GPI) whether it activates the mu- or kappa-system, or both, remains unclear. Neither is it known whether CCK-8 influences the withdrawal responses in GPI preparations briefly
H Nishiwaki et al.
Japanese journal of pharmacology, 78(1), 83-86 (1998-11-06)
Endomorphin-1 and -2, putative endogenous ligands for the mu-opioid receptor, inhibited acetylcholine (ACh) release evoked by electrical field stimulation (EFS) at 1 Hz, which partially activates muscarinic autoreceptors, but not at 10 Hz, which fully activates muscarinic autoreceptors, in longitudinal
Meixing Li et al.
Peptides, 39, 89-94 (2012-11-20)
MCRT (YPFPFRTic-NH(2)) is a chimeric opioid peptide based on morphiceptin and PFRTic-NH(2). In order to assess the cardiovascular effect of MCRT, it was administered by intravenous (i.v.) injection targeting at the peripheral nervous system and by intracerebroventricular (i.c.v.) injection targeting
B Henry et al.
Experimental neurology, 171(1), 139-146 (2001-08-25)
Long-term treatment of Parkinson's disease with levodopa is complicated by the emergence of involuntary movements, known as levodopa-induced dyskinesia. It has been hypothesized that increased opioid transmission in striatal output pathways may be responsible for the generation of dyskinesia. In
C M Hsueh et al.
Brain research, 737(1-2), 263-268 (1996-10-21)
The type of opioid receptors involved in the conditioned enhancement of natural killer (NK) cell activity is identified in the present study. In our previous observations, we have demonstrated that the conditioned enhancement of NK cell activity was dependent on
H C Jackson et al.
Psychopharmacology, 103(3), 380-383 (1991-01-01)
The effects of the selective opioid antagonists cyprodime (mu; 1, 3, 10, 30 mg/kg IP), norbinaltorphimine (kappa; 3, 10, 30 mg/kg IP) and naltrindole (delta; 0.3, 1, 3, 10 mg/kg IP) on electroshock seizure threshold in mice were compared with
Katarzyna Starowicz et al.
Neuroreport, 13(18), 2447-2452 (2002-12-25)
Co-localization of opioid and melanocortin receptor expression, especially at the spinal cord level in the dorsal horn and in the gray matter surrounding the central canal led to the suggestion that melanocortins might play a role in nociceptive processes. In
H Schmidhammer et al.
Journal of medicinal chemistry, 33(4), 1200-1206 (1990-04-01)
A series of cyprodime-related compounds (2, 4-12, and 26) has been synthesized and evaluated for opioid agonist and antagonist activity with the mouse vas deferens and guinea pig ileum preparations. None of the changes to cyprodime, including the introduction of
Zhih-Cherng Chen et al.
Pharmacology, 87(5-6), 257-264 (2011-04-16)
The role of opioid receptors in the regulation of vascular function remains unclear. In the current study, we evaluated the ability of loperamide, a peripheral opioid receptor agonist, to regulate blood pressure in spontaneously hypertensive rats (SHRs) and examined the
Mariana Spetea et al.
Journal of medicinal chemistry, 47(12), 3242-3247 (2004-05-28)
The synthesis, biological, and pharmacological evaluation of novel derivatives of cyprodime are described. Their binding affinities at mu, delta, and kappa opioid receptors were evaluated using receptor binding assay. It was observed that the affinity of these compounds was sensitive
H C Jackson et al.
Psychopharmacology, 111(4), 486-490 (1993-01-01)
This study investigates the possible involvement of opioid receptors in the action of a variety of anticonvulsant agents. The opioid antagonist naloxone (0.3, 1 mg/kg IP) and the selective mu-opioid antagonist cyprodime (3 mg/kg IP) significantly inhibited the increase in
Ana Baamonde et al.
Naunyn-Schmiedeberg's archives of pharmacology, 372(3), 213-219 (2005-11-12)
The stimulation of peripheral opioid receptors yields analgesic responses in a model of bone cancer-induced pain in mice. In order to know the type(s) of peripheral opiate receptors involved, the paw thermal withdrawal latencies were measured in C3H/HeJ mice bearing
M Cosentino et al.
Neuroscience letters, 194(3), 185-188 (1995-07-21)
We have studied the effects of mu- and kappa-opioid receptor blockade on endogenous acetylcholine and noradrenaline overflow from the myenteric plexus of the guinea-pig isolated colon. Cyprodime (putative mu-selective antagonist) and nor-binaltorphimine (kappa-selective antagonist) had a concentration-dependent facilitatory effect on
H Schmidhammer et al.
Archiv der Pharmazie, 324(4), 209-211 (1991-04-01)
N-Cyclopropylmethyl-4,14-dimethoxymorphinan (4) and N-cyclopropylmethyl-4-hydroxy-14-methoxymorphinan (5) have been prepared from cyprodime (1) by Wolff-Kishner reduction. Pharmacological studies (mouse vas deferens and guinea pig ileum preparations) revealed that there was no significant decrease of 4 in antagonist activity but in mu selectivity
A Márki et al.
European journal of pharmacology, 383(2), 209-214 (1999-12-11)
The use of compounds with high selectivity for each opioid receptor (mu, delta and kappa) is crucial for understanding the mechanisms of opioid actions. Until recently non-peptide mu-opioid receptor selective antagonists were not available. However, N-cyclopropylmethyl-4,14-dimethoxy-morphinan-6-one (cyprodime) has shown a
H Schmidhammer et al.
Journal of medicinal chemistry, 38(16), 3071-3077 (1995-08-04)
A series of 3-hydroxy-substituted analogues (3-7) of the mu selective opioid antagonist cyprodime has been synthesized in order to evaluate the role of a hydroxy group at C-3 concerning mu opioid antagonist selectivity. Compounds 3-7 were tested in bioassays (electrical
R Spanagel
Pharmacology, biochemistry, and behavior, 54(4), 645-649 (1996-08-01)
The aim of the present study was to investigate the role of different endogenous opioid systems in the expression of ethanol's discriminative stimulus effects in a two-lever operant drug discrimination paradigm. Wistar rats trained to make differential responses following the
Meixing Li et al.
Regulatory peptides, 179(1-3), 23-28 (2012-09-11)
A chimeric opioid peptide (MCRT, YPFPFRTic-NH(2)) was here designed and synthesized. This peptide was based on morphiceptin (YPFP-NH(2)) and a neuropeptide FF (NPFF) derivative (PFRTic-NH(2)) sharing one proline. This peptide is intended to produce potent analgesia. MCRT was found to
Wency Chen et al.
World journal of gastroenterology, 18(12), 1391-1396 (2012-04-12)
To investigate the role of opioid μ-receptor subtype in opiate-induced constipation (OIC). The effect of loperamide on intestinal transit was investigated in mice. Ileum strips were isolated from 12-wk-old male BALB/c mice for identification of isometric tension. The ileum strips
S Józefowski et al.
Polish journal of pharmacology, 49(4), 229-237 (1997-08-01)
The head kidney is the main lymphopoietic organ of teleost fish. It is the source of leukocytes inhabiting the peritoneal cavity during an experimental peritoneal inflammation (Gruca et al., Folia Biol.-Kraków, 1997, 44, 137-142). The number of elicited peritoneal leukocytes
Vitaliy Kapishon et al.
Biomacromolecules, 16(7), 2040-2048 (2015-06-13)
Alginate-based amphiphilic graft copolymers were synthesized by single electron transfer living radical polymerization (SET-LRP), forming stable micelles during polymerization induced self-assembly (PISA). First, alginate macroinitiator was prepared by partial depolymerization of native alginate, solubility modification and attachment of initiator. Depolymerized
B Nicol et al.
Neuroscience letters, 218(2), 79-82 (1996-11-01)
We have examined the effects of a range of opioid receptor subtype selective agonists on K+ evoked glutamate release from perfused rat cerebrocortical slices. Dual application (S1 and S2) of K+ (46 mM) evoked dual monophasic glutamate release profiles. When
Supratik Sen Mojumdar et al.
Langmuir : the ACS journal of surfaces and colloids, 28(27), 10230-10237 (2012-06-19)
Picosecond spectroscopy under a confocal microscope is employed to study solvation dynamics of coumarin 153 (C153) inside a single giant lipid vesicle (1,2-dilauroyl-sn-glycero-3-phosphocholine, DLPC) of diameter 20 μm. Fluorescence correlation spectroscopy (FCS) indicates that the diffusion coefficient (D(t)) of the
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