A series of Ruthenium-Quinolinol complexes (3a–d & 4a–d) has been synthesized by employing a simple, efficient and environmental friendly condition. Catalytic role of Amberlite IRA-120(H) has been demonstrated. The structures of the new compounds were elucidated by the analysis of spectroscopi...
Crystal structures of the three geometrical isomers (1, 2 and 3) of [RuCl(2eqn)2NO] (H2eqn = 2-ethyl-8-quinolinol) have been determined by X-ray diffraction. The Cl atom is cis to the NO group in 1 and 2, and is trans to the NO group in 3. The N and O atoms of the two quinolinolato ligands for 1...
Hydrous nitrosylruthenium(III) halide reacts with 8-quinolinol or its derivative (2-methyl- or 5-chloro-8-quinolinol) in ethyl alcohol or acetonitrile to give [RuX3(N-O)(NO)]− [X = Cl or Br; H(N-O) = 8-quinolinol or its derivative]. All the halide ions are coordinated cis to the nitrosyl and the...
A recognition pharmacophore for the delta opioid receptor was developed de novo. Through the use of the pharmacophore and a novel four-point recognition model, major differences were observed between oxymorphindole and SNC80. This work suggests that these two classes of delta selective opioids d...
The presence of a 6,7-fused indole group in the indolomorphinans was considered to be responsible for the delta opioid selectivity for this class of ligands. Herein is shown that 5′-halogenated analogs of oxymorphindole are opioids with little selectivity for delta receptors over mu opioid rece...
The potentiation of the toxic and lethal effects of cocaine by the selective δ-opioid receptor antagonist naltrindole was explored in unrestrained, unanesthetized rats that received a continuous intravenous infusion of cocaine until death. The lethal dose of cocaine was lowered dose dependently...
Pharmacological characterization of the main metabolites of nalfurafine hydrochloride ((E)–N-[17-(cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxymorphinan-6β-yl]-3-(furan-3-yl)–N-methylprop-2-enamide monohydrochloride; a selective κ-opioid receptor agonist and an antipruritic for uremic prurit...
A conditioned place preference paradigm was used to determine whether: (i) prior exposure to cocaine results in an enhancement of its rewarding effects, and (ii) the δ-opioid receptor antagonist naltrindole can prevent the development of this response. Rats received daily injections of saline o...
The effects of naltrindole, a selective δ-opioid receptor antagonist, on the capsaicin-induced cough reflex in mice and rats were studied. Intraperitoneal administration of naltrindole decreased the number of coughs both in mice and rats dose dependently. The cough-depressant effects reached a ...
The influence of the δ-opioid receptor antagonist naltrindole upon sensitization to the locomotor activating effects of cocaine was assessed. Activity in response to a challenge dose of cocaine (20 mg/kg, i.p.) was significantly increased in rats which had received cocaine (20 mg/kg, i.p.) once...
Although compounds with relative selectivity for the mu and kappa opiate receptors subtypes have been reported to condition taste aversions, it is not known whether systemically administered delta compounds have the ability to produce aversions. To that end, female Long-Evans rats were adapted t...
Although the interactions between the μ- and the δ-opiate receptor subtypes are well documented with regard to supraspinal analgesia, less is known about the mutual interactions on respiratory depression. To clarify the functional interactions between both opiate receptor subtypes with regard ...
We synthesized derivatives of the δ opioid receptor (DOR) antagonists naltrindole (NTI) and compound 1 that were modified with small alkyl or fluorinated ethyl substituents on the 17-nitrogen. Although the derivatives showed decreased binding affinities for the opioid receptors, their selectivi...
Intracerebroventricular (i.c.v.) injection of the δ-opioid receptor antagonist naltrindole hydrochloride (2.2–22.2 nmol) in mice produced a dose-dependent increase in tail flick and hot plate latencies with respective ED50 and 95% confidence limits of 10.6 (8.3–13.9) and 16.4 (9.2–62.3) nmol...
Oxycodone, a widely prescribed and very potent oral opioid analgesic agent, is highly addictive and has many side effects, including troublesome constipation. Our studies in mice indicated that pretreatment of naltrindole did not significantly affect the analgesic efficacy of oxycodone but atten...
In this paper, a novel soluble low bandgap π-conjugated polymer, poly{(3-butyryl)pyrrole-[2,5-diyl(p-hydroxybenzylidene)]} (PBPDHBE), was synthesized and characterized by 1H NMR, FT-IR, EA and GPC. The glass transition temperature (Tg) of PBPDHBE was found to be 272.11 °C that was about 70 °C...
The acylation of novobiocin by carboxylic acid anhydrides leading to preparation of three families of semi-synthetic acylated novenamine analogues is reported. ESI-MS was used to monitor the reaction progress and enabled the isolation of intermediate compounds that provided insights into the seq...
The inversion of the chiral centers in (R)/(S)-naproxen–(S)-tryptophan linked system under UV irradiation has been detected by the 1H NMR spectroscopy as an example of the (R,S)-diastereomer transformation into (S,S) analogue in an achiral environment.
The strong resolving graph GSR of a connected graph G was introduced by Oellermann and Peters-Fransen (2007) as a tool to study the strong metric dimension of G. Recently, Kuziak et al. (2018) studied the realization and characterization problems of strong resolving graphs and they pose a conjec...
(R,S)-Isoproterenol inhibits the formation of toxic granular tau oligomers associated with neuronal loss and development of cognitive disorders, and is an attractive drug candidate for Alzheimer’s disease. To elucidate its behavior in the brain by positron emission tomography, we synthesize (R,...
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