piperidine/הקאה

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Synthesis of spiro[isobenzofuran-1(3H),4'-piperidines] as potential central nervous system agents. 4. Central nervous system depressants.

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התחבר הרשם

The synthesis of 1'-[3-(4-fluorobenzyoyl)propyl]-3-phenylspiro[isobenzofuran-1(3H),4'-piperidine] (2a) and eight halo and methoxy analogues is described. The compounds were generally more potent per os than chlorpromazine in the Sidman avoidance paradigm in rats and less potent than haloperido.

Ethanol-induced emesis in the house musk shrew, Suncus murinus.

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התחבר הרשם

Ethanol-induced emesis were investigated using Suncus murinus and the emetogenic mechanisms of ethanol were compared with those of cisplatin. Intraperitoneal injection of ethanol caused dose-dependent emesis with ED50 value of 22.3% (v/v) when injection volume was adjusted to 4 ml/kg.

Sigma ligand-induced emesis in the pigeon.

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התחבר הרשם

Pigeons were fed a fixed amount of grain-based feed and behavior was observed after administration of doses of ditolyguanidine (DTG), (+)-3-(3-hydroxyphenyl)-N-(1-propyl)-piperidine [(+)-3-PPP], dextromethorphan, haloperidol, (+)-N-allylnormetazocine (NANM),

Exploration of a new type of antimalarial compounds based on febrifugine.

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התחבר הרשם

Febrifugine (1), a quinazoline alkaloid, isolated from Dichroa febrifuga roots, shows powerful antimalarial activity against Plasmodium falciparum. The use of 1 as an antimalarial drug has been precluded because of side effects, such as diarrhea, vomiting, and liver toxicity. However, the potent

In vitro and in vivo predictors of the anti-emetic activity of tachykinin NK1 receptor antagonists.

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התחבר הרשם

The ability of tachykinin NK1 receptor antagonists to inhibit GR73632 (D-Ala-[L-Pro9,Me-Leu8]substance P-(7-11))-induced foot tapping in gerbils was employed as an indirect measure of brain penetration and this was compared with their ability to prevent acute emesis induced by cisplatin in ferrets.

[Remifentanil].

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התחבר הרשם

Remifentanil is a potent mu-opioid receptor agonist and has some unique pharmacokinetic characteristics compared to other anilidopiperidine opioids (e.g. fentanyl, alfentanil, and sufentanil). As remifentanil is metabolised rapidly by nonspecific esterases that are widespread throughout the plasma

Pharmacological profiles of the putative dopamine autoreceptor agonists 3-PPP and TL-99.

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התחבר הרשם

The putative dopamine (DA) autoreceptor agonists, N-n-propyl-3-(3-hydroxyphenyl)-piperidine (3-PPP) and 6, 7-dihydroxy-2-dimethylaminotetralin (TL-99) were compared with apomorphine in a series of tests indicative of DA receptor activation. All three agents displaced [3H] apomorphine and [3H]

Identification of metabolites of a substance P (neurokinin 1 receptor) antagonist in rat hepatocytes and rat plasma.

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התחבר הרשם

[3R,5R,6S]-3-(2-cyclopropyloxy-5-trifluoromethoxyphenyl)-6-phenyl-1-oxa-7-azaspiro[4.5]decane is a substance P (Neurokinin 1 receptor) antagonist. Substance P antagonists are proven in concept to have excellent potential for the treatment of major depression, and they allow superior and sustained

Management of cognition and function: new results from the clinical trials programme of Aricept(R) (donepezil HCl).

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התחבר הרשם

Ideally, treatment for Alzheimer's disease (AD) should prevent or cure the disease. Unfortunately, these goals appear unobtainable in the foreseeable future. Nevertheless, symptomatic relief is a feasible treatment option for AD patients and is available currently in the form of cholinesterase

Efficacy of different dose of dexmedetomidine combined with remifentanil in colonoscopy: a randomized controlled trial

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התחבר הרשם

Background: Dexmedetomidine has advantages during colonoscopy as it allows the patient to cooperate during the procedure. Few studies examined the dexmedetomidine-remifentanil combination. This study was to evaluate the effects of

Separation of Unprecedented Degradants of Domperidone by Ultra-Performance Convergence Chromatography and Their Structure Elucidation.

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התחבר הרשם

Domperidone, a gastroprokinetic agent, is a common drug to treat emesis. It was subjected to acid, base-mediated hydrolysis, peroxide-mediated oxidation, photolysis and thermal degradation according to ICH guidelines to observe stability of the selected drug under the stress conditions. Although the

Structural optimization affording 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonist.

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התחבר הרשם

Structural modifications requiring novel synthetic chemistry were made to the morpholine acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this resulted in the discovery of 2-(R)-(1-(R)-3, 5-bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-ox o-1 ,2,4-triazol-5-yl)methyl

Poison hemlock (Conium maculatum L.).

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התחבר הרשם

One of the most poisonous species amongst higher plants is Conium maculatum. It is a very common nitrophile weed species, belonging to the Apiaceae (formerly Umbelliferae) family. It contains some piperidine alkaloids (coniine, N-methyl-coniine, conhydrine, pseudoconhydrine, gamma-coniceine), which

Donepezil: a clinical review of current and emerging indications.

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התחבר הרשם

This article reviews the piperidine derivative, donepezil hydrochloride (E2020, Aricept), a reversible central acetylcholinesterase inhibitor currently approved for treatment of mild-to-moderate Alzheimer's disease. Donepezil is well absorbed orally, unaffected by food or by time of administration;

Suicidal death after injection of a castor bean extract (Ricinus communis L.).

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התחבר הרשם

The castor bean plant (Ricinus communis L.) or wonder tree is cultivated in many countries as an ornamental annual plant in gardens. The highest concentration of the lectin ricin is present in the seeds and pods. Ricin is considered as one of the most toxic natural poisons. Ricinine is a piperidine

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