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PubMed1977

[Pharmacological studies of Shikon and Tooki. (2) Pharmacological effects of the pigment components, Shikonin and acetylshikonin].

Pharmacological effects of Shikonin and Acetylshikonin, pigment components of Shikon were studied in mice, rats, guinea pigs and rabbits. The only difference between the chemical structures of the two pigments is that Acetylshikonin has the acetyl radical, while Shikonin does not. Though the activity was slightly different between the two compounds, the pharmacological effect of Shikonin was similar to that of Acetylshikonin. As the two pigments were extracted by ether from Shikon, systemic administration of these pigments showed the same effect as that of ether extract of Shikon as outlined in the first report(1). These compounds had no effect on blood coagulation, but inhibited the anticoagulant effect of heparin in rats. Topical application of both pigments (50 mg of 0.1% ointment) inhibited an increased vascular permeability and acute edema induced by histamine, anti-rat rabbit serum and heat. The activity was similar to that of 0.1% phenylbutazone ointment. On the other hand, these pigments increased proliferation of granuloma tissue in the cotton pellet method and promoted would healing in rats. The results suggest that Shiunko, a main prescription of Shikon, is an effective ointment for cutaneous injuries.

Analgesics↗

PubMed1983

I. Pharmacological studies with derivatives of 2-aminotetralin, benzhydro[f]quinoline and clonidine suggest a pharmacological identity between peripheral and central alpha-2 adrenoceptors.

A series of hydroxy 2-aminotetralins, benzhydro[f]quinolines and clonidine were used to determine whether a pharmacological similarity could be demonstrated between presynaptic alpha adrenoceptors which modulate autonomic transmission in the guinea pig. Compounds were assayed on isolated field stimulated guinea-pig ilea (GPI) to determine their inhibitory activities on cholinergic transmission. Inhibition of noradrenergic transmission was determined by assaying compounds on isolated field stimulated guinea-pig atria. 2-Aminotetralins, benzhydro[f]quinolines and clonidine impaired cholinergic and noradrenergic transmission by interacting with presynaptic alpha-2 adrenoceptors. A correlation (r = 0.95; P less than .05) was demonstrated between the activity of a compound on the GPI and guinea-pig atria. IC50 values obtained on GPI were correlated with previously reported IC50 values obtained for binding [3H]clonidine sites in homogenates of calf frontal cortex. A significant correlation was demonstrated (r = 0.99; P less than .05). These data suggest that alpha-2 adrenoceptors localized on guinea-pig atria and GPI are pharmacologically similar. In addition, a similar structure activity relationship was demonstrated for presynaptic alpha-2 adrenoceptors on GPI and binding sites labeled by [3H]clonidine in the calf frontal cortex.

Animals↗

PubMed2025

Molecular mechanism of HaiZao-YuHu decoction in breast cancer treatment via network pharmacology and molecular docking: Computational pharmacology.

BACKGROUND: The molecular biological mechanisms of HaiZao-YuHu decoction were investigated using network pharmacology and molecular docking. METHODS: TCMSP database was used to collect the active ingredients and action targets of HaiZao-YuHu decoction, through the OMIM, PharmGkb, GeneCards, TDD, and DurgBank database query targets for breast cancer. Then, using the intersecting targets, the protein-protein interaction network of HaiZao-YuHu decoction was constructed using the STRING website. Network topology analysis was performed using Cytoscape 3.9.0 to identify the core targets. Gene ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analyses were performed with the R package. The Autodock software was used for molecular docking. RESULTS: Thirty-four active ingredients, 219 intersection targets and 4 key targets were obtained. gene ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis get 2152 biological processes and 186 pathways. Molecular docking showed that the 4 core targets could combine well with the 5 main active components. CONCLUSION: HaiZao-YuHu decoction can play a role in the treatment of breast cancer through multi-targets, multi-components, and multi-pathways.

Molecular Docking Simulation↗

PubMed1990

Clinical pharmacology and primary health care in Europe--a gap to bridge. The WHO Working Group on Clinical Pharmacology in Europe.

A group of senior European clinical pharmacologists presents a position paper on the possible role of clinical pharmacology (CP) in bridging the gap between academic drug evaluation and drug prescribing in primary health care (PHC). As a teaching, research and service discipline CP has developed in academic or other major hospitals while 80% of all drugs are prescribed in PHC. CP therefore has to extend its functions to PHC. Examples are given of how joint ventures between clinical pharmacologists and PHC physicians may improve the quality of drug research and increase the clinical relevance of drug information in PHC, thereby contributing towards rational drug utilization in PHC. Colleagues in PHC are invited to respond to this call for collaboration.

Drug Prescriptions↗

PubMed1993

Drug utilization and clinical pharmacology. Report on British Pharmacological Society Symposium at Trinity College Dublin on Thursday, 9th July, 1992.

The insatiable appetite for safer more effective, but increasingly more expensive, therapy in the face of increasing government reluctance to feed this demand has put the study of drug utilization and pharmacoeconomics centre stage. Clinical pharmacologists are uniquely positioned to determine the cost benefit and utility of modern therapy and give impartial advice on safe, effective and economic patient care. To mark the Quatercentenary Celebrations of Trinity College Dublin, eight speakers addressed this theme in a symposium held in conjunction with the British Pharmacological Society Meeting in July 1992.

Congresses as Topic↗

PubMed2003

Pharmacologically regulated induction of silent mutations (PRISM): combined pharmacological and genetic approaches for learning and memory.

Mouse transgenic and knock-out approaches have made fundamental contributions to our understanding of the molecular and cellular bases of learning and memory. These approaches have successfully identified a large number of molecules with either a central or modulatory role in learning and memory. However, there are limitations associated with first-generation mutant mice, which include, for example, the lack of temporal control over the mutation. Recent technical developments have started to address some of these shortcomings. Here, the authors review a newly developed inducible approach that takes advantage of synergistic interactions between subthreshold genetic and pharmacological manipulations. This approach is easily set up and can be used to study the functional interactions between molecules in signaling pathways.

Animals↗

PubMed1999

[Pharmacological vigilance and pharmacological epidemiology: principles, definition, methods and current trends in neurology].

It is now well established that only clinical trials performed before drug approval are not sufficient for a full modern pharmacological evaluation of drugs and treatments. The need of both pharmacovigilance and pharmacoepidemiology is underlined in order to evaluate drugs under real conditions. After a summary of methods used in pharmacoepidemiological trials (spontaneous reports, imputability assessment, cohorts, case control studies etc.), recent pharmacoepidemiological data useful for the neurologist are summarized: side effects of tacrine and vaccines, serotoninergic syndrome and side effects of new antiepileptic drugs.

Anticonvulsants↗

PubMed1997

Pharmacological management of alcohol withdrawal. A meta-analysis and evidence-based practice guideline. American Society of Addiction Medicine Working Group on Pharmacological Management of Alcohol Withdrawal.

OBJECTIVE: To provide an evidence-based practice guideline on the pharmacological management of alcohol withdrawal. DATA SOURCES: English-language articles published before July 1, 1995, identified through MEDLINE search on "substance withdrawal--ethyl alcohol" and review of references from identified articles. STUDY SELECTION: Articles with original data on human subjects. DATA ABSTRACTION: Structured review to determine study design, sample size, interventions used, and outcomes of withdrawal severity, delirium, seizures, completion of withdrawal, entry into rehabilitation, adverse effects, and costs. Data from prospective controlled trials with methodologically sound end points corresponding to the Diagnostic and Statistical Manual of Mental Disorders, Fourth Edition, were abstracted by 2 independent reviewers and underwent meta-analysis. DATA SYNTHESIS: Benzodiazepines reduce withdrawal severity, reduce incidence of delirium (-4.9 cases per 100 patients; 95% confidence interval, -9.0 to -0.7; P=.04), and reduce seizures (-7.7 seizures per 100 patients; 95% confidence interval, -12.0 to -3.5; P=.003). Individualizing therapy with withdrawal scales results in administration of significantly less medication and shorter treatment (P<.001). beta-Blockers, clonidine, and carbamazepine ameliorate withdrawal severity, but evidence is inadequate to determine their effect on delirium and seizures. Phenothiazines ameliorate withdrawal but are less effective than benzodiazepines in reducing delirium (P=.002) or seizures (P<.001). CONCLUSIONS: Benzodiazepines are suitable agents for alcohol withdrawal, with choice among different agents guided by duration of action, rapidity of onset, and cost. Dosage should be individualized, based on withdrawal severity measured by withdrawal scales, comorbid illness, and history of withdrawal seizures. beta-Blockers, clonidine, carbamazepine, and neuroleptics may be used as adjunctive therapy but are not recommended as monotherapy.

Adrenergic beta-Antagonists↗

PubMedDate not supplied

Trazodone hydrochloride: a wide spectrum antidepressant with a unique pharmacological profile. A review of its neurochemical effects, pharmacology, clinical efficacy, and toxicology.

Trazodone is a new antidepressant agent that was recently introduced in the United States. It has a unique pharmacological profile that is not typical of either tricyclic or monoamine oxidase inhibitor antidepressants. As such it represents a new class of antidepressant drugs. The efficacy of trazodone has been clearly established in comparative studies with imipramine and amitriptyline. Major depression is the principal indication for its use, but good results have been shown in a wide variety of depressive subtypes. Of particular importance is the low frequency of adverse reactions seen with this drug.

Animals↗

PubMed1995

Correlation between the pharmacology of long-term potentiation and the pharmacology of memory.

The pharmacology of memory has been recently studied by the infusion of drugs into the hippocampus (HIP), amygdala (AMY), medial septum (MS), and entorhinal cortex (EC) at various times after training or at the time of retention testing. It was found to be remarkably similar to that of long-term potentiation (LTP). Memory and LTP are blocked early on by antagonists of glutamate N-methyl-D-aspartate (NMDA) or metabotropic receptors (mGLUs), by the antagonist of the presynaptic membrane receptor to PAF, BN 52021, by the inhibitor of heme oxygenase, ZnPP, by the inhibitor of NO synthase, N-nitro-arginine, by GABA type A receptor agonists, or by muscarinic blockers. Both memory and LTP are enhanced, at this early stage, by glutamate, mGLU agonists, GABA-A antagonists, muscarinic agonists, and norepinephrine. In the next 1-3 h, memory and LTP are accompanied by enhanced activity of protein kinases and are blocked by specific inhibitors of calcium/calmodulin dependent protein kinase II and protein kinase C. At the time of expression, memory and LTP are blocked by antagonists of glutamate AMPA receptors and are accompanied by an enhanced sensitivity of these receptors. Memories that depend on HIP are affected by drugs given into the HIP but not the MS or AMY, memories that depend on the AMY are affected by drugs given into the AMY, and memories that depend on the HIP, AMY, and MS are affected by drugs given into the three structures.(ABSTRACT TRUNCATED AT 250 WORDS)

Amygdala↗

PubMed1982

An improved pharmacological procedure for depletion of noradrenaline: pharmacology and assessment of noradrenaline-associated behaviors.

A pharmacological procedure which initially depletes noradrenaline (NA), dopamine (DA) and 5-hydroxytryptamine (5-HT) but permits repletion of DA and 5-HT was used to evaluate the role of NA in feeding behavior and intracranial self-stimulation behavior. The rapid-onset 'reserpine-like' vesicular depletion drug RO 4-1284 reduced NA and 5-HT 99% and DA 90% in rat forebrain within 1 h after administration with complete repletion of all amines occurring within 6 to 12 h. Treatment with the dopamine-beta-hydroxylase inhibitor FLA-63 significantly reduced NA (maximum depletion 42%) but not DA or 5-HT over the 12 h period of evaluation. The two drugs together produced a specific depletion of NA. Forebrain levels of NA in subjects pretreated with FLA-63 then given RO 4-1284 0.5 h later were reduced to 2% of control values for 8 h while vesicular stores of DA and 5-HT were repleted 77% and 93%, respectively, within 8 h after administration. Selective depletion of NA, in this manner, reduced deprivation induced food intake and lateral hypothalamic self-stimulation.

2H-Benzo(a)quinolizin-2-ol, 2-Ethyl-1,3,4,6,7,11b-↗

PubMed2005

Benzodiazepine receptor ligands. 8: synthesis and pharmacological evaluation of new pyrazolo[5,1-c] [1,2,4]benzotriazine 5-oxide 3- and 8-disubstituted: high affinity ligands endowed with inverse-agonist pharmacological efficacy.

The synthesis and the binding study of new 3-arylesters and 3-heteroarylpyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide 8-substituted are reported. The nature of these substituents (in terms of lipophilic and electronic features) seems to influence the binding affinity. High-affinity ligands were studied in mice in vivo for their pharmacological effects, considering six potential benzodiazepine actions: anxiolytic-like effects, muscle relaxant effects, motor coordination, anticonvulsant action, spontaneous motor activity, and ethanol-potentiating action. Compounds 4d and 6d showed an inverse-agonist profile. These compounds were evaluated also for their binding at benzodiazepine site on GABAA receptor complex (GABAA/BzR complex) subtype to evaluate their subtype selectivity.

Animals↗

PubMed2002

Synthesis and pharmacological activity of new carbonyl derivatives of 1-aryl-2-iminoimidazolidine: part 2. Synthesis and pharmacological activity of 1,6-diaryl-5,7(1H)dioxo-2,3-dihydroimidazo[1,2-a][1,3,5]triazines.

Synthesis and pharmacological activity of 1,6-diaryl-5,7(1H)dioxo-2,3-dihydroimidazo-[1,2-a][1,3,5]triazines (C) are presented. The title compounds were obtained from 1-arylimidazolinurea derivatives in cyclization reaction with difunctional carbonyl reagents--phosgene (method I) or carbonyldiimidazole (CDI) (method II). Their molecular structures were confirmed by the X-ray analysis of 1-phenyl-6-(4-chlorophenyl)-5,7(1H)-dioxo-2,3-dihydroimidazo[1,2-a][1,3,5]triazine (C2) crystals. Compounds C exhibited significant depressive action on the central nervous system (CNS) of the laboratory animals, correlated with very low acute toxicity (LD(50) > 2000 mg kg(-1) i.p.), and showed antinociceptive activity in behavioural models. Reversion of this effect by small dose of naloxone (5 mg kg(-1)) can suggest opioid-like mechanism of antinociception produced by these and other carbonyl derivatives of 1-aryl-2-iminoimidazolidine. Additionally, an effect on the serotonin neurotransmission pathway was also observed. The receptor mechanism of activity for investigated compounds was confirmed only for the opioid mu receptor in binding affinity assay test. Same tests performed for the serotonin 5-HT(2) and benzodiazepine BZD receptors showed no affinity for tested compounds. The opioid-like and serotonergic activities are similar to these described earlier for chain carbonyl 1-aryl-2-iminoimidazolidine derivatives containing urea moiety, mainly due to similar chemical structure, although compounds C are not able to adopt any of the higher energy conformations of urea derivatives. Rigid location of aromatic ring (Ar') at N6, acting as a spacer blocking any direct access to the carbonyl groups (e.g. through the hydrogen bonding), could be responsible for lack of affinity toward 5-HT(2) expressed in the binding assay test.

5-Hydroxytryptophan↗

PubMed1997

Neuromuscular transmission and its pharmacological blockade. Part 2: Pharmacology of neuromuscular blocking agents.

Clinically, neuromuscular blockade is induced with either depolarizing or non-depolarizing relaxants. Suxamethonium is the only depolarizing relaxant still in use. It is hydrolysed in the plasma by pseudo-cholinesterase (plasma cholinesterase). In some patients and in particular diseases the plasma cholinesterase activity is low and hence the effect of suxamethonium prolonged. Suxamethonium is characterized by side-effects such as myalgia, fasciculations and increase in intraocular, intracranial and intragastric pressure. More serious adverse reactions are masseter muscle spasm and potassium release, in patients with some neuromuscular diseases and increase in extrajunctional acetylcholine receptors. As non-depolarizing muscle relaxants benzylisoquinolines and steroidal compounds are mainly used. Each relaxant has its own pharmacological characteristics. The effect of most relaxants depends on liver and renal function because the pharmacokinetic behaviour is strongly dependent on these organs. Also, acid base balance disturbances, change in temperature, and neurological diseases have an effect on the profile of the relaxants. A number of drugs (anaesthetics, antibiotics, antiepileptics, etc.) have an effect on neuromuscular transmission, and thus interact with the relaxants. Some non-depolarizing relaxants cause histamine release and cardiovascular effects.

Body Temperature↗

PubMed2026

Pharmacological and non-pharmacological modulation of striatal dopamine release: a meta-analysis of [11C]raclopride PET studies.

The dopaminergic system has long been a central focus of functional neuroimaging. Positron emission tomography (PET) with the D2/D3 receptor radioligand [11C]raclopride remains the most widely used method for indirectly quantifying striatal dopamine release in vivo. However, no previous meta-analysis has studied the relative magnitude and regional distribution of dopamine release across different interventions or cognitive interventions overall. To address this gap, in this meta-analysis of 92 [11C]raclopride PET studies (n = 1640), we compared the magnitude and regional distribution of dopamine release induced by amphetamine, methylphenidate, ketamine, alcohol, and cognitive challenges with and without reward. Amphetamine induced approximately four-fold greater dopamine release than cognitive challenges (10.9 vs. 2.7%, p < 0.001), and approximately twice that of alcohol (4.8%, p < 0.001), with effects comparable to methylphenidate (11.5%) and slightly greater than ketamine (9.8%). Psychostimulant-induced increase in synaptic dopamine was greater in putamen and ventral striatum than in caudate, whereas alcohol preferentially engaged ventral striatum. Dopamine release did not differ between rewarded and non-rewarded cognitive tasks in the ventral striatum (p > 0.14) or overall striatum (p > 0.10). Methylphenidate-induced increases in synaptic dopamine appeared to attenuate with advancing age, whereas cognitive challenges were associated with greater dopamine release in older individuals. These findings demonstrate that individual pharmacological and cognitive interventions differ markedly in both magnitude and regional pattern of dopamine release. They also suggest that [¹¹C]raclopride PET may have limited sensitivity for distinguishing reward-related from non-reward-related dopamine release. These findings have implications for the design and interpretation of future neuroimaging studies of dopaminergic function in health and disease.

Journal Article↗

PubMed1998

What do pharmacological approaches to obesity management offer? Linking pharmacological mechanisms of obesity management agents to clinical practice.

Obesity is characterised by pathophysiological defects affecting both sides of the energy balance equation. Individuals with a predisposition to obesity have impaired appetite control when diets are fat-rich and energy dense. They also exhibit a lower than expected resting metabolic rate (RMR). A low RMR, in concert with a sedentary lifestyle, contributes to a low total energy output, which may lead to obesity if continued over a period of years. A low metabolic rate seems to be genetically determined, and is partly caused by low sympathetic nervous system activity. Classical treatment programmes for obesity do not provide a satisfactory long-term outcome for the majority of patients. Patients who achieve only a small weight loss during dietary therapy, and have a tendency to weight regain, are characterised by lower energy expenditure, lower sympathetic activity, and a reduced ability to mobilise fat stores, compared with patients who are more successful at losing weight. It is reasonable to improve or normalise these traits by supporting the dietary approach with pharmacological manipulation of central and peripheral pathways. Agents which stimulate adrenergic neurons are particularly suitable because they offer mechanisms for inhibiting hunger and for stimulating energy expenditure, lipolysis and fat oxidation. Sympathomimetic compounds can reduce appetite and increase energy expenditure. Energy expenditure can be increased by 5-10% via stimulation of a combination of beta-adrenoceptors; beta3-adrenoceptors may predominate during chronic therapy. This increased energy expenditure increases the relative proportion of fat oxidation; as this is not fully compensated by increased energy intake, a negative energy balance occurs. This mechanism may be responsible for the long-term weight loss efficiency of agents like ephedrine/caffeine and sibutramine. Pharmacotherapy can be used to support short-term induction of weight loss or long-term weight maintenance. In the latter case, adrenergic agents enable a greater proportion of patients to maintain a satisfactory weight loss, compared with patients treated with conventional programmes alone. Pharmacotherapy which stabilises the size of fat stores at a lower level contributes indirectly to a pronounced improvement of risk factors, leading to a decreased potential for cardiovascular disease, type 2 diabetes and associated morbidity.

Adrenergic beta-Agonists↗

PubMed1991

T-cadinol: a pharmacologically active constituent of scented myrrh: introductory pharmacological characterization and high field 1H- and 13C-NMR data.

Fractionation of an ethyl acetate extract of scented myrrh (resin of Commiphora guidottii Chiov., Burseraceae), using the guinea pig ileum test to monitor pharmacological activity, resulted in isolation of the sesquiterpene (+)-T-cadinol. High field NMR spectroscopy yielded new detailed 1H- and 13C-NMR data for the compound. T-cadinol was shown to have a concentration-dependent smooth muscle relaxing effect on the isolated guinea pig ileum and a dose-dependent inhibitory effect on cholera toxin-induced intestinal hypersecretion in mice.

Animals↗

PubMed1984

Pharmacological studies on ginger. I. Pharmacological actions of pungent constitutents, (6)-gingerol and (6)-shogaol.

General pharmacological studies were performed on (6)-gingerol and (6)-shogaol which are the pungent constituents of ginger (Zingiber officinale Roscoe). Intravenous (i.v.) administration of (6)-gingerol (at 1.75-3.5 mg/kg) or (6)-shogaol (at 1.75-3.5 mg/kg) and oral administration of them (at 70-140 mg/kg) produced an inhibition of spontaneous motor activity, an antipyretic and analgesic effects, prolonged hexobarbital-induced sleeping time, and these effects of (6)-shogaol were mostly more intensive than that of (6)-gingerol. (6)-Shogaol showed an intense antitussive effect in comparison with dihydrocodeine phosphate. In the electro-encephalogram of cortex, the low amplitude fast wave pattern was observed for 5 min after i.v. administration of (6)-shogaol, and then changed to the drowsy pattern, which was restored after 60 min. In the gastro-intestinal system, (6)-shogaol intensively inhibited the traverse of charcoal meal through the intestine in contrast with (6)-gingerol after i.v. administration of 3.5 mg/kg, but (6)-shogaol facilitated such an intestinal function after oral administration of 35 mg/kg. Both (6)-shogaol and (6)-gingerol suppressed gastric contraction in situ, and the suppression by the former was more intensive than that by the latter. In the cardiovascular system, both (6)-shogaol and (6)-gingerol produced depressor response at lower doses on the blood pressure. At high doses, both drugs produced three phase pattern.

Analgesics↗