Dibenzoquinolines derived in plants from (S)-reticuline (BENZYLISOQUINOLINES).
A plant genus of the family ANNONACEAE. Members contain asarone, isoguattouregidine (an isoquinoline alkaloid), norlaureline, puterine, noraporphine alkaloids.
The custard-apple plant family of the order Magnoliales, subclass Magnoliidae, class Magnoliopsida. Some members provide large pulpy fruits and commercial timber. Leaves and wood are often fragrant. Leaves are simple, with smooth margins, and alternately arranged in two rows along the stems.
A group of related plant alkaloids that contain the BERBERINE heterocyclic ring structure.
The rotation of linearly polarized light as it passes through various media.
Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).
A plant genus of the family ANNONACEAE. It has edible fruit and seeds which contain acetogenins and benzoquinazoline and other alkaloids.
A plant genus of the family LAURACEAE. Members contain laurotetanine and other APORPHINES.
A plant genus of the family MONIMIACEAE. Members contain boldine ALKALOIDS. Some PEUMUS species have been reclassified as CRYPTOCARYA.
A plant genus of the family MAGNOLIACEAE. Members include hardwood trees of eastern North America with distinct large tuliplike flowers.
Organic nitrogenous bases. Many alkaloids of medical importance occur in the animal and vegetable kingdoms, and some have been synthesized. (Grant & Hackh's Chemical Dictionary, 5th ed)
Oils which evaporate readily. The volatile oils occur in aromatic plants, to which they give odor and other characteristics. Most volatile oils consist of a mixture of two or more TERPENES or of a mixture of an eleoptene (the more volatile constituent of a volatile oil) with a stearopten (the more solid constituent). The synonym essential oils refers to the essence of a plant, as its perfume or scent, and not to its indispensability.
Agents destructive to the protozoal organisms belonging to the suborder TRYPANOSOMATINA.
A disease endemic among people and animals in Central Africa. It is caused by various species of trypanosomes, particularly T. gambiense and T. rhodesiense. Its second host is the TSETSE FLY. Involvement of the central nervous system produces "African sleeping sickness." Nagana is a rapidly fatal trypanosomiasis of horses and other animals.
Infections with unicellular organisms formerly members of the subkingdom Protozoa.
A genus of flagellate protozoa comprising several species that are pathogenic for humans. Organisms of this genus have an amastigote and a promastigote stage in their life cycles. As a result of enzymatic studies this single genus has been divided into two subgenera: Leishmania leishmania and Leishmania viannia. Species within the Leishmania leishmania subgenus include: L. aethiopica, L. arabica, L. donovani, L. enrietti, L. gerbilli, L. hertigi, L. infantum, L. major, L. mexicana, and L. tropica. The following species are those that compose the Leishmania viannia subgenus: L. braziliensis, L. guyanensis, L. lainsoni, L. naiffi, and L. shawi.
An order of flagellate protozoa. Characteristics include the presence of one or two flagella arising from a depression in the cell body and a single mitochondrion that extends the length of the body.
An enzyme that catalyzes the hydrolysis of ACETYLCHOLINE to CHOLINE and acetate. In the CNS, this enzyme plays a role in the function of peripheral neuromuscular junctions. EC 3.1.1.7.
A group of ISOQUINOLINES in which the nitrogen containing ring is protonated. They derive from the non-enzymatic Pictet-Spengler condensation of CATECHOLAMINES with ALDEHYDES.
A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.
Agents that cause vomiting. They may act directly on the gastrointestinal tract, bringing about emesis through local irritant effects, or indirectly, through their effects on the chemoreceptor trigger zone in the postremal area near the medulla.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
The principal alkaloid in opium and the prototype opiate analgesic and narcotic. Morphine has widespread effects in the central nervous system and on smooth muscle.
Databases devoted to knowledge about PHARMACEUTICAL PRODUCTS.
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
The metabolism of drugs and their mechanisms of action.
Poisoning by the ingestion of plants or its leaves, berries, roots or stalks. The manifestations in both humans and animals vary in severity from mild to life threatening. In animals, especially domestic animals, it is usually the result of ingesting moldy or fermented forage.
The variety of all native living organisms and their various forms and interrelationships.
The systematic arrangement of entities in any field into categories classes based on common characteristics such as properties, morphology, subject matter, etc.
A province of Canada lying between the provinces of Manitoba and Quebec. Its capital is Toronto. It takes its name from Lake Ontario which is said to represent the Iroquois oniatariio, beautiful lake. (From Webster's New Geographical Dictionary, 1988, p892 & Room, Brewer's Dictionary of Names, 1992, p391)
A province of eastern Canada. Its capital is Quebec. The region belonged to France from 1627 to 1763 when it was lost to the British. The name is from the Algonquian quilibek meaning the place where waters narrow, referring to the gradually narrowing channel of the St. Lawrence or to the narrows of the river at Cape Diamond. (From Webster's New Geographical Dictionary, 1988, p993 & Room, Brewer's Dictionary of Names, 1992, p440)
PLANTS, or their progeny, whose GENOME has been altered by GENETIC ENGINEERING.
A feeling of restlessness associated with increased motor activity. This may occur as a manifestation of nervous system drug toxicity or other conditions.
A publication issued at stated, more or less regular, intervals.
Individual's rights to obtain and use information collected or generated by others.
Those support services other than room, board, and medical and nursing services that are provided to hospital patients in the course of care. They include such services as laboratory, radiology, pharmacy, and physical therapy services.
The use of statistical methods in the analysis of a body of literature to reveal the historical development of subject fields and patterns of authorship, publication, and use. Formerly called statistical bibliography. (from The ALA Glossary of Library and Information Science, 1983)
"The business or profession of the commercial production and issuance of literature" (Webster's 3d). It includes the publisher, publication processes, editing and editors. Production may be by conventional printing methods or by electronic publishing.
The evaluation by experts of the quality and pertinence of research or research proposals of other experts in the same field. Peer review is used by editors in deciding which submissions warrant publication, by granting agencies to determine which proposals should be funded, and by academic institutions in tenure decisions.
A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.
A plant genus of the family FUMARIACEAE (classified by some in PAPAVERACEAE) that contains isoquinoline alkaloids.
A genus of leguminous shrubs or trees, mainly tropical, yielding useful compounds such as ALKALOIDS and PLANT LECTINS.
Substances that are destructive to protozoans.
A group of compounds consisting in part of two rings sharing one atom (usually a carbon) in common.
A parasitic hemoflagellate of the subgenus Leishmania leishmania that infects man and animals including rodents. The Leishmania mexicana complex causes both cutaneous (LEISHMANIASIS, CUTANEOUS) and diffuse cutaneous leishmaniasis (LEISHMANIASIS, DIFFUSE CUTANEOUS) and includes the subspecies amazonensis, garnhami, mexicana, pifanoi, and venezuelensis. L. m. mexicana causes chiclero ulcer, a form of cutaneous leishmaniasis (LEISHMANIASIS, CUTANEOUS) in the New World. The sandfly, Lutzomyia, appears to be the vector.

Bronchodilator and anti-inflammatory activities of glaucine: In vitro studies in human airway smooth muscle and polymorphonuclear leukocytes. (1/80)

1. Selective phosphodiesterase 4 (PDE4) inhibitors are of potential interest in the treatment of asthma. We examined the effects of the alkaloid S-(+)-glaucine, a PDE4 inhibitor, on human isolated bronchus and granulocyte function. 2. Glaucine selectively inhibited PDE4 from human bronchus and polymorphonuclear leukocytes (PMN) in a non-competitive manner (Ki=3.4 microM). Glaucine displaced [3H]-rolipram from its high-affinity binding sites in rat brain cortex membranes (IC50 approximately 100 microM). 3. Glaucine inhibited the spontaneous and histamine-induced tone in human isolated bronchus (pD2 approximately 4.5). Glaucine (10 microM) did not potentiate the isoprenaline-induced relaxation but augmented cyclic AMP accumulation by isoprenaline. The glaucine-induced relaxation was resistant to H-89, a protein kinase A inhibitor. Glaucine depressed the contractile responses to Ca2+ (pD'2 approximately 3.62) and reduced the sustained rise of [Ca2+]i produced by histamine in cultured human airway smooth muscle cells (-log IC50 approximately 4.3). 4. Glaucine augmented cyclic AMP levels in human polymorphonuclear leukocytes challenged with N-formyl-Met-Leu-Phe (FMLP) or isoprenaline, and inhibited FMLP-induced superoxide generation, elastase release, leukotriene B4 production, [Ca2+]i signal and platelet aggregation as well as opsonized zymosan-, phorbol myristate acetate-, and A23187-induced superoxide release. The inhibitory effect of glaucine on superoxide generation by FMLP was reduced by H-89. 5. In conclusion, Ca2+ channel antagonism by glaucine appears mainly responsible for the relaxant effect of glaucine in human isolated bronchus while PDE4 inhibition contributes to the inhibitory effects of glaucine in human granulocytes. The very low PDE4/binding site ratio found for glaucine makes this compound attractive for further structure-activity studies.  (+info)

Mechanical effects of liriodenine on the left ventricular-arterial coupling in Wistar rats: pressure-stroke volume analysis. (2/80)

1. In a recent in vivo study, liriodenine, an aporphine alkaloid, has been identified as a prominent anti-arrhythmic agent that can prevent rats' sudden deaths, even at the dose as low as 10(-7) g kg(-1). The aim of this study was to determine whether liriodenine at its effective anti-arrhythmic dose of 10(-7) g kg(-1) had effects on the left ventricular (LV)-arterial coupling in Wistar rats. 2. LV pressure and ascending aortic flow signals were recorded to construct the ventricular and arterial end-systolic pressure-stroke volume relationships to calculate LV end-systolic elastance (E(es)) and effective arterial volume elastance (E(a)), respectively. The optimal afterload (Q(load)) determined by the ratio of E(a) to E(es) was used to measure the optimality of energy transmission from the left ventricle to the arterial system. 3. Liriodenine at the dose of 10(-7) g kg(-1) showed no significant changes in basal heart rate (HR), cardiac output (CO), LV end-systolic pressure (P(es)), E(a), E(es), and Q(load). 4. By contrast, liriodenine at the dose of 10(-6) g kg(-1) produced a significant fall of 2.0% in HR and a significant rise of 5.8% in CO, but no significant change in P(es). Moreover, liriodenine administration of 10(-6) g kg(-1) to rats significantly decreased E(es) by 8.5% and E(a) by 10.6%, but did not change Q(load). 5. We conclude that liriodenine at the dose of 10(-7) g kg(-1) has no effects on the mechanical properties of the heart and the vasculature and the matching condition for the left ventricle coupled to its vasculature in rats. Even at 10 times the effective anti-arrhythmic dose, liriodenine shows no effects on the efficiency of energy transferred from the left ventricle to the arterial system.  (+info)

Dicentrine is preferentially antagonistic to rat aortic than splenic alpha 1-adrenoceptor stimulation. (3/80)

AIM: Dicentrine is a known alpha 1-adrenoceptor antagonist, but its alpha 1-adrenoceptor subtype selectivity has not yet been determined. We therefore, investigated the putative alpha 1-adrenoceptor subtype selectivity of this agent. METHODS: Graded isometric contractile responses of rat aortic rings and spleen to phenylephrine were observed in the absence or presence of various concentrations of dicentrine. The pA2 values for dicentrine were determined. RESULTS: Aortic tissues were more sensitive to phenylephrine-induced contraction than the spleen tissues. Dicentrine was approximately 100 times more potent as an antagonist to the aortic contraction, than it was to the splenic contractions. CONCLUSION: Dicentrine is an alpha 1-adrenoceptor antagonist which is more selective towards the putative alpha 1D-adrenoceptor subtype of the rat aorta than the alpha 1B-adrenoceptor of the spleen.  (+info)

Multiple actions of glaucine on cyclic nucleotide phosphodiesterases, alpha 1-adrenoceptor and benzothiazepine binding site at the calcium channel. (4/80)

1. In the present study, the properties of glaucine (an aporphine structurally related to papaverine) were compared with those of papaverine, diltiazem, nifedipine and prazosin. The work includes functional studies on rat isolated aorta contracted with noradrenaline, caffeine or KCl, and a determination of the affinity of glaucine at calcium channel binding sites of alpha-adrenoceptors, by use of [3H]-(+)-cis-diltiazem, [3H]-nitrendipine and [3H]-prazosin binding to cerebral cortical membranes. The effects of glaucine on the different molecular forms of cyclic nucleotide phosphodiesterases (PDE) isolated from bovine aorta were also determined. 2. Contraction evoked by noradrenaline (1 microM) or depolarizing solution (60 mM KCl) were inhibited in a concentration-dependent manner by all the compounds tested. As expected, prazosin showed a greater selectivity of action on NA-induced contraction, whereas nifedipine and diltiazem appeared more potent on KCl-induced contraction. Glaucine had a greater potency on the contraction elicited by noradrenaline whereas papaverine acted non specifically. 3. In Ca(2+)-free solution, prazosin (0.1 microM) and glaucine (0.1 mM) inhibited the contraction evoked by NA; diltiazem (0.1 mM) diminished this contraction whereas nifedipine (1 microM) had no effect. Preincubation of tissues with glaucine, diltiazem, nifedipine and prazosin did not modify the contractile response induced by caffeine. In contrast, papaverine (0.1 mM) significantly inhibited the contractions evoked by NA or caffeine in Ca(2+)-free medium. 4. Glaucine and papaverine show affinity at the [3H]-prazosin binding site and at the benzothiazepine binding site of the Ca(2+)-channel receptor complex, but have no effect at the dihydropyridine binding site in rat cerebral cortex. Glaucine exerts some selectivity as an inhibitor of [3H]-prazosin binding as opposed to [3H]-(+ )-cis-diltiazem binding while papaverine appears to have approximately equal affinity in this respect.5. This study confirms the presence of four phosphodiesterase (PDE) activities in bovine aorta: a calmodulin-activated PDE (CaM-PDE type I) which hydrolyzed preferentially guanosine 3':5'-cyclic monophosphate (cyclic GMP); a cyclic GMP selective form (cGMP-PDE type V); and two low Km adenosine 3':5'-cyclic monophosphate (cyclic AMP) PDEs that are insensitive to the stimulatory effect of CaM, one of which was inhibited by cyclic GMP (CGI-PDE, type III) and the other by rolipram (cAMP-PDE, type IV). Glaucine selectively inhibits one of the two forms of Ca2+-independent low Km cAMP-PDE, the type IV. In contrast, papaverine exerts a non-selective inhibitory effect upon all PDE forms.6. The present work provides evidence that glaucine, a benzyltetrahydroisoquinoline alkaloid, has interesting properties as an alpha l-adrenoceptor antagonist, calcium entry blocker (through the benzothiazepine recognition site in the calcium channel) and as a selective inhibitor of the rolipram-sensitive cAMP-PDE, type IV PDE.  (+info)

Haemodynamic effects of dicentrine, a novel alpha 1-adrenoceptor antagonist: comparison with prazosin in spontaneously hypertensive and normotensive Wistar-Kyoto rats. (5/80)

1. The haemodynamic effects of dicentrine, an aporphine derivative isolated from the plant Lindera megaphylla, were investigated and compared with prazosin in rats. 2. In anaesthetized normotensive Wistar-Kyoto (WKY) rats, i.v. administration of dicentrine (0.1, 0.5, 1.0 mg kg-1) and prazosin (0.01, 0.05, 0.1 mg kg-1) induced a dose-related reduction of mean arterial pressure (MAP) which reached a maximal effect 5-10 min after injection and persisted for 2 h. 3. In anaesthetized WKY rats, a higher dose of dicentrine (1.0 mg kg-1, i.v.) did not cause any significant changes in heart rate (HR), cardiac output (CO) and stroke volume (SV) but markedly increased tail blood flow. In contrast, a higher dose of prazosin (0.1 mg kg-1, i.v.) produced a decrease in HR which paralleled the time course of the hypotensive response. 4. The hypotensive activity of dicentrine was completely abolished by alpha-adrenoceptor blockade. Both dicentrine and prazosin significantly attenuated pressor responses to noradrenaline but failed, even at maximal hypotensive doses, to impair the pressor effects of angiotensin II or vasopressin. These observations suggest that dicentrine appears to exert its hypotensive action through alpha 1-adrenoceptor blockade. 5. In conscious normotensive and spontaneously hypertensive (SH) rats, dicentrine (0.5-2.0 mg kg-1, i.v.) and prazosin (0.05-0.2 mg kg-1, i.v.) also evoked dose-related decreases in MAP which were of greater magnitude in SH rats. Oral administration of dicentrine (5 and 8 mg kg-1) to conscious SH rats caused a hypotensive effect which persisted for over 15 h.6. These results suggest that dicentrine may have therapeutic potential as an oral antihypertensive drug via alpha-adrenoceptor blockade.  (+info)

Reactive oxygen species (ROS) generation inhibited by aporphine and phenanthrene alkaloids semi-synthesized from natural boldine. (6/80)

Four phenanthrene and one aporphine alkaloids semi-synthesized from boldine were evaluated for their inhibitory effect on reactive oxygen species (ROS) generation. ROS generation by neutrophils stimulated with N-formyl-methionyl-leucyl-phenylalanine was inhibited in a concentration dependent manner. Alkaloids exerted similar inhibitory effect in the hypoxanthine-xanthine oxidase system than in stimulated neutrophils, which could be attributed to a direct ROS scavenging activity. None of the alkaloids assayed had any effect on xanthine oxidase activity. Therefore the synthesized alkaloids might constitute an alternative therapy in inflammation disorders in which ROS generation is involved.  (+info)

Effect of boldine, secoboldine, and boldine methine on angiotensin II-induced neutrophil recruitment in vivo. (7/80)

Angiotensin-II (Ang-II) has inflammatory activity and is involved in different diseases associated with the cardiovascular system. This study has evaluated the effect of boldine (B), and two phenanthrene alkaloids semisynthesized by us, secoboldine (SB) and boldine methine (BM), on Ang-II-induced neutrophil recruitment. Intraperitoneal administration of 1 nM Ang-II induced significant neutrophil accumulation, which was maximal at 4-8 h. BM inhibited neutrophil infiltration into the peritoneal cavity at 4 h and 8 h by 73% and 77%, respectively, SB at 8 h by 55%, and B had no effect on this response. Although BM inhibited the release of cytokine-inducible neutrophil chemoattractant/keratinocyte-derived chemokine, macrophage inflammatory protein-2 (MIP-2), and platelet-activating factor (PAF) elicited by Ang-II, SB only reduced the release of MIP-2 after 4 h of its administration. Sixty-minute superfusion of the rat mesentery with 1 nM Ang-II induced a significant increase in the leukocyte-endothelial cell interactions and P-selectin up-regulation, which were inhibited by 1 microM BM and SB. The generation of reactive oxygen species (ROS) in endothelial cells stimulated with Ang-II was inhibited significantly by the three alkaloids tested. BM also diminished Ang-II-induced interleukin-8 release from endothelial cells and blocked the PAF receptor on human neutrophils (concentration of the compound needed to produce 50% inhibition value: 28.2 microM). Therefore, BM is a potent inhibitor of Ang-II-induced neutrophil accumulation in vivo. This effect appears to be mediated through inhibition of CXC chemokine and PAF release, ROS scavenging activity, and blockade of the PAF receptor. Thus, it may have potential therapeutic interest for the control of neutrophil recruitment that occurs in inflammation associated with elevated levels of Ang-II.  (+info)

Characterization and inhibitor discovery of one novel malonyl-CoA: acyl carrier protein transacylase (MCAT) from Helicobacter pylori. (8/80)

Type II fatty acid synthesis (FAS II) is an essential process for bacteria survival, and malonyl-CoA:acyl carrier protein transacylase (MCAT) is a key enzyme in FAS II pathway, which is responsible for transferring the malonyl group from malonyl-CoA to the holo-ACP by forming malonyl-ACP. In this work, we described the cloning, characterization and enzymatic inhibition of a new MCAT from Helicobacter pylori strain SS1 (HpMCAT), and the gene sequence of HpfabD was deposited in the GenBank database (Accession No. AY738332 ). Enzymatic characterization of HpMCAT showed that the K(m) value for malonyl-CoA was 21.01+/-2.3 microM, and the thermal- and guanidinium hydrochloride-induced unfolding processes for HpMCAT were quantitatively investigated by circular dichroism spectral analyses. Moreover, a natural product, corytuberine, was discovered to demonstrate inhibitory activity against HpMCAT with IC(50) value at 33.1+/-3.29 microM. Further enzymatic assay results indicated that corytuberine inhibits HpMCAT in an uncompetitive manner. To our knowledge, this is the firstly reported MCAT inhibitor to date. This current work is hoped to supply useful information for better understanding the MCAT features of H. pylori strain, and corytuberine might be used as a potential lead compound in the discovery of the antibacterial agents using HpMCAT as target.  (+info)

Aporphines are a group of tetracyclic alkaloids that belong to the ubiquitous tetrahydroisoquinoline family. The aporphine template is known to be associated with a range of biological activities. Aporphines have been explored as antioxidants, anti-tuberculosis, antimicrobial and anticancer agents. Within the Central Nervous Systems (CNS), aporphine alkaloids are known to possess high affinity for several clinically valuable targets including dopamine receptors (predominantly D1 and D2), serotonin receptors (5-HT1A and 5-HT7) and α adrenergic receptors. Aporphines are also inhibitors of the acetylcholinesterase enzyme - a clinical target for the treatment of Alzheimers disease. Considering the diverse profile of aporphine alkaloids at CNS receptors they can be considered as
Pretreatment with thaliporphine before ischemia affords cardioprotective effects against reperfusion injury via antioxidant activity. This study evaluated whether thaliporphine administered at a certain period after myocardial ischemia conferred the same cardioprotection and assessed its possible new mechanism. The left main coronary artery of anaesthetized rats was occluded for 1 h and then reperfused for 2 h. Thaliporphine was administered at 10 min before reperfusion. Controls received saline only. Morphine, a nonselective opioid receptor agonist, was used as reference compound at 0.3 mg/kg. Thaliporphine at 0.05 and 0.5 mg/kg were found to reduce the infarct size. Recovery of cardiac function was higher in thaliporphine (0.5 mg/kg) group, as assessed by a significant improvement in the rates of pressure development (+dp/dt (max)). This compound also reduced plasma creatine kinase and cardiac MPO activity. These protective effects afforded by thaliporphine were diminished by the opioid receptor
What is Boldine? Where does Boldine Come From? Boldine Benefits, Bodybuilding, Side Effects, Safety, Dosage, Negatives, Supplements, When to Take Boldine..
Introduction: Boldine is an aporphine alkaloid that is found in high amount in boldo tree and Lindera aggregate. It is used as homeopathic and herbal medicine that has various antioxidant and anti-cancer. Our previous study has reported anti-telomerase effect of this alkaloid. In order to enhance this valuable inhibitory effect, ...
way the herb is usually simmered in water for 10-20 minutes before drinking. Some people like to infuse it into wine and then drink the wine. When prepared this way the herb is mixed with wine and allowed to infuse for anywhere from a few hours to a few weeks. The flowers contain the alkaloids aporphine and nuciferine as well as other related compounds. Some people like to smoke a mixture of blue lotus and cannabis (typically a 50:50 blend). ED POPPY FLOWER PETALS produce a mild sedative effect that is useful for treating anxiety and insomnia.. Some people like to infuse it into wine and then drink the wine. When prepared this way the herb is mixed with wine and allowed to infuse for anywhere from a few hours to a few weeks. The flowers contain the alkaloids aporphine and nuciferine as well as other related compounds. Some people like to smoke a mixture of blue lotus and cannabis (typically a 50:50 blend). ED POPPY FLOWER PETALS produce a mild sedative effect that is useful for treating anxiety ...
Title: Derivatives as 5HT1A Receptor Ligands-Past and Present. VOLUME: 12 ISSUE: 15. Author(s):G. Caliendo, V. Santagada, E. Perissutti and F. Fiorino. Affiliation:Dipartimento di Chimica Farmaceutica e Tossicologica, Via D. Montesano, 49, 80131 Naples, Italy.. Keywords:serotonin, neurotransmitter, g protein-coupled receptors, median raphe nucleus (mrn), ohdpat, enantioselectivity, indolylalkylamines, ergolines, aporphines, qsar. Abstract: Serotonin is a neuromediator, well-know for its implication in mood regulation, anxiety, depression and, insomnia as well as in normal human function such as sleep, sexual activity and appetite. In this way, serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists and pharmaceutical companies. Among 5-HTRs, the 5-HT1A subtype is the best studied, and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind 5-HT1A ...
Product Name: NUCIFERINE Synonyms: (-)-nucipherine;(r)-1,2-dimethoxyaporphine;1,2-dimethoxy-6a-beta-aporphin;5,6,6a,7-tetrahydro-1,2-dimethoxy-6-methyl-g)quinolin(r)-4h-dibenzo(d;l-5,6-dimethoxyaporphine;l-nuciferine;nuciferin;NUCIFERINE CAS:...
Representative images and quantitative analysis of CAOV-3 cells treated or not treated with liriodenine at 24 hours.Notes: The cells were stained with Hoechst,
Liriodenine (L), an active component of the anticancer traditional Chinese medicine (TCM), was isolated from Zanthoxylum nitidum. Its reactions with Pt(II) and Ru(II) afforded three metal complexes: cis-[PtCl2(L)] (1), cis-[PtCl2(L)(DMSO)] (2), and cis-[RuCl2(L)(DMSO)(2)]center dot 1.5H(2)O (3), the crystal structures of L, 2 and 3 were determined by single-crystal X-ray diffraction methods. These complexes were fully characterized by elemental analysis, IR spectrophotometry, H-1 and C-13 NMR spectroscopies, and ES mass spectrometry. The in vitro cytotoxicity of L and complexes 1-3 against 11 human tumour cell lines was assayed. The metal-based compounds exhibit enhanced cytotoxicity vs. free L, suggesting that these compounds display synergy in the combination of metal ions and liriodenine. The binding properties of L and its complexes 1-3 to ct-DNA were investigated through UV-vis, fluorescence, CD spectra, viscosity and agarose gels electrophoretic measurements.. ...
Lotus leaf flavone nuciferine powder HACCP Kosher FDA factory 20% lotus leaf extract,US $ 1 - 300 / Kilogram, lotus leaf extract, Powder, Leaf.Source from Changsha World-Way Biotech Inc. on Alibaba.com.
Leishmaniasis and trypanosomiasis are protozoan diseases caused respectively by the kinetoplastid protozoan Leishmania parasites transmitted by the female phlebotomine sa..
Sigma-Aldrich offers abstracts and full-text articles by [Shuiying Zhang, Qian Zhang, Qiang Guo, Yunfang Zhao, Xiaoli Gao, Xingyun Chai, Pengfei Tu].
Sixteen compounds were extracted and purified from the leaves of Liriodendron tulipifera. These compounds include aporphines, oxoaporphine, coumarin, sesquiterpene lactone, benzenoids, cyclitol and steroids. (+)-Norstephalagine (2) (an aporphine) and scopoletin (8) (a coumarin) were isolated from Liriodendron tulipifera leaves from the first time. The identified compounds were screened for their antiradical scavenging, metal chelating and ferric reducing power activities. The results have showed that these compounds have antioxidative activity. The study has also examined the chemopreventive property of the isolated compounds against human melanoma cells A375. The results shown that (−)-anonaine (1), (−)-liridinine (3), (+)-lirinidine (6), lysicamine (7) and epitulipinolide diepoxide (9) significantly inhibited the proliferation of melanoma cells. These results revealed that these compounds have antioxidative activity and chemopreventive activity in skin melanoma cells.
bulbocapnine: was heading 1975-94 (Prov 1975-90); use APORPHINES to search BULBOCAPNINE 1975-94 (as Prov 1975-94); alkaloid from Corydalis cava and other plants; induces catalepsy probably due to its antagonism of DOPAMINE
Nandina domestica is an evergreen Shrub growing to 2.5 m (8ft) by 2 m (6ft) at a medium rate. It is hardy to zone (UK) 7 and is not frost tender. It is in leaf 12-Jan It is in flower from Jun to July. The flowers are hermaphrodite (have both male and female organs)Suitable for: light (sandy), medium (loamy) and heavy (clay) soils and prefers well-drained soil. Suitable pH: acid, neutral and basic (alkaline) soils. It cannot grow in the shade. It prefers moist soil.
Two of the four parameters in the rule of five, molecular weight and log P, which can be detected and predicted by mass spectrometry and compound retention on reversed-phase HPLC, were used as guidelines in natural product isolation. A new aporphine alkaloid, (6aR)-normecambroline (1), was isolated from the bark of Neolitsea dealbata (R. Br.) Merr. Its structure was determined on the basis of NMR, MS and CD analysis. It is the first time the absolute configuration of the roemerine-N-oxide was assigned for both roemerine-N α-oxide (3) and roemerine-Nβ-oxide (4). Physico-chemical property evaluation demonstrated all alkaloids had no Lipinski violation. Compound 1 inhibited selectively against cervical cancer cells (HeLa) with an IC50 of 4.0 μM. © 2010 Elsevier Ltd. All rights reserved.
Reports of recreational use of glaucine have recently been published, and effects include dissociative-type symptoms; feeling detached and in another world, as well as nausea, vomiting and dilated pupils. These reports mirror those about the effects of clinical use, which state dissociative-type symptoms as well as lethargy, fatigue, hallucinations.[8][9] Investigation of side effects in a clinical setting also reports that the hallucinatory effects manifest as bright and colorful visualizations. They also report that patients perceive their environments clearly yet feel detached from it; the patient sees and understands everything and is oriented well enough, but cannot take a clear and adequate action.[8]. One particular report of recreational use gone awry described the form of distribution as tablets being marketed as a 1-benzylpiperazine (BZP)-free herbal high which the patient referred to as head candy.[9]. ...
Swedish teen climate activist Greta Thunberg hitched a renewable-energy ride back to Europe on Wednesday, sailing into the Atlantic on a trip she hopes will get her to Madrid in time for another climate conference, and then home for the holidays. Thunberg tweeted as she took to the sea on the 48-foot
Supplementary MaterialsSupplementary Movie 1 41598_2020_65742_MOESM1_ESM. 120?rpm and a pullback velocity of 50 m/s and 500 m/sec to achieve an interval between frames was 25 m and 250 m. Each Nuciferine blood vessel was also imaged using a conventional OCT system at the same position with the same frame interval (51.2k A-line rate with a rotation speed of 3000?rpm and pullback velocity of 1 1.25?mm/s and 12.5?mm/s) to allow direct comparison against the OCT. Intravascular OCT system, used in this study, was built based on a prototype device from a commercial OCT manufacturer (NinePoint Medical, Cambridge, MA, USA). The axial and lateral resolution, defined as FWHM of peak intensity at the focal plane, of the OCT system was 11.58 m and 22.67 m, respectively. Following imaging, the animal blood vessels were resected, fixed, and processed for histopathological analysis. All animal studies were approved by the Institutional Animal Care and Use Committee of Korea University College of Medicine ...
Lotus plumule is another type of Lotus flower that is far less famous than the Blue Lily and Blue Lotus flowers, but it has potent characteristics unique to itself. The main consituents, as expected, are nuciferine, but veterans and fans of Blue Lotus will notice a different energy about this tincture, especially because it is a Full Spectrum extract containing the entire energy signature of the plant, but in a stronger form that a straight hydrosol ...
Resumo: Introdução: Situações de doença aguda podem tornar-se crônicas, a exemplo das feridas, especialmente as úlceras venosas. Estas são definidas por lesões em membros inferiores relacionadas à insuficiência venosa e acometem os aspectos familiares, sociais e laborais. A Bota de Unna é uma tecnologia utilizada para o tratamento das úlceras venosas que constituem importante problema de saúde pública pela elevada incidência, prevalência, impacto socioeconômico, cronicidade e frequência das recidivas. Objetivos: Analisar a efetividade da tecnologia Bota de Unna no tratamento da úlcera venosa; caracterizar o perfil sócio demográfico e clínico dos pacientes com feridas crônicas; e mensurar a recidiva das úlceras venosas após tratamento com a tecnologia Bota de Unna. Método:Pesquisa retrospectiva documental realizada no Ambulatório de Tratamento de Feridas de um hospital de ensino de Curitiba-Paraná, no período de dois anos (2013-14), coleta de dados abrangeu o ...
Thousands of miles away from his impeachment trial in Washington, President Trump was in Davos where he pledged to plant join an initiative to plant trillion trees. Teen climate activist Greta Thunberg delivered her retort. Joe Davies reports.
Wake County Public Schools says they have received no complaints over a mural of child climate activist Greta Thunberg and a quote by rapper Lil Nas X painted on the wall of a boys bathroom in Apex Friendship High School.
Climate activist Greta Thunberg arrived in Madrid Friday to join thousands of other young people in a march to demand world leaders take real action against...
Fluorescent micrographs and quantitative analysis of CAOV-3 cells double-stained with acridine orange and propidium iodide. Cells were treated with liriodenine
A fine green leaf of the Nandina Plant makes an attractive choice for this hanging foliage. The plant sprays out the side to approximately 40cm in width but does not hang below the bottom of the pot. It is a delicate and mid-green house plant which will enhance any room. The brass planter measures 42cm in length from the top of the hanger to the base of the pot. It is held by 3 gold coloured chains with a metal ring at the top (please note: wall bracket or hook for hanging is not included). The width of the pot is 15cm. ...
Broncholytin information about active ingredients, pharmaceutical forms and doses by Sopharma, Broncholytin indications, usages and related health products lists
Among the activists and thinkers who are concerned about the increasing heat and instability of the climate there has been a long-running debate about what exactly motivates people to take action. Some say that a realistic form of hope backed with practical action works best, and that fear and despair are very disempowering, while others say that a good scare never did anyone any harm, and will get people off their butts. Sixteen year old Greta Thunberg told the worlds wealthy elite assembled at Davos in January 2019: Adults keep saying: we owe it to the young people to give them hope. But I dont want your hope. I dont want you to be hopehttp://Greta Thunberg told the worlds wealthy elite assembled at Davos in January 2019ful; I want you to panic. I want you to feel the fear I feel every day. And then I want you to act. I want you to act as you would in a crisis.. Thunberg suffered a deep depression before she decided that taking action was the way out of despair, and she is now doing a ...
Tratamento endovascular da doença venosa oclusiva central: experiência de um centro . Fernando Barbosa Trevisan ; Wander Eduardo Sardinha ; Domingos Moraes Filho ; Eduardo Durante Ramires ; Silfayner Victo. Biblioteca virtual para leer y descargar libros, documentos, trabajos y tesis universitarias en PDF. Material universiario, documentación y tareas realizadas por universitarios en nuestra biblioteca. Para descargar gratis y para leer online.
The following are my personal views arising from The following are my personal views arising from Gretas words.On climate changeLike Greta, I am
Thalfoetines A-D (1-4), unique hybrid aporphine alkaloids with a C-7 aromatic unit formed by a new C-C bond linking two building blocks, were isolated from Thalictrum foetidum. Their structures were elucidated by extensive spectroscopic and computational analysis. They inhibited bacteria significantly, and compound 1 damaged the cell structure of Staphylococcus aureus and inhibited its DNA synthesis ...
This year has been so hard. It has been by far the most difficult despite everything we had already been through. Mae has been witness to too many traumatizing and devastating things. She has sat quietly as doctors have discussed infections, strokes, seizures, cancer, and terrible odds. She has seen her baby sister scream in pain. She has walked beside us the many times Phoebe has been transferred to the ICU. She has seen Jon and I completely broken. She has asked if Phoebe will ever come home. She has watched as Phoebe is sedated. She has wondered out loud if the Phoebe that she loves so much would come back to her after a stroke and fungal infection in the brain caused her to be unrecognizable. She has sat by and held her little sisters hand through days that would cause the strongest people to completely break down. Despite a fungal infection that has left marks and scars on Phoebes skin that are most likely permanent - Mae sees nothing but pure beautiful and brave Phoebe. Unlike some ...
Scene: Central Perk. All except Chandler, plus Emma.]. Phoebe: Oh hey you guys, I couldn t get a reservation for the night of my birthday, so we have to do dinner Thursday night instead.. Joey: Thursday? But that s Halloween.. Phoebe: So?. Joey: [It s just] So spooky, that s all.. Ross: So, so, is Mike coming to dinner?. Phoebe: No! It s my first birthday with a boyfriend, and he has to work. Uch, I get mad at him, but I think it s a little to soon to show my true colors.. Rachel: Pheebs, I would make a reservation for five, because one of us has to stay home and watch Emma. (to Ross:) Which one of us should go to dinner?. Phoebe: Oh, Rachel!. Ross: Actually, um, I was thinking maybe both of us could go.. Phoebe: Oh, yay!. Ross: Thanks, I put a lot of extra thoughts on your gift.. Phoebe: Alright, okay, so we can all go now. That is fun. Hey, you know what? We all haven t been together the six of us in such a long time.. Monica: What are you talking about? We re all together right now.. Rachel: ...
Papaver fugax Poiret population Khalkhal was shown to contain four major alkaloids, roemerine (0.19%), mecamberine (0.39%), liriodenine (0.20%) and salutaridine (0.10%). Papaver caucasicum M. B. population Elika was shown to contain four major alkaloids, nuciferine (0.50%), amurensinine (0.15%), lysicamine (0.30%) and nornuciferine (0.40%). Lysicarnine and nornuciferine were detected for the first time in Papaveraceae
Phoebes latest bone marrow chimerism shows that just 9% of her cells are donor cells and the remaining 91% are leukemia. This is slightly higher than on the last test. The leukemia is now predominantly AML, with some ALL still present. Phoebes blood and spinal fluid remain clear of leukemia and although the bone marrow results are terrible and devastating, Phoebe is not a sick little girl. She is eating, playing, laughing, singing and telling us exactly how she feels. She is often the last person to go to sleep and the first to wake up in the morning and she brings the joy and spunk to our days. She has earned the title of tiny boss lady because as joyful as she is, she is also very bossy and determined. At least once a day, I hear Mae tell Phoebe - you are not the boss of me. Phoebe has so little control over her days that she tries her best to control what she can, including Mae ... and Jon and I too. ...
The main event will be the lecture given by world-renown humanitarian child prodigy, Greta Thunberg - a recognized expert on multiple subjects including virology, ecology, public policy, epidemiology, climate science, and public health.. Thunbergs philosophical treatise on the balance between constitutional rights and public police measures within the context of global pandemics, Do it My Way, or Else, earned her an honorary doctorate awarded by the University of Cambridge.*. Dr. Thunberg was awarded Times Person of the Year award while also being nominated for a Nobel Peace Prize in 2019, (and one of Forbes 100 Most Powerful Women).. CNN announced Wednesday it will feature Dr. Greta Thunberg in its next Coronavirus: Facts and Fears town hall program set for Thursday night on the cable channel.. The town hall will be hosted by AC 360 anchor Anderson Cooper and CNN chief medical correspondent Dr. Sanjay Gupta.. The town hall on Thursday night comes one week after the network welcomed ...
Nandina (Nandina domestica), also known as heavenly bamboo, originates from Japan and belongs to the Berberis family. The evergreen, tender shrub produces un-branched limbs and deeply divided leaves ...
Recently, there has been interest in the antiarrhythmic potential of the novel antianginal agent, ranolazine, the first Food and Drug Administration-approved drug that specifically blocks the late component of the Na+ current. Like most antiarrhythmics that target cardiac ion channels (eg, flecainide and amiodarone), ranolazine blocks multiple channels, including the repolarizing hERG current IKr, with therapeutic concentrations. The result is a mild concentration-dependent QTc prolongation seen in patients with chronic stable angina.11 Because of this, ranolazine is contraindicated for patients using other QT-prolonging drugs, those with preexisting QT prolongation,12 and those with repolarization abnormalities.. In this study, we sought to use a computationally based approach to determine whether ranolazines unintended pathological block of promiscuous K+ channels would prevail over therapeutic drug effects in 2 specific patient populations: LQT3-ΔKPQ carriers and those with acquired ...
Lindera is cultivated for its attractive, aromatic foliage, star-shaped, mid-April flowers and showy red to black fruit. Growth habit is rounded with
Theres a lot to talk about when it comes to youth climate activist Greta Thunberg like her notable speeches calling out politicians or her appointment as Times person of the year. Instead, radio host and former Trump aide Sebastian Gorka decided…
Teenage climate activist Greta Thunberg accused political and business leaders of polishing their images rather than taking aggressive action in the fight against climate change at a United Nations summit on Wednesday. Lauren Anthony reports.
Los Angeles singer/songwriter Phoebe Bridgers stopped by the Paste studio on July 31 to perform a few tracks ahead of the release of her debut album, Stranger in the Alps . Bridges started off with Georgia from her 2015 EP Killer , then performed her two latest singles, Smoke Signals and Motion Sickness. Stranger in the Alps arrives September 22.
THE X Factor is now a distant memory but Phoebe Brown, who battled through to the final stages of the contest with girl band Hope, has built on the groups success.
stranger in the alps by phoebe bridgers buy online at resident, ten soul-shattering songs of brutally honest lyrical unburdening worthy of keaton
Get this from a library! Selection, preparation, and pharmacological evaluation of plant material. [Elizabeth M Williamson; D T Okpako; Fred J Evans]
Hosagoudar, V. B., G. Rajkumar, C. K. Biju & T. K. Abraham. Amazonia goniothalami sp. nov. and some additional records of fungi on Goniothalamus wightii from India. Mycotaxon 77: 431-433. 2001.. ABSTRACT: An endemic plant, Goniothalamus wightii, was infected with four fungi. Of these, Amazonia gonioithalami was found to be an undescribed species; Trichasterina goniothalami is reported here in a new locality. Spiropes dorycarpus and S. guareicola are hyperparasites on these two fungi.. KEYWORDS: Amazonia, Trichasterina, Hyperparasites. NOMENCLATURAL NOVELTIES ...
The dextrorotary (R)-(+)-enantiomer is the most pharmacologically active, although a variety of related derivatives have been studied.[3] Side effects including chest pain (suggestive of possible cardiovascular toxicity) have been seen following recreational use of diphenylprolinol, although it was combined with glaucine in a party pill product, thus making it impossible to say for certain which drug was responsible.[4] ...
Thurs. 02.23.17 - For years I have used the word conuberation to mean a rather exuberant mashup of people or things or emotions as…. ...
You know how you meet little old ladies, who see you with your child, and they smile and say Enjoy this, they grow up so fast! I always smile and nod and say Oh I understand. Because they mean well, and theyre right - 3 out of 4 times. I dont say Well, THIS one…
You know how you meet little old ladies, who see you with your child, and they smile and say Enjoy this, they grow up so fast! I always smile and nod and say Oh I understand. Because they mean well, and theyre right - 3 out of 4 times. I dont say Well, THIS one…
I honestly think the best part, though, may be that Simon is like a different dog. Hes always been terrified of strangers, yet on one of our lengthy lets-wear-out-the-puppy walks this week he walked up to a complete stranger to say hello, and allowed said stranger to pat his head. I have never ever ever seen him do anything like it. Hes no longer at all anxious in the car (although Phoebe is still barfing any time shes in a moving vehicle for more than 10 minutes). Hes no longer whining in his crate. His appetite has returned. Hes happily trotting along next to Phoebe on walks with the double leash, and no longer jumping at every sound. Its like someone flipped a neuroses off switch in the dim recesses of his fuzzy little brain. I so desperately hope it lasts ...
Im 26, have had diabetes since I was 8, have been on a pump since 2000, and have been a nurse since January of 2011. My life is kind of crazy - but then again, so am I so it all works! I just moved to a new city in a new state for a new job, so theres a lot to figure out in addition to the usual stuff that requires figuring. Join me on my crazy journey through life as a nurse with diabetes.. ...
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Aug. 19, 2019 - The Jupiter-Saturn Conjunction Brings Economic Shift; Hong Kong Fights for Independence; Great Thunberg and the UN Climate Summit
Phoebe is being released from the hospital tomorrow. She has done pretty well with this round of chemo, but it was discovered that she has unrinary tract infection. I am glad they finally figured out what was bothering her. She had complained that her bottom was hurting for about 2 weeks but we could never…
Embolia crônica e trombose da veia poplítea direita icd 10. Sinais de trombose venosa profunda no pé. PAtologia - Doenças vasculares , cardíacas e pulmonares Icd da 10 veia e embolia direita trombose crônica poplítea, 5 principais veias do corpo.
... is an anti-cholinergic aporphine alkaloid. Naaz, H; Singh, S; Pandey, VP; Singh, P; Dwivedi, UN (2013). "Anti- ...
The most common structural types are the benzylisoquinolines and the aporphines. According to current knowledge, a total of ...
Azasteroid Aporphine Heterocyclic compound India portal Chemistry portal His adviser for master's degree was S. M. Mukherji ... Among the other natural products and drugs he synthesized include steroidal sapogenins, phenanthridine, aporphine, quinculidine ... for the synthesis of the phenanthridine ring system and other heterocyclic systems as well as the synthesis of aporphine and ...
Miller RJ, Kelly PH, Neumeyer JL (1976). „Aporphines. 15. Action of aporphine alkaloids on dopaminergic mechanisms in rat brain ... 1976). „Aporphines. 14 Dopaminergic and antinociceptive activity of aporphine derivatives. Synthesis of 10-hydroxyaporphines ...
The leaves of Annona muricata contain annonamine, which is an aporphine-class alkaloid featuring a quaternary ammonium group.[ ... Matsushige, A; Kotake, Y; Matsunami, K; Otsuka, H; Ohta, S; Takeda, Y (2012). "Annonamine, a new aporphine alkaloid from the ...
Zetler, G (1988). "Neuroleptic-like, anticonvulsant and antinociceptive effects of aporphine alkaloids: Bulbocapnine, ...
... acts as a potent agonist for the 5HT2A receptor,[1][2] with a Ki of 0.061 nM at the human 5HT2A receptor, similar to the better-known compound 25I-NBOMe, making it some twelve times the potency of 2C-I itself. Although in vitro tests show this compound acts as an agonist, animal studies to confirm these findings have not been reported. While the N-benzyl derivatives of 2C-I had significantly increased binding to 5HT2A receptor fragments, compared to 2C-I, the N-benzyl derivatives of DOI were less active compared to DOI.[3] 25I-NBOH is notable as one of the most selective agonist ligands for the 5-HT2A receptor with an EC50 value of 0.074 nM with more than 400 times selectivity over the 5-HT2C receptor.[4] ...
... is a potent and long lasting anticholinergic deliriant drug, related to the chemical warfare agent 3-Quinuclidinyl benzilate (QNB). It was developed under contract to Edgewood Arsenal during the 1960s as part of the US military chemical weapons program, during research to improve upon the properties of earlier agents such as QNB. The main advantages of EA-3443 were not only increased potency over QNB, but also a significantly improved central to peripheral effects ratio. Anticholinergic drugs produce both incapacitating deliriant effects through action in the brain, and a variety of distinctive physical symptoms such as dry mouth, dilated pupils, blurred vision and hot flushed skin, all of which together comprise the "anticholinergic syndrome" which is generally easy for doctors to diagnose. EA-3443 however is mainly selective for the brain, and when administered in a narrow dose range of around 0.3mg can produce the central effects of confusion, hallucinations and amnesia, but without ...
Schedule I in Sweden. 2C-T-2 was first classified as "health hazard" under the act Lagen om förbud mot vissa hälsofarliga varor (translated Act on the Prohibition of Certain Goods Dangerous to Health) as of April 1, 1999, under SFS 1999:58[6] that made it illegal to sell or possess. The Riksdag added 2C-T-2 to Narcotic Drugs Punishments Act under Swedish schedule I ("substances, plant materials and fungi which normally do not have medical use") as of March 16, 2004, published by Medical Products Agency (MPA) in regulation LVFS 2004:3 listed as 2C-T-2, 2,5-dimetoxi-4-etyltiofenetylamin.[7] ...
In the United Kingdom, 2C-E is a Class A controlled substance. The UK has the strictest laws in the EU on designer drugs. The Misuse Of Drugs Act was amended in 2002 to include a "catch most" clause outlawing every drug, and possible future drug, from the LSD (ergoline) and MDMA (phenethylamine) chemical families (including 2C-E). The amendment is a near verbatim quote from the books of the American biochemist Alexander Shulgin, who obtained a PhD from the University of California, Berkeley. Dr. Shulgin, a former research chemist at the Dow Chemical Company, re-discovered the synthesis for MDMA in 1976 and published the syntheses for more than 200 phenethylamine compounds of his own invention, and 55 tryptamine compounds many of which were also his own invention. The Shulgins were motivated to release the synthesis information as a way to protect the public's access to information about psychedelic compounds, a goal Alexander Shulgin has noted many times. ...
... (INN) (brand names Lethidrone, Nalline), also known as N-allylnormorphine, is a mixed opioid agonist-antagonist with opioid antagonist and analgesic properties.[1] It was introduced in 1954[2] and was used as an antidote to reverse opioid overdose and in a challenge test to determine opioid dependence.[3] It acts at two opioid receptors - the μ-opioid receptor (MOR) where it has antagonistic effects, and at the κ-opioid receptor (KOR) (Ki = 1.6 nM; EC50 = 483 nM; Emax = 95%) where it exerts high-efficacy partial agonist/near-full agonist characteristics.[4] Nalorphine was the second opioid antagonist to be introduced, preceded by nalodeine (N-allylnorcodeine) in 1915 and followed by naloxone in 1960 and naltrexone in 1963.[2] Due to potent activation of the KOR, nalorphine produces side effects such as dysphoria, anxiety, confusion, and hallucinations, and for this reason, is no longer used medically.[1][2][5] Nalorphine has a number of analogues including niconalorphine (the ...
... (JB-318) is an anticholinergic drug related to the chemical warfare agent 3-Quinuclidinyl benzilate.. N-Ethyl-3-piperidyl benzilate is less potent and shorter acting than 3-quinuclidyl benzilate, but like 3-QNB its effects on the central nervous system predominate over peripheral effects. It produces deliriant and hallucinogenic effects similar to those of plants such as datura and may be used recreationally at low doses; however, unpleasant side effects such as dysphoria, nausea and vomiting, dizziness and extreme dry mouth tend to make abuse of drugs of this kind uncommon. Both the N-methyl and N-ethyl analogues of 3-piperidyl benzilate are, however, Schedule I controlled drugs.. Radiolabelled versions of this drug have been used in scientific research to map the distribution of muscarinic acetylcholine receptors in the brain, however this drug has slightly lower binding affinity than the N-methyl analogue and so is less potent and not so widely used for this ...
... is widely used in preparations as an enhancing agent for some analgesics and antitussives (acetaminophen, dihydrocodeine, codeine, hydrocodone). It is widely used in certain parts of the world as cough suppressant usually with codeine, and sometimes by itself or in addition to dextromethorphan as it, like diphenhydramine, possesses antitussive action of its own and is particularly useful in semi-productive coughs because of its moderate drying action. Phenyltoloxamine has analgesic and anti-spasmodic properties of its own[citation needed] and is used in combination with paracetamol, aspirin and other salicylates and other drugs in proprietary preparations available over the counter for backache, muscle strains and similar conditions. In this respect, it is similar to a closely related antihistamine, orphenadrine, and both drugs are very closely related to diphenhydramine and to doxylamine, the latter of which is the active ingredient in NyQuil and many other cough ...
The effects of dissociatives can include sensory dissociation, hallucinations, mania, catalepsy, analgesia and amnesia.[5][6][7] The characteristic features of dissociative anesthesia were described as catalepsy, amnesia and analgesia.[5] According to Pender (1972), "the state has been designated as dissociative anesthesia since the patient truly seems disassociated from his environment."[8] Bonta (2004) described dissociative anaesthesia as "... a peculiar anaesthetic state in which marked sensory loss and analgesia as well as amnesia is not accompanied by actual loss of consciousness."[9] Both Pender (1970) and Johnstone et al. (1959) reported that patients under anaesthesia due to either ketamine or phencyclidine were prone to purposeless movements and had hallucinations (or "dreams"[10]) during and after anaesthesia. Some patients found the hallucinations euphoric while others found them disturbing. At sub-anesthetic doses, dissociatives alter many of the same cognitive and perceptual ...
The full name of the chemical is 2,5-dimethoxy-4-bromoamphetamine. DOB has a stereocenter and R-(-)-DOB is the eutomer. This is an important finding as it is suggestive that it is targeting different receptors relative to most other phenethylamines (e.g. MDMA) where the R-isomer serves as the distomer. The toxicity of DOB is not fully known, although high doses may cause serious vasoconstriction of the extremities. DOB is one of the most potent compounds in PiHKAL; while the active dose is similar to that of DOI, another psychedelic amphetamine, DOB has been shown to have a higher efficacy in triggering downstream effects mediated by 5-HT2 receptors,[4] making it likely to be slightly more dangerous than DOI in overdose, due to greater vasoconstrictive action. Omission of the amphetamine related α-methyl leads to 2C-B, a compound that possesses a lower affinity for the 5-HT2A receptor and is a weaker receptor agonist which results in drastically reduced vasoconstriction.[citation needed] ...
... (5-Me-MiPT) is a tryptamine derivative that is thought to be a psychedelic drug. It was first made in 1989. In vitro binding experiments on brain homogenates showed it to have a binding affinity between that of MiPT and 5-MeO-MiPT,[1] both of which are known to be active psychedelics in humans.. ...
Drug discrimination studies showed that 5-methyl-MDA substitutes for MDA, MMAI, and LSD, but not amphetamine, suggesting that it produces a mix of entactogen and hallucinogenic effects without any stimulant effects.[2]. 5-Methyl-MDA acts as a selective serotonin releasing agent (SSRA) with IC50 values of 107nM, 11,600nM, and 1,494nM for serotonin, dopamine, and norepinephrine efflux.[1] It is over 5x more potent than MDA, with a suitable active dose possibly being around 15-25 mg.[1][2] Subsequent testing, however, has found that it is not as potent as once thought and is active at at least 100mg. 2-Methyl-MDA is also much more potent than MDA, but is not quite as potent as 5-methyl-MDA.[1] 6-methyl-MDMA (also known as Madam-6) is mostly inactive, likely due to steric hindrance.[1][3]. Recent research has used data on 2-methyl-MDA and 5-methyl-MDA to help guide computer modeling of the serotonin transporter complex.[4]. ...
... ,[2] sold under the brand name Talwin among others, is a painkiller used to treat moderate to severe pain. It is believed to work by activating (agonizing) κ-opioid receptors (KOR) and blocking (antagonizing) μ-opioid receptors (MOR). As such it is called an opioid as it delivers its effects on pain by interacting with the opioid receptors. It shares many of the side effects of other opioids like constipation, nausea, itching, drowsiness and respiratory depression, but unlike most other opioids it fairly frequently causes hallucinations, nightmares and delusions. It is also, unlike most other opioids, subject to a ceiling effect, which is when at a certain dose (which differs from person-to-person) no more pain relief, or side effects, is obtained by increasing the dose any further.[3] Chemically it is classed as a benzomorphan and it comes in two enantiomers, which are molecules that are exact (non-superimposable) mirror images of one another. It was patented in 1960 and approved ...
... is an arylcyclohexylamine dissociative anesthetic drug with hallucinogenic and stimulant effects. It is around the same potency as phencyclidine, although slightly less potent than its ethyl homologue eticyclidine,[1] and has reportedly been sold as a designer drug in Germany and other European countries since the late 1990s.[2][3] Several other related derivatives have also been encountered, with the n-propyl group of PCPr replaced by a 2-methoxyethyl, 2-ethoxyethyl or 3-methoxypropyl group to form PCMEA, PCEEA and PCMPA respectively.[4][5][6] ...
For example, aporphine alkaloid liriodenine produced by the tulip tree protects it from parasitic mushrooms. In addition, the ...
There are a variety of clinically useful ergoline derivatives for the purpose of vasoconstriction, the treatment of migraines, and treatment of Parkinson's disease. Ergoline alkaloids found their place in pharmacology long before modern medicine as preparations of ergot were often used by midwives in the 12th century to stimulate childbirth.[10] Following Arthur Stoll's isolation of ergometrine, the therapeutic use of ergoline derivatives became well explored. The induction of uterine contractions via the preparation of ergot was attributed to ergonovine, an ergoline derivative found in ergot, which is a powerful oxytocic. From this, methergine, a synthetic derivative, was elucidated.[7] While used to facilitate child birth, ergoline derivatives can pass into breast milk and should not be used during breastfeeding.[11] They are uterine contractors that can increase the risk of miscarriage during pregnancy.[3] Another example of medically relevant ergoline alkaloids is ergotamine, an alkaloid ...
... (DOPR) is a psychedelic drug of the phenethylamine and amphetamine chemical classes. It was first synthesized by Alexander Shulgin, and was described in his book PiHKAL (Phenethylamines i Have Known And Loved). Shulgin described DOPR is a "heavy duty psychedelic", complete with alterations of the thought process and visual distortion.[1] Very little data exists about the pharmacological properties, metabolism, and toxicity of DOPR. The alternative structural isomer DOIP, with a 4-isopropyl substitution, is also known but is around ten times weaker than DOPR, with an active dose of some 20-30 mg (as compared to 2-5 mg for DOPR).[1] ...
... (5-bromo-N,N-dimethyltryptamine) is a psychedelic brominated indole alkaloid found in the sponges Smenospongia aurea and Smenospongia echina, as well as in Verongula rigida (0.00142% dry weight) alongside 5,6-Dibromo-DMT (0.35% dry weight) and seven other alkaloids.[1][2][3][4] It is the 5-bromo derivative of DMT, a psychedelic found in many plants and animals. 5-Bromo-DMT has a pEC50 value of 5.51 for the 5-HT2A receptor.[5] Animal studies on 5-Bromo-DMT showed that it produces effects suggestive of sedative and antidepressant activity and caused significant reduction of locomotor activity in the rodent FST model.[6] 5-Bromo-DMT was reported to be psychoactive at 20-50 mg via vaporization with mild psychedelic-like activity.[7] ...
Sveriges riksdags health ministry Statens folkhälsoinstitut classified 4-AcO-DiPT as "health hazard" under the act Lagen om förbud mot vissa hälsofarliga varor (translated Act on the Prohibition of Certain Goods Dangerous to Health) as of Mar 1, 2005, in their regulation SFS 2005:26 listed as 4-acetoxi-N,N-diisopropyltryptamin (4-AcO-DIPT), making it illegal to sell or possess.[3] ...
Hallucinogenic Drug" means those specified in Section 7 of this rule including stramonium, mescaline or peyote, lysergic acid diethylamide, and psilocybin, and all synthetic equivalents of chemicals contained in resinous extractives of Cannabis sativa, or any salts or derivatives or compounds of any preparations or mixtures thereof, and any other substance having a hallucinogenic effect in the regulations adopted by the Board of Health under 18 V.S.A.§ 4202. ... • Cannabimimetic Agents means, collectively, any chemical that is a cannabinoid receptor type 1 (CB1) or cannabinoid receptor type 2 (CB2) agonist, or any salts, isomers, derivatives, or analogs of these chemicals. Structural classes include but are not limited to: (a) 2-(3-hydroxycyclohexyl)phenol with substitution at the 5-position of the phenolic ring by alkyl or alkenyl, whether or not substituted on the cyclohexyl ring to any extent. (b) 3-(1-naphthoyl)indole or 3-(1-naphthyl)indole with substitution at the nitrogen atom of the ...
N,N-Dimethyllysergamide or N,N-dimethyl-D-lysergamide (DAM-57) is a derivative of ergine. There has been a single report of observing N,N-dimethyl-D-lysergamide in the illicit drug market.[1] This compound did induce autonomic disturbances at oral levels of some ten times the dosage required for LSD, presumably in the high hundreds of micrograms. There is some disagreement as to whether there were psychic changes observed.[2] ...
... (DOEF), also known as dimethoxyfluoroethylamphetamine, is a lesser-known psychedelic drug and member of the DOx class.[1][2] DOEF was first synthesized by Alexander Shulgin. In his book PiHKAL (Phenethylamines i Have Known And Loved), the dosage range is listed as 2-3.5 mg, and the duration is listed as 12-16 hours.[3] Very little data exists about the pharmacological properties, metabolism, and toxicity of DOEF. ...
... has been clinically tested in cancer patients for its pain relief and antiemetic benefits. Cancer patients that endure chemotherapy often develop intense nausea, and Levonantradol has been tested to reduce these emetic symptoms. It is often used instead of THC because it has a higher efficacy. Levonantradol also acts on pain pathways in the central nervous system, which enables the drug to alleviate pain. Studies have shown an absence of emetic side effects within the half-life of the Levonantradol administered. Other studies suggest that cannabinoid agonists can synergize opioid anti-nociception. Cannabinoid receptors are located in nociceptive pathways, and CBs can promote signal transduction in TRP channels. Although Levonantradol relieves nociceptive and postoperative pain, decreases nausea, and improves spasticity in addition to being more effective than placebos, it has yet to be approved as legal medicine. Researchers have concluded that Levonantradol is no more effective ...
... acts on M2 and M3[3] subtypes of muscarinic receptors whereas older antimuscarinic treatments for overactive bladder act more specifically on M3 receptors. Tolterodine, although it acts on all types of receptors, has fewer side effects than oxybutynin (M3 and M1 selective, but more so in the parotid than in the bladder) as tolterodine targets the bladder more than other areas of the body. This means that less drug needs to be given daily (due to efficient targeting of the bladder) and so there are fewer side effects.[citation needed] ...
... (also known as NBOMe-2C-TFM, 2C-TFM-NBOMe, and Cimbi-138) is a derivative of the phenethylamine hallucinogen 2C-TFM, discovered in 2004 by Ralf Heim at the Free University of Berlin.[1] It acts as a potent partial agonist for the 5HT2A receptor, though its relative potency is disputed, with some studies finding it to be of lower potency than 25I-NBOMe,[2][3] while others show it to be of similar or higher potency,[4] possibly because of differences in the assay used.[5] 2C-TFM-NB2OMe can be taken to produce psychedelic effects similar to 2C-I-NB2OMe and 2C-D-NB2OMe. ...
The aporphine template is known to be associated with a range of biological activities. Aporphines have been explored as ... Aporphines are also inhibitors of the acetylcholinesterase enzyme - a clinical target for the treatment of Alzheimers disease ... Within the Central Nervous Systems (CNS), aporphine alkaloids are known to possess high affinity for several clinically ... Considering the diverse profile of aporphine alkaloids at CNS receptors they can be considered as ...
The aporphine alkaloid boldine improves endothelial function in spontaneously hypertensive rats. Exp Biol Med (Maywood). 2012 ...
The flowers contain the alkaloids aporphine and nuciferine as well as other related compounds. Some people like to smoke a ... The flowers contain the alkaloids aporphine and nuciferine as well as other related compounds. Some people like to smoke a ...
Boldine is an aporphine alkaloid that is found in high amount in boldo tree and Lindera aggregate. It is used as homeopathic ... Introduction: Boldine is an aporphine alkaloid that is found in high amount in boldo tree and Lindera aggregate. It is used as ...
Liriodenine, an aporphine alkaloid from Enicosanthellum pulchrum, inhibits proliferation of human ovarian cancer cells through ... Liriodenine, an aporphine alkaloid from Enicosanthellum pulchrum, inhibits proliferation of human ovarian cancer cells through ...
Aporphine and tetrahydroprotoberberine alkaloids from the leaves of Guatteria friesiana (Annonaceae) and their cytotoxic ... The presence of aporphine and tetrahydroprotoberberine alkaloids in the leaves of G. friesiana is consistent with previous ... Aporphine and tetrahydroprotoberberine alkaloids isolated from the leaves of Guatteria friesiana (Annonaceae). ... 13 as well as aporphine alkaloids.8 The alkaloids and essential oils exhibited antitumor and antimicrobial properties,4,6-9 as ...
Aporphine alkaloids are its characteristic ingredients and responsible for its bioactivities, especially anti-inflammatory and ... The fragmentation pathways by loss of CO, ·CH3 , ·NH3 , and ·NH2 CH3 were detected as characteristic for aporphine alkaloids. ... The established method is simple, rapid, and specific for characterization and quantitation of aporphine alkaloids in Dou-chi- ... The quantification method was validated in terms of linearity, precision, and accuracy for six major aporphine alkaloids, which ...
The organic solvent extracts of M. crispat, M. brevipes and their isolated aporphines showed varied levels of activity against ... The oxoaporphines were generally the most active especially against L. donovani (14.59 ≤ IC50 ≥ 52.20 μm). The aporphine, (+)- ... Eleven aporphines alkaloids (Figure 1) identified as, (-)- mocrispatine (1); (-)-pallidine (2); (-) N-méthylarmépavine (3 ... The generally low antiprotozoal activity of the aporphines does not make them good candidates for either leishmaniasis or ...
en] Purification of a cytotoxic crude alkaloid extract of Cassytha filiformis led to the isolation of four known aporphine ... en] 3T3 Cells/drug effects ; Animals ; Aporphines/chemistry/pharmacology ; Female ; HL-60 Cells/drug effects ; Hela Cells/drug ...
Oliveroline is an anti-cholinergic aporphine alkaloid. Naaz, H; Singh, S; Pandey, VP; Singh, P; Dwivedi, UN (2013). "Anti- ...
The most common structural types are the benzylisoquinolines and the aporphines. According to current knowledge, a total of ...
Omar, H.; Hashim, N.M.; Zajmi, A.; Nordin, N.; Abdelwahab, S.I.; Azizan, A.H.S.; Hadi, A.H.A.; Ali, H.M. Aporphine alkaloids ... Results: Cinnamic acid (1) and two aporphine alkaloids (liridine (2) and lysicamine (3)) have been successfully purified and ... Title:Purification of Cinnamic Acid and Aporphine Alkaloids from Enicosanthellum pulchrum Twig Extract and their Biological ... Results: Cinnamic acid (1) and two aporphine alkaloids (liridine (2) and lysicamine (3)) have been successfully purified and ...
Aporphine alkaloids from Piper erecticaule and acetylcholinesterase inhibitory activity Aporphine alkaloids from Piper ... Full text: Available Index: LILACS (Americas) Main subject: Aporphines / Acetylcholinesterase / Plant Extracts / Cholinesterase ... Aporphines/pharmacology , Acetylcholinesterase/drug effects , Plant Extracts/chemistry , Cholinesterase Inhibitors/pharmacology ... Piper/chemistry , Alkaloids/pharmacology , Aporphines/chemistry , Terpenes/isolation & purification , Cholinesterase Inhibitors ...
Aporphine, 1,2,10-trimethoxy-, dl- - Similar structures search, synonyms, formulas, resource links, and other chemical ... Substance Name: Aporphine, 1,2,10-trimethoxy-, dl-. RN: 28277-71-6. InChIKey: RZERUPREKNWRRD-UHFFFAOYSA-N. ...
The Aporphines. I. Introduction II. A Classical Degradation of an Aporphine III. Apomorphine IV. Nonbiogenetic Syntheses of ... Ushinsunine: A C-7 Hydroxylated Aporphine XV. Steporphine: A C-4 Hydroxylated Aporphine XVI. The Dehydroaporphines References ... The Oxidation of Aporphines and the Reduction of Oxoaporphines. IV. An Unusual Demethoxylation Reaction V. Pharmacology VI. NMR ... The Aporphine-Benzylisoquinoline Dimers. I. Introduction II. Structural Elucidation and Synthesis III. Biosynthesis IV. ...
Aporphine. Aporphine Chemical structure of aporphine colspan=2 style="background:#f8eaba; border-top:2px solid transparent; ... Aporphine is a 5-HT1a partial agonist with a ki of 80nM and a 5-HT7 antagonist with a ki of 88nM.[2] Aporphine is a Dopamine D1 ... Aporphine is one of a class of quinoline alkaloids. Many different relatives of this compound have been purified from plants.[1 ... This page is based on the copyrighted Wikipedia article Aporphine; it is used under the Creative Commons Attribution-ShareAlike ...
Alkaloids from Cassytha filiformis and related aporphines : antitrypanosomal activity, cytotoxicity and interaction with DNA ... Home» Alkaloids from Cassytha filiformis and related aporphines : antitrypanosomal activity, cytotoxicity and interaction with ... Alkaloids from Cassytha filiformis and related aporphines : antitrypanosomal activity, cytotoxicity and interaction with DNA ...
New Analogues of Aporphine Alkaloids. , 2018; 18(19): 1590-1602.. Yi-Chao Ge and Kui-Wu Wang*. DOI: 10.2174/ ...
Miller RJ, Kelly PH, Neumeyer JL (1976). „Aporphines. 15. Action of aporphine alkaloids on dopaminergic mechanisms in rat brain ... 1976). „Aporphines. 14 Dopaminergic and antinociceptive activity of aporphine derivatives. Synthesis of 10-hydroxyaporphines ...
Aquatic herbs, rhizomatous; mycorrhizae 0; latex, aporphine alkaloids +; radicle aborts; root stele polyarch; cork?; plant with ...
Aporphines and Alzheimers Disease: Towards a Medical Approach Facing the Future. Seyed Mohammad Nabavi, Eugenio Uriarte, Luca ...
Topics: Medicinal chemistry; Natural products; Photochemistry reactivity; Aporphines, oxoaporphines, and oxoisoaporphines; ... Topics: Medicinal chemistry; Natural products; Photochemistry reactivity; Aporphines, oxoaporphines, and oxoisoaporphines; ... Topics: Medicinal chemistry; Natural products; Photochemistry reactivity; Aporphines, oxoaporphines, and oxoisoaporphines; ...
For example, aporphine. alkaloid liriodenine produced by the tulip tree protects it from parasitic mushrooms. In. addition, the ... Aporphines [77]. Proaporphines [77]. Homoaporphines [92]. Homoproaporphines [92]. Morphines[93]. ipecoside [89]. Sanguinarine, ...
The very planar conformation of oxo-aporphine alkaloid 1 may account for its higher genotoxicity vs. its less-planar analogues ... 0 (Alkaloids); 0 (Analgesics, Opioid); 0 (Aporphines); 0 (Plant Extracts); 1HG84L3525 (Formaldehyde); 7V31YC746X (Chloroform); ...
Monimiaceae [Hernandiaceae + Lauraceae]]: aporphine alkaloids and variants +; (cork cambium outer cortical); crystals +, small ... about half of them are aporphine alkaloids (Conserva et al. 2005; see also J.-J. Chen et al. 2011). Their distributions show no ...
... aporphine); Luteanine; S-(+)-Isocorydine; 4H-Dibenzo(de,g)quinolin-11-ol, 5,6,6a,7-tetrahydro-1,2,10-trimethoxy-6-methyl-, (S ...
Aporphines. Sub Class. Not Available. Direct Parent. Aporphines. Alternative Parents. Phenanthrenes and derivatives / ... Aporphine / Benzoquinoline / Phenanthrene / 2-naphthol / 1-naphthol / Naphthalene / Quinoline / Tetrahydroisoquinoline / 1- ... This compound belongs to the class of organic compounds known as aporphines. These are quinoline alkaloids containing the ...
... is a aporphine alkaloid (CHEBI:134209) Synonym Source Boldine KEGG COMPOUND ...
... and aporphine, such as xylopine (Table 1). ...
The leaves of Annona muricata contain annonamine, which is an aporphine-class alkaloid featuring a quaternary ammonium group.[ ... Matsushige, A; Kotake, Y; Matsunami, K; Otsuka, H; Ohta, S; Takeda, Y (2012). "Annonamine, a new aporphine alkaloid from the ...
Montenegro, H.; Gutierrez, M.; Romero, L.I.; Ortega-Barria, E.; Capson, T.L.; Rios, L.C. Aporphine alkaloids from Guatteria spp ...
2014) reported that aporphine alkaloids are the primary components of Illigeralu zonensis, exhibited varying degrees of ... 2014) discovered that the plant Illigera luzonensis Merr contains aporphine alkaloids. These researchers also found that ... Antiplatelet activity of N-methoxycarbonyl aporphines from Rollinia mucosa. Phytochemistry 57, 421-425. doi: 10.1016/S0031-9422 ... actinodaphnine, which belongs to aporphine alkaloids, exhibited significant inhibition of the aggregation of washed rabbit ...
  • Aporphines are a group of tetracyclic alkaloids that belong to the ubiquitous tetrahydroisoquinoline family. (cuny.edu)
  • Within the Central Nervous Systems (CNS), aporphine alkaloids are known to possess high affinity for several clinically valuable targets including dopamine receptors (predominantly D 1 and D 2 ), serotonin receptors (5-HT 1A and 5-HT 7 ) and α adrenergic receptors. (cuny.edu)
  • Considering the diverse profile of aporphine alkaloids at CNS receptors they can be considered as "privileged scaffold" for the design of CNS drugs. (cuny.edu)
  • The aporphine alkaloid nantenine is a 5-HT 2A receptor antagonist and has moderate affinity for the 5-HT 2A receptor. (cuny.edu)
  • Liriodenine, an aporphine alkaloid from Enicosanthellum pulchrum, inhibits proliferation of human ovarian cancer cells through induction of apoptosis via the mitochondrial signaling pathway and blocking cell cycle progression. (nih.gov)
  • The aporphine template is known to be associated with a range of biological activities. (cuny.edu)
  • [ 4 ] Aporphine and its related alkaloids bulbocapnine, boldine, glaucine and corytuberine are antipsychotic, exert naloxone -reversible antinociceptive activity and with the exception of corytuberine are anticonvulsant. (omicsgroup.org)
  • Study of butanol extract of leaves and twigs yielded two new aporphine alkaloids, namely litseglutine A and B, along with two known aporphine alkaloids, boldine and laurolitsine. (stuartxchange.org)
  • Isoquinoleinic alkaloids (0.2-0.5%): Boldo contains about 20 alkaloids derived from aporphine, the most important being boldine, which represents 25-30% of the total alkaloids. (botanical-online.com)
  • It contains 0.2% aporphine alkaloids with boldine as its main compound, as well as flavonols and their glycosides (boldoglucin and isorhamnetin). (ageless.co.za)
  • The most common structural types are the benzylisoquinolines and the aporphines. (wikipedia.org)
  • Genus Phoebe have been reported to produce isoquinoline alkaloids as aporphines, noraporphines, and benzylisoquinolines. (phcogj.com)
  • Aporphine and protopine, which are isoquinoline alkaloids, have been found in Dicentra species. (gc.ca)
  • The chromatographic conditions were optimized on a SinoChrom ODS-BP column to obtain a good separation of the four types of alkaloid analytes, including two aporphines (isocorydine, corydine), two protopines (protopine and allocryptopine), a morphine (sinoacutine), and three quaternary protoberberine alkaloids (berberrubine, 5-hydroxycoptisine, and berberine). (jove.com)
  • Anti-protozoal activity of aporphine and protoberberine alkaloids from Annickia kummeriae (Engl. (ac.ke)
  • In the search for agents from tropical medicinal plants to treat these two neglected tropical diseases, serially extracted petroleum ether, dichloromethane and methanol extracts of the leaves of Monodora crispata and Monodora brevipes , and eleven aporphines alkaloids isolated from the dried powdered leaves of the two plants were evaluated against Leishmania donovani promastigotes and Trypanosoma brucei brucei trypomastigotes. (omicsonline.org)
  • Cytotoxic aporphine alkaloids from Cassytha filiformis. (uliege.be)
  • en] Purification of a cytotoxic crude alkaloid extract of Cassytha filiformis led to the isolation of four known aporphine alkaloids: neolitsine, dicentrine, cassythine (= cassyfiline) and actinodaphnine. (uliege.be)
  • This supports the idea that aporphine alkaloids are responsible for the plant's cytotoxic activity. (naturalnews.com)
  • Two new natural azaflu-orene alkaloids and a cytotoxic aporphine alkaloid from Poiyaithia longifolia . (springer.com)
  • Cerasoidine, a bis-aporphine alkaloid isolated from Poiyaithia cerasoides during screening for Wnt signal inhibitors. (springer.com)
  • Asimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. (medchemexpress.com)
  • These compounds will further expand our understanding of the tolerance of the aporphine core required for 5-HT 2A antagonism. (cuny.edu)
  • Accordingly, there is a need in the art for new methods in addition to the linear skin incision model in rats which allow direct observations and measurements of wound-healing acceleration in taspine and taspinates and their aporphine-derived analogs and other aporphine-derived compounds. (google.com)
  • They were able to identify four major compounds, which were the aporphine alkaloids actinodaphnine, anonaine, isoboldine, and nornuciferine. (naturalnews.com)
  • In order to understand the structural tolerance of the aporphine core required for 5-HT 2A antagonism an exhaustive Structure Activity Relationship (SAR) study was designed.Accordingly, a diverse library of nantenine analogues was synthesized and evaluated for affinity at the 5-HT 2A receptor. (cuny.edu)
  • Based on results of these studies, it is concluded that the interaction of C3 halogenated aporphine analogues with Phe339/Phe340 residues might be responsible for their enhanced affinity. (cuny.edu)
  • These are analogues of Aporphines, where a nitrogen atom replaces the carbon atom at position 1, and a keto group at C7. (hmdb.ca)
  • Comparative assessment of dopamine agonist aporphines as anticonvulsants in two models of reflex epilepsy. (axonmedchem.com)
  • 14 Dopaminergic and antinociceptive activity of aporphine derivatives. (wikipedia.org)
  • The aporphine alkaloid nantenine is a 5-HT 2A receptor antagonist and has moderate affinity for the 5-HT 2A receptor. (cuny.edu)
  • The aporphine core of nantenine serves as a valuable lead for the identification of selective 5-HT 2A antagonists. (cuny.edu)
  • Scientists attribute the family's wide range of pharmacological activities to acetogenins and isoquinolines, specifically aporphine alkaloids . (naturalnews.com)
  • The relative concentration of alkaloids and phenolics in boldo leaves and their activity suggest that free-radical scavenging effect is mainly due to catechin and flavonoids and that antioxidant effect is mainly related with the catechin content The high catechin content of boldo leaves and its bioactivity suggest that quality control of Boldo folium has to combine the analysis of catechin as well as their characteristic aporphine alkaloids. (worldwidescience.org)
  • 1976). „Aporphines. (wikipedia.org)
  • Cotzias GC, Papavasiliou PS, Tolosa ES, Mendez JS, Bell-Midura M (1976) Treatment of Parkinson's disease with aporphines. (springer.com)
  • Phylogenetic analysis was performed for each of 15 different enzyme/protein groupings, highlighting many novel genes with potential involvement in the formation of one or more alkaloid types, including morphinan, aporphine, and phthalideisoquinoline alkaloids. (beds.ac.uk)
  • Se evaluó en laboratorio la actividad insecticida de polvo y extractos líquidos etanólicos y hexánicos del boldo ( Peumus boldus Molina sobre S. zeamais y T. castaneum. (worldwidescience.org)
  • [ 5 ] Some derivatives of aporphine such as S(+)-N-propylnorapomorphine have potential as low side effect profile antipsychotics. (omicsgroup.org)
  • Aporphine alkaloids are its characteristic ingredients and responsible for its bioactivities, especially anti-inflammatory and analgesic effects. (sigmaaldrich.com)
  • The fragmentation pathways by loss of CO, ·CH3 , ·NH3 , and ·NH2 CH3 were detected as characteristic for aporphine alkaloids. (sigmaaldrich.com)
  • The high catechin content of boldo leaves and its bioactivity suggest that quality control of boldo folium has to combine the analysis of catechin as well as their characteristic aporphine alkaloids. (sigmaaldrich.com)
  • Aporphines have been explored as antioxidants, anti-tuberculosis, antimicrobial and anticancer agents. (cuny.edu)
  • Norstephalagine ( 2 ) (an aporphine) and scopoletin ( 8 ) (a coumarin) were isolated from Liriodendron tulipifera leaves from the first time. (mdpi.com)
  • Aporphine Alkaloids from the Leaves of Phoebe grandis (Nees) Mer. (mdpi.com)
  • The quantification method was validated in terms of linearity, precision, and accuracy for six major aporphine alkaloids, which was successfully applied for simultaneous determination in ten batches of samples. (sigmaaldrich.com)
  • Results: Cinnamic acid (1) and two aporphine alkaloids (liridine (2) and lysicamine (3)) have been successfully purified and identified. (eurekaselect.com)
  • BBB-permeable aporphine-type alkaloids in Nelumbo nucifera flowers with accelerative effects on neurite outgrowth in PC-12 cells. (nih.gov)
  • Considering the diverse profile of aporphine alkaloids at CNS receptors they can be considered as "privileged scaffold" for the design of CNS drugs. (cuny.edu)