Feb 2, 2006 ... Pyrgomorphidae. Zonocerus variegatus. Grasshopper. Tata adults. Orthoptera. Acrididae. Cytacanthacris naeruginosus unicolor. Short horned grasshoppers. Tata adult. Coleoptera. Scarabaeidae. Analeptes trifasciata. Rhinoceros beetle. Ipe larvae. Coleoptera. Scarabaeidae. Oryctes boas. Scarab beetles.
Luis Enrique Aguirre Galvis
MAHz and 90 MHz of the analeptic sesquiterpene lactone coriamyrtin, isolated from the colombian plant Coriaria microphyUn, Poir., is discussed, and analogies are made with the spectra of authentic samples of picrotin and picrotoxinin.
Seventeen species of edible insects representing nine families from south western Nigeria were analyzed for nutrient composition. They include the orders of Orthoptera, Lepidoptera, Coleoptera, Hymenoptera, and Isoptera. Analeptes trifasciata, Rhynchophorus phoenicis and Zonocerus variegatus has the highest crude ...
I. I. Aksyonova-Seliuk
Full Text Available The purpose of the work was to investigate the effect of 5-(4-(tret-butylphenyl-4-R-amino-4H-1,2,4-triazole-3-thiols on the duration of thiopental-sodium narcosis for laboratory rats and to identify the regularities of the dependence “chemical structure – biological effect”. Materials and methods. The objects of research were 15 new compounds, derivatives of 4-amino-5-(4-(tret-butylphenyl-4H-1,2,4-triazole-3-thiols. These compounds are the crystal substances which are odorless, insoluble in water and soluble in organic solvents. The combined reception and interaction of the compounds with anesthetic agents for rats were considered. The time of the anesthetic thiopental sodium narcosis was marked by the time while the animal was in lateral position, since losing reversal’s reflex. Aminazine and caffeine-sodium benzoate (10 mg/kg and 50 mg/kg were used as a standard of comparison. Results and discussion. In the study we have found that 5-(4-(tret-butylphenyl-4-R-amino-4H-1,2,4-triazole-3-thiols exhibit different effects – deprimo action or analeptic action. For example, the presence of fluorine in the structure of compound contributes to some analeptic activity and vice versa the transition to disubstituted fluoride molecules causes small deprimo action. However the presence of chlorine leads to the appearance of clear raising to a higher power actions regarding to sodium thiopental, that is more than standard of comparison – aminazine. It is interesting to observe the activity change of a series of nitro containing compounds. Conclusions. The leader compound has been identified among the investigated compounds. It exceeds the standard of comparing (aminazine by indexes. Some regularities “chemical structure – biological effect” have been established. These results can be used in the future for targeted search of substances with analeptic or deprimo activity.
Rivera, D; Obón, C
The ethnopharmacology of Madeira and Porto Santo Islands is extremely interesting because of the cultural and biogeographic features of this region, which make it a centre of medicinal plant diversity (richness of endemic flora, geographical isolation in the Atlantic sea, crosscultural influences, and past abundance of local healers). The medicinal flora of Madeira is composed of 259 species. Some noteworthy medicinal taxa, endemic or locally relevant, are: Acanthus mollis, Aeonium glandulosum, Aeonium glutinosum, Bidens pilosa, Borago officinalis, Chamaemelum nobile var. discoideum, Culcita macrocarpa, Echium nervosum, Euphorbia platiphylla, Helichrysum melaleucum, Helichrysum obconicum, Hypericum glandulosum, Hypericum humifussum, Kleinia repens, Laurus azorica, Monizia edulis, Ocotea foetens, Psoralea bituminosa, Rubus bollei, Rumex maderensis, Sambucus lanceolata, Scilla maderensis, Sedum brissemoretii, Sedum farinosum, Sedum nudum, Sibthorpia peregrina, Teucrium betonicum, Thymus caespititius, Trifolium squamosum and Vaccinium padifolium. Among the medicinal cryptogams, one can underline the parasitic fungus Laurobasidium lauri, which grows on the stems of Laurus azorica and is used as an antirheumatic, haemostatic, emmenagogue, insecticide and analeptic.
Oh, Sa Rang; Kim, Su-Jin; Kim, Dong Hyun; Ryu, Jong Hoon; Ahn, Eun-Mi; Jung, Ji Wook
Memory impairment is the most common symptom in patients with Alzheimer's disease (AD). Angelica keiskei (AK) has traditionally been used as a diuretic, laxative, analeptic and galactagogue. However, the anti-amnesic effects of AK and its molecular mechanisms have yet to be clearly elucidated. The aim of the present study is to evaluate the effects of AK on scopolamine-induced memory impairments in mice. The regulatory effect of AK on memory impairment was investigated using passive avoidance, Y-maze and the Morris water maze tasks. Acetylcholinesterase (AChE) activity assay was performed to investigate the cholinergic antagonistic effect of AK in the hippocampus. The effect of AK on phosphorylation of cAMP response element-binding protein (CREB) and expression of brain-derived neurotrophic factor (BDNF) were evaluated by Western blot assays and immunohistochemistry. The findings showed that AK significantly attenuated scopolamine-induced cognitive impairment in mice. Increase of AChE activity caused by scopolamine was significantly attenuated by AK. Additionally, AK significantly recovered the phosphorylation of CREB and expression of BDNF reduced by scopolamine in the hippocampus. Taken together, these results provide experimental evidence that AK might be a useful agent in preventing deficit of learning and memory caused by AD and aging.
Brännlund, Annica; Strandh, Mattias; Nilsson, Karina
Education profoundly affects adult socioeconomic status, so it is important to ensure that all children have the capability and opportunity to achieve educational goals. The study aimed to examine the relationship between mental-health during adolescence and upper secondary school completion and grades, which has received comparatively little research attention to date. Longitudinal administrative and registered data were used to analyse the relationship between school achievement and prescriptions of psycholeptic and psycho-analeptic drugs. The sample consisted of all children born in Sweden in 1990 (n = 109 223), who were followed from birth to age 20. Logistic and OLS regressions were performed separately for boys and girls, controlling for birth health and family characteristics. A negative relationship between mental-health problems and educational outcomes was found; this result was almost independent of the controls. Only minor differences between the sexes were detected. Poor mental-health during childhood correlated negatively with educational attainment. Given the strong link between educational success and adult life, more resources are needed to support children with mental-health problems.
Naftalin, Richard J; Cunningham, Philip; Afzal-Ahmed, Iram
1 Nootropic drugs increase glucose uptake into anaesthetised brain and into Alzheimer's diseased brain. Thyrotropin-releasing hormone, TRH, which has a chemical structure similar to nootropics increases cerebellar uptake of glucose in murine rolling ataxia. This paper shows that nootropic drugs like piracetam (2-oxo 1 pyrrolidine acetamide) and levetiracetam and neuropeptides like TRH antagonise the inhibition of glucose transport by barbiturates, diazepam, melatonin and endogenous neuropeptide galanin in human erythrocytes in vitro. 2 The potencies of nootropic drugs in opposing scopolamine-induced memory loss correlate with their potencies in antagonising pentobarbital inhibition of erythrocyte glucose transport in vitro (Paniracetam and levetiracetam, while antagonising pentobarbital action, also inhibit glucose transport. Analeptics like bemigride and methamphetamine are more potent inhibitors of glucose transport than antagonists of hypnotic action on glucose transport. 4 There are similarities between amino-acid sequences in human glucose transport protein isoform 1 (GLUT1) and the benzodiazepine-binding domains of GABAA (gamma amino butyric acid) receptor subunits. Mapped on a 3D template of GLUT1, these homologies suggest that the site of diazepam and piracetam interaction is a pocket outside the central hydrophilic pore region. 5 Nootropic pyrrolidone antagonism of hypnotic drug inhibition of glucose transport in vitro may be an analogue of TRH antagonism of galanin-induced narcosis.
Full Text Available The cashew stem girdler, Analeptes trifasciata , is a major insect pest of cashew in Nigeria causing economic damage in cashew plantations even at low density. In this study, newly emerged adults of A. trifasciata reared from field-infested cashew stems were collected from the rearing cages, sexed, and dissected to reveal the internal structures of the insects. The gut was excised and separated into the foregut, midgut, and hindgut. The dissected gut compartments were blotted dry by sandwiching in sterile Whatman No. 1 (150 mm filter paper for a minute. The inoculated gut parts showed the presence of eight fungi flora, namely, Aspergillus repens, Trichoderma spp., Fusarium verticillioides, Lasiodiplodia theobromae , yeast, Aspergillus niger, Fusarium spp., and Rhizopus stolonifer . The frequencies of occurrence of bacteria in the gut compartments of A. trifasciata were Enterobacter spp.: 83.33%; Escherichia coli and Streptococcus spp.: 55.56% each; Staphylococcus spp.: 44.44%; Klebsiella pneumonia : 50% and Salmonella shigella : 11.11%, while each of Serratia marceascea, Pseudomonas spp., and Micrococcus lutea had 5.56% occurrence. The occurrence of mycoflora and microbiota species varied in the gut compartments of A. trifasciata , indicating the role of these microorganisms in metabolic and other bioprocesses of A. trifasciata during digestion and synthesis of complex food substances from the cashew stem substrate. This study would provide basic information for enzymatic studies of A. trifasciata with a view to developing an integrated pest management (IPM protocol for managing the pest in cashew plantations.
Mikhailov, V. P.; Deulin, E. A.
The patented linear motion feedthrough is based on elastic thin rubber walls usage being reinforced with analeptic string fixed in the middle part of the walls. The pneumatic or hydro actuators create linear movement of stock. The length of this movement is two times more the rubber wall length. This flexible wall is a sealing element of feedthrough. The main advantage of device is negligible resistance force that is less then mentioned one in sealing bellows that leads to positioning error decreasing. Nevertheless, the thin wall rubber sealing element (TRE) of the feedthrough is the main unreliable element that was the reason of this element longevity research. The theory and experimental results help to create equation for TRE longevity calculation under vacuum or extra high pressure difference action. The equation was used for TRE longevity determination for hydraulic or vacuum equipment realization also as it helps for gas flow being leaking through the cracks in thin walls of rubber sealing element of linear motion feedthrough calculation.
Mucke, Hermann A M
Among the psychedelic drugs that enjoyed a period of popularity in psychiatric research during the 1950s and 1960s, lysergic acid diethylamide (LSD) is the most prominent one. Psychiatrists of that time had seen LSD not only as a tool for psychotherapy but also as a potential therapeutic for anxiety, depression, alcohol abuse, autism, and even schizophrenia. When it became a quasi-religious epitome of the Hippie counterculture in the mid 1960s, and cases of what we now call hallucinogen persisting perception disorder and acute psychotic "flashbacks" mounted, authorities moved to make LSD illegal. Although research was never actually forbidden, the field almost completely dried out until the early 2010s. Using today's tools of molecular pharmacology, functional imaging, and neuronal network theory, neuropsychiatry is now resurrecting LSD research-with implications that leave us with many medical and ethical questions. Few people are aware that this is a repurposed compound, originally developed in an effort to synthesize a new analeptic. On top of all potential LSD might have in psychiatry, it also serves as a reminder of the unexpected potential that discarded early-stage compounds can have.
Naftalin, Richard J; Cunningham, Philip; Afzal-Ahmed, Iram
Nootropic drugs increase glucose uptake into anaesthetised brain and into Alzheimer's diseased brain. Thyrotropin-releasing hormone, TRH, which has a chemical structure similar to nootropics increases cerebellar uptake of glucose in murine rolling ataxia. This paper shows that nootropic drugs like piracetam (2-oxo 1 pyrrolidine acetamide) and levetiracetam and neuropeptides like TRH antagonise the inhibition of glucose transport by barbiturates, diazepam, melatonin and endogenous neuropeptide galanin in human erythrocytes in vitro. The potencies of nootropic drugs in opposing scopolamine-induced memory loss correlate with their potencies in antagonising pentobarbital inhibition of erythrocyte glucose transport in vitro (PPiracetam and TRH have no direct effects on net glucose transport, but competitively antagonise hypnotic drug inhibition of glucose transport. Other nootropics, like aniracetam and levetiracetam, while antagonising pentobarbital action, also inhibit glucose transport. Analeptics like bemigride and methamphetamine are more potent inhibitors of glucose transport than antagonists of hypnotic action on glucose transport. There are similarities between amino-acid sequences in human glucose transport protein isoform 1 (GLUT1) and the benzodiazepine-binding domains of GABAA (gamma amino butyric acid) receptor subunits. Mapped on a 3D template of GLUT1, these homologies suggest that the site of diazepam and piracetam interaction is a pocket outside the central hydrophilic pore region. Nootropic pyrrolidone antagonism of hypnotic drug inhibition of glucose transport in vitro may be an analogue of TRH antagonism of galanin-induced narcosis. PMID:15148255
Meena, Chhuttan L; Ingole, Shubdha; Rajpoot, Satyendra; Thakur, Avinash; Nandeker, Prajwal P; Sangamwar, Abhay T; Sharma, Shyam S; Jain, Rahul
TRH-like peptides were synthesized in which the critical N -terminus residue L-pGlu was replaced with various heteroaromatic rings, and the central residue histidine with 1-alkyl-L-histidines. All synthesized TRH-like peptides were evaluated in vitro as agonists in HEK mTRH-R1 and HEK mTRH-R2 cell lines, an expressing receptor binding assay (IC 50 ), and cell signaling assay (EC 50 ). The analeptic potential of the synthesized peptides was evaluated in vivo by using the antagonism of a pentobarbital-induced sleeping time. The peptides 6a , 6c and 6e were found to activate TRH-R2 with potencies (EC 50 ) of 0.002 μM, 0.28 μM and 0.049 μM , respectively. In contrast, for signaling activation of TRH-R1, the same peptides required higher concentration of 0.414 μM, 50 μM and 19.1 μM, respectively in the FLIPR assay. The results showed that these peptides were 207, 178 and 389-fold selective towards TRH-R2 receptor subtype. In the antagonism of a pentobarbital-induced sleeping time assay, peptide 6c showed a 58.5% reduction in sleeping time. The peptide 6c exhibited high stability in rat blood plasma, a superior effect on the scopolamine-induced cognition impairment mice model, safe effects on the cardiovascular system, and general behavior using a functional observation battery (FOB).
Full Text Available In broad biological terms, neurosteroids can be defined as a class of endogenous steroids synthesized in the brain or in peripheral steroidogenic tissues having potent and relatively selective activity on brain gamma-aminobutyric acid A (GABAA receptors. In this regard, the most important neurosteroids are allopregnanolone and allotetrahydrodeoxycorticosterone (allo THDOC. These α-reduced derivatives of pregnenolone and progesterone act as positive allosteric modulators of GABAA receptors. As such, they potentiate the inhibitory action of GABA on GABAA receptors and produce a wide spectrum of behavioral actions ranging from anxiolytic, anticonvulsive, sedative, hypnotic, amnestic (loss of memory, myorelaxant, and anesthetic effects. Sulfated derivatives of pregnenolone and dehydroepiandrosterone ,pregnenolone sulfate (PS and dehydroepianddrosterone sulfate (DHEAS, are also very important neurosteroids. In contrast to allopregnolone and alloTHDOC, PS and DHEAS induce excitatory effect on neurons because they facilitate the block of GABAA receptors. The spectrum of behavioral effects of PS and DHEAS consists of analeptic, anxiogenic, proconvulsive, and anamnestic (cognitive enhancing. The purpose of this review paper is to analyze recent research in the field of neurosteroids and neurosteroid-based drugs with emphasis on interaction of neurosteroids with brain GABAA receptors. This article also provides an overview of neurosteroids-based strategies for the development of innovative therapeutic approaches. GABAA receptor modulating steroids (GAMS, GABAA receptor modulating steroid antagonists (GAMSA, and translocator protein (TSPO activators are examples of innovative therapeutic approaches in treating clinically important neurological and psychiatric diseases. Consequently, the therapeutic potential of GAMS, GAMSA, and TSPO activators will be briefly evaluated.
Full Text Available The modern constitutive equations of the rheology of analeptic media and of the polarization in dielectric media are discussed in the time and frequency domains. It is seen that the most appropriate form of the constitutive equations of these media is based on the convolution of the stress and strain, and of the electric field and induction respectively, with appropriate functions representing the memory of the medium to previous stress or induction. The most successful memory forma]ism in representing the observed phenomena is that of the derivative of fractional order which allows a variety of problems to be solved by means of the Laplace Trans- form. The consequent index of refraction, generally, is a set valued function which implies that a monochromatic wave generated in the medium is split into a set of waves with the same frequency but different wavelength which interfere and have a quasi periodically varying amplitude. The eigenfunctions of these media, associated to the ordinarily used principal values of the index of retraction, are split and so are the tree modes. The fatigue of anelastic media is studied using the new constitutive equations containing fractional derivatives; a phenomenological method is introduced to compute the number of cycles which gives fatigue for a strain or stress with given amplitude and frequency. The number of cycles which may cause fatigue is proportional to the amplitude and frequency of the applied strain or stress, or inversely proportional to the rate of stress or strain. A criterion is also established to see whether an applied cyclic stress or strain may cause fatigue. This criterion is tested with experimental data on steel and rocks verifying that, in general, it is consistent with the data although thc data are not always in the linear range. It is tentatively seen that fatigue docs not seem one of the causes of the release of the elastic energy stored in the Earth.
A. S. Gotsulya
types of biological activity. Diuretic and analeptic activities dominate among the most likely types of that predicted activities for all 13 compounds.
K. V. Аleksandrova
Full Text Available Introduction Nowadays, research of novel biological active compounds with low toxicity, are carried out among different classes of organic compounds of natural and synthetic genesis. One of the main ways of these studies is search of water-soluble compounds – convenient objects for pharmacological researches. In recent years researchers paid attention to xanthine derivatives, because of their high variativity of possible chemical modification and ability to form different salts with wide spectrum of biological action. Thus, among water-soluble xanthine derivatives were found compounds with pronounced antioxidant, diuretic and analeptic properties. Primary methods of obtaining water-soluble xanthine derivatives are direct interaction of bases with xanthine molecule or insertion basic or acidic residues in positions 7 or 8 of xanthine bicycle. According from the above, search of biologically active compounds among water-soluble substituted xanthines is prospective and actual. The aim of the study was development of synthetic ways of obtaining novel water-soluble derivatives of 3-benzyl-8-methylxanthine and studying their physical and chemical properties. Material and methods Melting points of obtained compounds were determined by capillary method on PTP (M device. ІR-spectra of synthesized compounds were recorded on the Bruker Alpha device (company «Bruker» – Germany on 4000-400 sm-1 with using console ATR (direct insertion of compound. 1Н NMR-spectra were recorded on the Varian Mercury VX-200 device (company «Varian» – USA solvent – (DMSO-d6, internal standart – ТМС. Elemental analysis was made on Elementar Vario L cube device. Chromatoraphic studies were made on the plates Sorbfil-AFV-UV (company «Sobrpolimer» –Russia. Systhems for chromatography: «acetone-propanol-2» in ratio 2:3, «propanol-2-benzene» in ratio 10:1 and exersized in UV-light in wave 200-300 nm. Results and discussion We developed methodic of synthesis
-operation from the small but prosperous pharmaceutical company "Kaštel" in Zagreb. On behalf of the agreement, Prelog and his department obtained funds to fit up the laboratory and to start very prosperous research in the synthesis and studies of pharmaceutically interesting compounds. With his assistants, students and other collaborators, Prelog started research of cinchona bark alkaloids, preferentially oriented to the synthesis of quinine. For example, Prelog's method of double intramolecular alkylation to synthetize the quinuclidine moiety of quinine was patented by "Kaštel". With R. Seiwerth he developed the first useful synthesis of adamantane. Prelog's group started research in the field of sulphonamides and commercial success of "Streptazole" stimulated the development of the research laboratories within "Kaštel". The collaboration in the research continued in fields of other chemotherapeutics, analeptics, spasmolitics, barbiturates etc. Within the period 1935-1941, Prelog published 48 scientific papers and 8 patents. In less than seven years, his results enormously influenced the entire organic chemistry in Zagreb till nowadays. Under the confused and uncertain circumstances caused by the beginning of World War II, Prelog left Zagreb in 1941 and continued his extraordinary scientific career at the ETH in Zürich.During the war (1942-1945 the tuition and the Department were run by Dr. Rativoj Seiwerth, former collaborator and first assistant to V. Prelog. In almost unbelievable conditions, the young assistant, then assistant professor (since January 1943, R. Seiwerth fully succeeded in continuing most activities founded by Professor Prelog. After the war (1945, R. Seiwerth was forced to resign. Nevertheless, soon after R. Seiwerth continued his research work, firstly in the Institute for Industrial Research in Zagreb (1946-1952, and later in the Research Institute of "Pliva" in Zagreb. He retired in 1980.In post-war conditions (1945/46, the activity of the Technical