8 results on '"Lavian G"'
Search Results
2. Modification of alpha-2 presynaptic receptor activity and catecholamine release following chronic MAO inhibition
- Author
-
Finberg, J. P. M., Ari, G., Lavian, G., Hovevey-Sion, D., Riederer, Peter, editor, and Youdim, Moussa B. H., editor
- Published
- 1990
- Full Text
- View/download PDF
3. THE ADVENT OF NEW GENERATION OF MONOAMINE OXIDASE INHIBITOR ANTIDEPRESSANTS
- Author
-
Lavian, G., primary, Finberg, J. P.M., additional, and Youdim, M. B.H., additional
- Published
- 1992
- Full Text
- View/download PDF
4. Novel Dual Inhibitors of AChE and MAO Derived from Hydroxy Aminoindan and Phenethylamine as Potential Treatment for Alzheimer's Disease
- Author
-
Sterling, J., Herzig, Y., Goren, T., Finkelstein, N., Lerner, D., Goldenberg, W., Miskolczi, I., Molnar, S., Rantal, F., Tamas, T., Toth, G., Zagyva, A., Zekany, A., Lavian, G., Gross, A., Friedman, R., Razin, M., Huang, W., Krais, B., Chorev, M., Youdim, M. B., and Weinstock, M.
- Abstract
Carbamate derivatives of N-propargylaminoindans (Series I) and N-propargylphenethylamines (Series II) were synthesized via multistep procedures from the corresponding hydroxy precursors. The respective rasagiline- and selegiline-related series were designed to combine inhibitory activities of both acetylcholine esterase (AChE) and monoamine oxidase (MAO) by virtue of their carbamoyl and propargylamine pharmacophores. Each compound was tested for these activities in vitro in order to find molecules with similar potencies against each enzyme. Compounds with such dual AChE and MAO inhibitory activities are expected to have potential for the treatment of Alzheimer's disease. The observed SAR also offers insight into the requirements of the active sites on these enzymes. A carbamate moiety was found to be essential for AChE inhibition, which was absent in the corresponding hydroxy precursors. The propargyl group caused 2−70-fold decrease in AChE inhibitory activity (depending on the position of the carbamoyl group) of Series I, but had little or no effect in Series II. Thus, the 6- and 7-carbamyloxyphenyls in Series I were either equipotent to, or slightly (2- to 5-fold) less active as AChE inhibitors than, the corresponding compounds in Series II, while the 4-carbamyloxyphenyls were more potent. The presence of the carbamate moiety in 6- and 7-carbamyloxyphenyls of Series I, considerably decreased MAO-A and -B inhibitory activity, compared to that of the parent hydroxy analogues, while the opposite was true for Series II. Thus, the 6- and 7-carbamyloxyphenyls in Series I were 2−3 orders of magnitude weaker MAO inhibitors while the 4- carbamyloxyphenyls were equipotent with the corresponding compounds in Series II. In both series, N-methylation of the propargylamine enhanced the MAO (A and B equally) inhibitory activities and decreased the AChE inhibitory activity. Two candidates belonging to the indan and tetralin ring systems (
24c ,27b ) and one phenethylamine (53d) were identified as possible leads for further development based on the following criteria: (a) comparable AChE and MAO-B inhibitory activities, (b) good to moderate AChE inhibitory activity, and (c) lack of strong MAO-A selectivity. However, it is likely that these compounds will be metabolized to the corresponding phenols, with inhibitory activities against AChE and/or MAO-A or -B, different from those of the parent carbamates. Thus, the apparent enzyme inhibition will be a result of the combined inhibition of all of these individual metabolites. The results of our ongoing in vivo screening programs will be published elsewhere.- Published
- 2002
- Full Text
- View/download PDF
5. Global COVID-19 lockdown highlights humans as both threats and custodians of the environment.
- Author
-
Bates AE, Primack RB, Biggar BS, Bird TJ, Clinton ME, Command RJ, Richards C, Shellard M, Geraldi NR, Vergara V, Acevedo-Charry O, Colón-Piñeiro Z, Ocampo D, Ocampo-Peñuela N, Sánchez-Clavijo LM, Adamescu CM, Cheval S, Racoviceanu T, Adams MD, Kalisa E, Kuuire VZ, Aditya V, Anderwald P, Wiesmann S, Wipf S, Badihi G, Henderson MG, Loetscher H, Baerenfaller K, Benedetti-Cecchi L, Bulleri F, Bertocci I, Maggi E, Rindi L, Ravaglioli C, Boerder K, Bonnel J, Mathias D, Archambault P, Chauvaud L, Braun CD, Thorrold SR, Brownscombe JW, Midwood JD, Boston CM, Brooks JL, Cooke SJ, China V, Roll U, Belmaker J, Zvuloni A, Coll M, Ortega M, Connors B, Lacko L, Jayathilake DRM, Costello MJ, Crimmins TM, Barnett L, Denny EG, Gerst KL, Marsh RL, Posthumus EE, Rodriguez R, Rosemartin A, Schaffer SN, Switzer JR, Wong K, Cunningham SJ, Sumasgutner P, Amar A, Thomson RL, Stofberg M, Hofmeyr S, Suri J, Stuart-Smith RD, Day PB, Edgar GJ, Cooper AT, De Leo FC, Garner G, Des Brisay PG, Schrimpf MB, Koper N, Diamond MS, Dwyer RG, Baker CJ, Franklin CE, Efrat R, Berger-Tal O, Hatzofe O, Eguíluz VM, Rodríguez JP, Fernández-Gracia J, Elustondo D, Calatayud V, English PA, Archer SK, Dudas SE, Haggarty DR, Gallagher AJ, Shea BD, Shipley ON, Gilby BL, Ballantyne J, Olds AD, Henderson CJ, Schlacher TA, Halliday WD, Brown NAW, Woods MB, Balshine S, Juanes F, Rider MJ, Albano PS, Hammerschlag N, Hays GC, Esteban N, Pan Y, He G, Tanaka T, Hensel MJS, Orth RJ, Patrick CJ, Hentati-Sundberg J, Olsson O, Hessing-Lewis ML, Higgs ND, Hindell MA, McMahon CR, Harcourt R, Guinet C, Hirsch SE, Perrault JR, Hoover SR, Reilly JD, Hobaiter C, Gruber T, Huveneers C, Udyawer V, Clarke TM, Kroesen LP, Hik DS, Cherry SG, Del Bel Belluz JA, Jackson JM, Lai S, Lamb CT, LeClair GD, Parmelee JR, Chatfield MWH, Frederick CA, Lee S, Park H, Choi J, LeTourneux F, Grandmont T, de-Broin FD, Bêty J, Gauthier G, Legagneux P, Lewis JS, Haight J, Liu Z, Lyon JP, Hale R, D'Silva D, MacGregor-Fors I, Arbeláez-Cortés E, Estela FA, Sánchez-Sarria CE, García-Arroyo M, Aguirre-Samboní GK, Franco Morales JC, Malamud S, Gavriel T, Buba Y, Salingré S, Lazarus M, Yahel R, Ari YB, Miller E, Sade R, Lavian G, Birman Z, Gury M, Baz H, Baskin I, Penn A, Dolev A, Licht O, Karkom T, Davidzon S, Berkovitch A, Yaakov O, Manenti R, Mori E, Ficetola GF, Lunghi E, March D, Godley BJ, Martin C, Mihaly SF, Barclay DR, Thomson DJM, Dewey R, Bedard J, Miller A, Dearden A, Chapman J, Dares L, Borden L, Gibbs D, Schultz J, Sergeenko N, Francis F, Weltman A, Moity N, Ramírez-González J, Mucientes G, Alonso-Fernández A, Namir I, Bar-Massada A, Chen R, Yedvab S, Okey TA, Oppel S, Arkumarev V, Bakari S, Dobrev V, Saravia-Mullin V, Bounas A, Dobrev D, Kret E, Mengistu S, Pourchier C, Ruffo A, Tesfaye M, Wondafrash M, Nikolov SC, Palmer C, Sileci L, Rex PT, Lowe CG, Peters F, Pine MK, Radford CA, Wilson L, McWhinnie L, Scuderi A, Jeffs AG, Prudic KL, Larrivée M, McFarland KP, Solis R, Hutchinson RA, Queiroz N, Furtado MA, Sims DW, Southall E, Quesada-Rodriguez CA, Diaz-Orozco JP, Rodgers KS, Severino SJL, Graham AT, Stefanak MP, Madin EMP, Ryan PG, Maclean K, Weideman EA, Şekercioğlu ÇH, Kittelberger KD, Kusak J, Seminoff JA, Hanna ME, Shimada T, Meekan MG, Smith MKS, Mokhatla MM, Soh MCK, Pang RYT, Ng BXK, Lee BPY, Loo AHB, Er KBH, Souza GBG, Stallings CD, Curtis JS, Faletti ME, Peake JA, Schram MJ, Wall KR, Terry C, Rothendler M, Zipf L, Ulloa JS, Hernández-Palma A, Gómez-Valencia B, Cruz-Rodríguez C, Herrera-Varón Y, Roa M, Rodríguez-Buriticá S, Ochoa-Quintero JM, Vardi R, Vázquez V, Requena-Mesa C, Warrington MH, Taylor ME, Woodall LC, Stefanoudis PV, Zhang X, Yang Q, Zukerman Y, Sigal Z, Ayali A, Clua EEG, Carzon P, Seguine C, Corradini A, Pedrotti L, Foley CM, Gagnon CA, Panipakoochoo E, Milanes CB, Botero CM, Velázquez YR, Milchakova NA, Morley SA, Martin SM, Nanni V, Otero T, Wakeling J, Abarro S, Piou C, Sobral AFL, Soto EH, Weigel EG, Bernal-Ibáñez A, Gestoso I, Cacabelos E, Cagnacci F, Devassy RP, Loretto MC, Moraga P, Rutz C, and Duarte CM
- Abstract
The global lockdown to mitigate COVID-19 pandemic health risks has altered human interactions with nature. Here, we report immediate impacts of changes in human activities on wildlife and environmental threats during the early lockdown months of 2020, based on 877 qualitative reports and 332 quantitative assessments from 89 different studies. Hundreds of reports of unusual species observations from around the world suggest that animals quickly responded to the reductions in human presence. However, negative effects of lockdown on conservation also emerged, as confinement resulted in some park officials being unable to perform conservation, restoration and enforcement tasks, resulting in local increases in illegal activities such as hunting. Overall, there is a complex mixture of positive and negative effects of the pandemic lockdown on nature, all of which have the potential to lead to cascading responses which in turn impact wildlife and nature conservation. While the net effect of the lockdown will need to be assessed over years as data becomes available and persistent effects emerge, immediate responses were detected across the world. Thus, initial qualitative and quantitative data arising from this serendipitous global quasi-experimental perturbation highlights the dual role that humans play in threatening and protecting species and ecosystems. Pathways to favorably tilt this delicate balance include reducing impacts and increasing conservation effectiveness., Competing Interests: Authors declare no competing interests., (© 2021 Published by Elsevier Ltd.)
- Published
- 2021
- Full Text
- View/download PDF
6. In vivo extracellular recording of sympathetic ganglion activity in a chronic animal model.
- Author
-
Lavian G, Kopelman D, Shenhav A, Konyukhov E, Gardi U, Zaretzky A, Shofti R, Finberg JP, and Hashmonai M
- Subjects
- Animals, Electrocardiography, Electronic Data Processing, Electrophysiology instrumentation, Equipment Design, Respiratory Physiological Phenomena, Software, Stellate Ganglion surgery, Time Factors, Dogs, Electrodes, Implanted, Extracellular Fluid physiology, Ganglia, Sympathetic physiology, Models, Animal, Stellate Ganglion physiology
- Abstract
Surgery of the sympathetic system is performed for a variety of indications, hyperhidrosis being a major one. Despite excellent results, sympathectomy for hyperhidrosis bears a number of sequels, some of which may be devastating. Several surgical methods, empirically advocated to alleviate these problems, have only limited success. Chronic in vivo recording of the electrical activity from sympathetic ganglia may assist in understanding and clarifying complex problems of sympathetic surgery; however, no suitable method has been reported. An electrode device developed by our group was implanted on the stellate ganglion, in a chronic animal model (dog). The signals obtained were amplified, filtered, and transmitted via an A/D interface to be acquired and saved on a computer, using special software which we developed. Our method enabled the separate recording of neuroelectrical signals, ECG, and respiration waves. An additional software program, also developed by our group, was used to analyze the data. This chronic animal model allows investigation of surgical and pharmacological manipulations of the sympathetic system.
- Published
- 2003
- Full Text
- View/download PDF
7. The advent of a new generation of monoamine oxidase inhibitor antidepressants: pharmacologic studies with moclobemide and brofaromine.
- Author
-
Lavian G, Finberg JP, and Youdim MB
- Subjects
- Animals, Blood Pressure drug effects, Clorgyline pharmacology, Desipramine pharmacology, Heart Rate drug effects, Kidney drug effects, Kidney innervation, Moclobemide, Rats, Rats, Sprague-Dawley, Sympathetic Nervous System drug effects, Antidepressive Agents pharmacology, Benzamides pharmacology, Monoamine Oxidase Inhibitors pharmacology, Piperidines pharmacology
- Abstract
Severe side effects such as hepatotoxicity and potentiation of the sympathomimetic action of tyramine ("the cheese effect") caused the withdrawal of nonselective irreversible monoamine oxidase (MAO) inhibitors from use in psychiatric therapy. The development of selective irreversible inhibitors for MAO type A did not eliminate cardiovascular side effects such as "the cheese effect" or, conversely, the hypotensive effect of these drugs. To overcome at least "the cheese effect," selective reversible MAO-A inhibitor antidepressants such as moclobemide and brofaromine have been developed. Being reversibly bound to MAO, these drugs may be displaced from their binding site in the intestine by ingested, indirectly sympathomimetic amines such as tyramine, thus avoiding the initiation of the hypertensive crises. Using a rat renal nerve preparation, we have demonstrated that acute administration of either moclobemide or brofaromine (10 mg/kg) does not cause a decrease in blood pressure or a significant reduction in sympathetic renal nerve activity. These data contrast with those obtained with clorgyline or desipramine. The results indicate that moclobemide and brofaromine may be devoid of a hypotensive effect, including orthostatic hypotension.
- Published
- 1993
8. Inhibition of sympathetic nerve activity by acute administration of the tricyclic antidepressant desipramine.
- Author
-
Lavian G, Di Bona G, and Finberg JP
- Subjects
- Animals, Blood Pressure drug effects, Drug Interactions, Heart Rate drug effects, Kidney innervation, Male, Prazosin pharmacology, Rats, Rats, Inbred Strains, Receptors, Adrenergic, alpha drug effects, Receptors, Adrenergic, alpha physiology, Splanchnic Nerves drug effects, Yohimbine pharmacology, Desipramine pharmacology, Sympathetic Nervous System drug effects
- Abstract
In rats anesthetized with pentobarbital/chloral hydrate, the i.v. injection of desipramine (0.3 mg/kg) caused a rapid fall in mean arterial blood pressure accompanied by a reduction in efferent renal nerve integrated activity. A similar reduction in electrical activity was seen in the preganglionic splanchnic nerve. Pretreatment of the rats with yohimbine (0.3 mg/kg) increased renal nerve activity by 20%, and the decrease in blood pressure and renal nerve activity elicited by a subsequent dose of desipramine was blocked. I.v. injection of prazosin (0.05 mg/kg) caused a reduction in systemic blood pressure. The hypotensive effect of a subsequent dose of desipramine was largely blocked, whereas the fall in renal nerve activity was attenuated, but still present. The data are consistent with an action of desipramine to reduce central sympathetic tone by increasing the release of endogenous noradrenaline which acts on alpha 2-adrenoceptors at CNS sites controlling sympathetic activity. An additional involvement of central alpha 1-adrenoceptors cannot be ruled out.
- Published
- 1991
- Full Text
- View/download PDF
Catalog
Discovery Service for Jio Institute Digital Library
For full access to our library's resources, please sign in.