DOCSLIB.ORG

Cap11 Adrenolitico

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Cap11 Adrenolitico SECCION II: CAPITULO 11 DROGAS SIMPATICOLITICAS O ADRENOLITICAS Malgor - Valsecia Como anteriormente se mencionara, el siste- Son un grupo de drogas que actúan en la ter- ma Simpático o Adrenérgico cumple num ero- minación adrenérgica, a nivel axoplasmático o sas e importantísimas funciones biológicas sobre receptores presinápticos alfa2, salvo indispensables para la modulación y regula- estos últimos agentes, los adrenolíticos presi- ción de organismos y sistemas que son vitales nápticos tienen ac tualmente un uso clínico para el mantenimiento de una vida normal. terapéutico limitado. CLASIFICACIÓN DE DROGAS SIMPATICO- Las drogas simpaticolíticas o adrenolíticas LÍTICAS son un grupo numeroso de fármacos que in- terfieren con las funciones del sistema simpá- I.SIMPATICOLITICOS PRESINAPTICOS. tico, las mismas actúan básicamente de dos maneras diferentes: a.Axoplasmáticos: I- Inhiben la liberación de las catecolaminas en *Reserpina (Serpasol) la terminación adrenérgica, actuando a nivel Deserpidina presináptico y Rescinamina Guanetidina (Ismelin) II- Bloquean los receptores adrenérgicos en Batanidina las células efectoras a nivel postsináptico. Debrisoquina (Declinax,Sintiapress) Bretilio Las primeras son drogas simpaticolíticas que IMAO:Pargilina (Eutonil;Tranilcipromina (Parna- inhiben la síntesis de catecolaminas. Interfie- te) ren con los proceso de depósito y liberación de las mismas. Algunas actúan a nivel central reduciendo la activi dad simpática cerebral. b.Agonistas alfa 2:(Adrenoliticas de accion Este grupo de fármacos son los llam ados central) Simpaticolíticos presinápticos. Los simpati- colíticos postsinápticos son los bloqueantes Clonidina (Catapresan) de los receptores alfa y beta adrenérgicos. *Alfa-metil-dopa (Aldomet) Guanabenz (Rexitene) Todos estos agentes adrenolíticos son drogas Guanfacina (Estulic,Hipertensal) de gran utilidad terapéutica, capaces de gene- rar una solución farmacológica a numerosos padecimientos clínicos, principalmente en el II.SIMPATICOLITICOS POSTSINAPTICOS área cardiovascular. a.BLOQUEADIRES ALFA 1 ADRENERGI- COS: I. FARMACOS SIMPATICOLITICOS PRESI- NAPTICOS. *Prazosin (Minipres) Trimazosin Terazosin 117 Doxazosin no para convertirlo en 5-hidroxitriptamina o serotonina, etc. b.BLOQUEADORES ALFA 2 ADRENERGI- COS La metildopa es una droga de un uso extensivo en terapéutica antihipertensiva, incorporada Yohimbina para tal fin en la década del 60. c.BLOQUEADORES ALFA TOTALES Mecanismo de acción: La alfa -metildopa, se (alfa 1 y alfa 2) distribuye am pliamente, sufre el proceso de racaptación neuronal y es biotransformada por Fentolamina (Regitina) la DOPA-decarboxilasa a alfa-metil-dopamina. Fenoxibenzamina Este precursor ingresa como si fuera dopami- Alcaloides dihidrogenados del na al gránulo adrenérgico y allí es transfor- Ergot,dihidroergotoxina (Hidergina) mado en alfa-metil-noradrenalina por la enzima dopamino-ß-hidroxilasa (DBH) La metilnora- drenalina liberada en el.proceso exocitósico es b.BLOQUEADORES BETA ADRENERGICOS un efectivo agonista de los receptores alfa2 presinápticos, que cuando se activan inducen Bloqueadores beta 1-2: un mecanismo de autorregulación negativo, inhibiendo la liberación de noradrenalina con el *Propanolol (Inderal) consiguiente efecto simpaticolítico. La metil- Timolol (Proflax) dopa actúa en el SNC a nivel del núcleo tracto Nadolol (Corgard) solitario y núcleo ambiguo, la respuesta sim- Pindolol (Visken) pática noradrenérgica refleja varios estímulos Sotalol (Betacardone) (barorreceptores por ejemplo), nace en dichos núcleos para alcanzar los centros de control Bloqueadores beta 1:(cardioselectivos) cardiovascular en el bulbo. La alfa-metilno- radrenalina, activando receptores alfa2, produ- *Atenolol (Prenormine) ce una inhibición simpática central y un efecto Metoprolol (Lopresor) antihipertensivo importante, entre otras accio- Acebutolol (Rodhiasectral) nes simpaticolíticas. Bloqueadores beta 2: Acciones farmacológicas: La metildopa re- duce la resistencia periférica y la presión arte- Butoxamine rial. No afecta significativamente la frecuencia Zinterol cardíaca, el volumen minuto y los reflejos va- somotores. Como interfiere con el funciona- Bloqueadores alfa y beta: miento del sistema simpático puede producir hipertensión ortostática. Labetalol (Labelol) La metildopa no afecta el flujo sanguíneo renal * AGENTES PROTOTIPOS. ni la filtración glomerular . Ocasiona sin em- bargo retención de Na+ e incrementa la prolac- tina plas mática. Este efecto ocurre porque la 1.Agonistas de los receptores alfa 2 presi- dopamina en el SNC produce una modulación nápti cos: o regulación inhibitoria de la secreción de pro- -Alfa-metil-dopa lactina. La metildopa origina por decarboxila- -Clonidina ción, la presencia de _-metildopamina en las -Guanfacina neuronas dopaminérgicas, que se libera como -Guanabenz un falso neurotransmisor y no desarrolla dicha acción inhibitoria. ALFA-METIL-DOPA: es un agonista análogo de la DOPA (dihidroxifenilalanina), inhibidor de Farmacocinética: Se absorbe principalmente la dopa-decarboxilasa o decarboxilasa de ami- por vía oral (50% de la dosis aproximadamen- noácidos aromáticos. Esta enzima decarboxila te). El efec to hipotensor máximo se desarrolla la DOPA para convertirla en dopamina. Ta m- luego de 4-6 horas. Se liga escasamente a bién decarboxila otra aminas como el triptofa- proteínas plasmáticas y atraviesa la barrera hematoencefálica. La metildopa pasa a través 118 de la placenta y se excreta en la leche mater- Estas reacciones son irreversibles si el trata- na. La metildopa se metaboliza formando con- miento se suspende rápidamente. jugados (metildopa- mono-O-sulfato) en el hígado e intestino, que parecen ser activos. Se eliminan por filtración glomerular en forma inal- Otros efectos adversos: náuseas, vómitos y terada o por sus conjugados. Su vida media sequedad de boca, urticaria, eczema, hiper- plasmática es de 2 horas. queratosis, congestión nasal, pueden ocurrir con el uso crónico de metildopa. También Usos terapéuticos: La metildopa se usa para ginecomastia, galactorrea e hiperprolactine- el tratamiento de la hipertensión arterial mode- mia. Ocasionalmente puede observarse tam- rada o grave. Actualmente los inhibidores bién impotencia, signos de parkinsonismo y adrenérgicos de este tipo se utilizan en la 2ª depresión psíquica. etapa del tratamiento para pacientes que no responden a terapia con monodrogas. Es más Los pacientes que se encuentran con trata- efectiva generalmente, si se la administra con- miento crónico de metildopa deben controlarse juntamente con diuréticos tiazídicos. Puede la función hepática y las transaminasas cada usarse también la combinación con otras dro- 2-3 meses. gas. La metildopa es probablemente una de las drogas de mayor uso como anti - hipertensivo. Esta droga también es útil en el CLONIDINA, GUANABENZ, GUANFACINA. manejo de la hipertensión de la embarazada. Clonidina es un derivado imidazólico. Guanfa- cina y guanabenz son drogas químicamente Efectos adversos: relacionadas derivadas de la feni- lacetilguanidina. El agente de mayor uso es la SNC: el efecto adverso más común es la se- clonidina. Son drogas liposolubles que atra- dación, aunque con el uso prolongado tiende a viesan fácilmente la barrera hematoenc efálica. desaparecer por tolerancia. También se obser- vó disminución de la memoria y dificultad para concentrarse, astenia, cefalea, vértigo y debili- Mecanismos de acción: Al igual que la me- dad. tildopa estos agentes son agonistas a adre- nérgicos, que actúan a nivel central desenca- Aparato cardiovascular: La hipotensión or- denando un efecto simpaticolítico sobre los tostática aparece con frecuencia, acompañada centros vasomotores, hipotensión arterial y de bradicardia, si no se adminis tra junto con bradicardia. Con dosis altas o cuando se ad- un diurético puede observarse retención de ministran por vía i.v. pueden activar también Na+ y agua y edemas. Este efecto puede los receptores alfa2 postsinápticos del múscu- agravar una insuficiencia cardíaca. lo liso vascular, ocasionando vas oconstric ción y efecto hipertensivo, solo inicial, que poste- Efectos hematológicos: Luego de 6-12 me- riormente es seguido por el efecto hipotensor ses de tratamiento puede aparecer un test de más prolongado. Coombs positivo, que no indica necesidad imprescindible de suspender el tratamiento. Acciones farmacológicas: Son similares a la Raramente puede aparecer anemia hemolítica, alfa-metildopa: descenso de la presión sistóli- debiendo suspenderse la metildopa en este ca y diastólica, disminución del volumen minu- caso. También leucopenia (granulocitopenia) to y bradicardia. Este efecto también puede reversible. La anemia hemolítica puede apare- ser originado en un es tímulo parasimpático cer con más frecuencia en pacientes con defi- central. La clonidina puede desarrollar hipoten- ciencia genética de glucosa-6-fosfato deshi - sión ortostática por disminución del retorno drogenasa. venoso. El flujo sanguíneo renal y la filtración glomerular no se altera con estos agentes y Reacciones de hipersensibilidad y hepato- puede ocurrir retención de agua y sodio, por lo toxicidad: El tratamiento prolongado con me- que también en este caso es conveniente el tildopa puede producir fiebre y eosinofilia por uso conjunto de un diurético tiazídico. Los hipersensibilidad. Esta reacción puede acom- efectos antihipertensivos de los diuréticos pañarse con alteración de la función hepática, tiazídicos y los agonistas alfa2, son aditivos. incremento de fosfatasa alcalina y más rara- Lo mismo ocurre con la mayoría
Load more

Recommended publications
  • Modulation of Dialysate Levels of Dopamine, Noradrenaline
    Modulation of Dialysate Levels of Dopamine, Noradrenaline, and Serotonin (5-HT) in the Frontal Cortex of Freely-Moving Rats by (-)-Pindolol Alone and in Association with 5-HT Reuptake Inhibitors: Comparative Roles b of -Adrenergic, 5-HT1A, and 5-HT1B Receptors Alain Gobert, Ph.D. and Mark J. Millan, Ph.D. (-)-Pindolol, which possesses significant affinity for 5-HT1A, involved. (-)-Pindolol potentiated the increase in FCX levels b 5-HT1B, and 1/2-adrenergic receptors (AR)s, dose- of 5-HT elicited by the 5-HT reuptake inhibitors, fluoxetine dependently increased extracellular levels of dopamine and duloxetine, and also enhanced their ability to elevate (DA) and noradrenaline (NAD) versus 5-HT, in dialysates FCX levels of DA—though not of NAD. In contrast to of the frontal cortex (FCX), but not accumbens and (-)-pindolol, betaxolol and ICI118,551 did not affect the striatum, of freely-moving rats. In distinction, the actions of fluoxetine, whereas both WAY100,635 and b preferential 1-AR antagonist, betaxolol, and the SB224,289 potentiated the increase in levels of 5-HT—but b preferential 2-AR antagonist, ICI118,551, did not increase not DA or NAD levels—elicited by fluoxetine. In basal levels of DA, NAD, or 5-HT. Further, they both dose- conclusion, (-)-pindolol modulates, both alone and together dependently and markedly blunted the influence of with 5-HT reuptake inhibitors, dopaminergic, adrenergic, (-)-pindolol upon DA and NAD levels. The selective 5-HT1A and serotonergic transmission in the FCX via a complex b receptor antagonist, WAY100,635, slightly attenuated the pattern of actions at 1/2-ARs, 5-HT1A, and 5-HT1B (-)-pindolol-induced increase in DA and NAD levels, while receptors.
    [Show full text]
  • G Protein‐Coupled Receptors
    S.P.H. Alexander et al. The Concise Guide to PHARMACOLOGY 2019/20: G protein-coupled receptors. British Journal of Pharmacology (2019) 176, S21–S141 THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors Stephen PH Alexander1 , Arthur Christopoulos2 , Anthony P Davenport3 , Eamonn Kelly4, Alistair Mathie5 , John A Peters6 , Emma L Veale5 ,JaneFArmstrong7 , Elena Faccenda7 ,SimonDHarding7 ,AdamJPawson7 , Joanna L Sharman7 , Christopher Southan7 , Jamie A Davies7 and CGTP Collaborators 1School of Life Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK 2Monash Institute of Pharmaceutical Sciences and Department of Pharmacology, Monash University, Parkville, Victoria 3052, Australia 3Clinical Pharmacology Unit, University of Cambridge, Cambridge, CB2 0QQ, UK 4School of Physiology, Pharmacology and Neuroscience, University of Bristol, Bristol, BS8 1TD, UK 5Medway School of Pharmacy, The Universities of Greenwich and Kent at Medway, Anson Building, Central Avenue, Chatham Maritime, Chatham, Kent, ME4 4TB, UK 6Neuroscience Division, Medical Education Institute, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK 7Centre for Discovery Brain Sciences, University of Edinburgh, Edinburgh, EH8 9XD, UK Abstract The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website.
    [Show full text]
  • New Concepts in Pharmacological Efficacy at 7TM Receptors: IUPHAR
    British Journal of DOI:10.1111/j.1476-5381.2012.02223.x www.brjpharmacol.org BJP Pharmacology Dr Terry Kenakin, University of International Union of Basic North Carolina, Pharmacology, Chapel Hill, North Carolina, and Clinical Pharmacology United States, Phone: 919-962-7863, Fax: 919 966 7242 Review or 5640, [email protected] ---------------------------------------------------------------- Keywords receptor theory; agonism; New concepts in efficacy; drug discovery ---------------------------------------------------------------- Received pharmacological efficacy at 8 May 2012 Revised 3 August 2012 7TM receptors: IUPHAR Accepted Review 2 12 September 2012 This is the second in a series of reviews written by committees Terry Kenakin of experts of the Nomenclature Committee of the International Department of Pharmacology, University of North Carolina School of Medicine, Chapel Hill, NC, Union of Basic and Clinical USA Pharmacology (NC-IUPHAR). A listing of all articles in the series and the Nomenclature Reports from IUPHAR published in Pharmacological Reviews can be found at http://www. GuideToPharmacology.org. This website, created in a The present-day concept of drug efficacy has changed completely from its original collaboration between the British Pharmacological Society description as the property of agonists that causes tissue activation. The ability to (BPS) and the International visualize the multiple behaviours of seven transmembrane receptors has shown that Union of Basic and Clinical drugs can have many efficacies and also that the transduction of drug stimulus to Pharmacology (IUPHAR), various cellular stimulus–response cascades can be biased towards some but not all is intended to become a pathways. This latter effect leads to agonist ‘functional selectivity’, which can be “one-stop shop” source of favourable for the improvement of agonist therapeutics.
    [Show full text]
  • Customs Tariff - Schedule
    CUSTOMS TARIFF - SCHEDULE 99 - i Chapter 99 SPECIAL CLASSIFICATION PROVISIONS - COMMERCIAL Notes. 1. The provisions of this Chapter are not subject to the rule of specificity in General Interpretative Rule 3 (a). 2. Goods which may be classified under the provisions of Chapter 99, if also eligible for classification under the provisions of Chapter 98, shall be classified in Chapter 98. 3. Goods may be classified under a tariff item in this Chapter and be entitled to the Most-Favoured-Nation Tariff or a preferential tariff rate of customs duty under this Chapter that applies to those goods according to the tariff treatment applicable to their country of origin only after classification under a tariff item in Chapters 1 to 97 has been determined and the conditions of any Chapter 99 provision and any applicable regulations or orders in relation thereto have been met. 4. The words and expressions used in this Chapter have the same meaning as in Chapters 1 to 97. Issued January 1, 2019 99 - 1 CUSTOMS TARIFF - SCHEDULE Tariff Unit of MFN Applicable SS Description of Goods Item Meas. Tariff Preferential Tariffs 9901.00.00 Articles and materials for use in the manufacture or repair of the Free CCCT, LDCT, GPT, UST, following to be employed in commercial fishing or the commercial MT, MUST, CIAT, CT, harvesting of marine plants: CRT, IT, NT, SLT, PT, COLT, JT, PAT, HNT, Artificial bait; KRT, CEUT, UAT, CPTPT: Free Carapace measures; Cordage, fishing lines (including marlines), rope and twine, of a circumference not exceeding 38 mm; Devices for keeping nets open; Fish hooks; Fishing nets and netting; Jiggers; Line floats; Lobster traps; Lures; Marker buoys of any material excluding wood; Net floats; Scallop drag nets; Spat collectors and collector holders; Swivels.
    [Show full text]
  • Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
    20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0
    [Show full text]
  • Stembook 2018.Pdf
    The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances FORMER DOCUMENT NUMBER: WHO/PHARM S/NOM 15 WHO/EMP/RHT/TSN/2018.1 © World Health Organization 2018 Some rights reserved. This work is available under the Creative Commons Attribution-NonCommercial-ShareAlike 3.0 IGO licence (CC BY-NC-SA 3.0 IGO; https://creativecommons.org/licenses/by-nc-sa/3.0/igo). Under the terms of this licence, you may copy, redistribute and adapt the work for non-commercial purposes, provided the work is appropriately cited, as indicated below. In any use of this work, there should be no suggestion that WHO endorses any specific organization, products or services. The use of the WHO logo is not permitted. If you adapt the work, then you must license your work under the same or equivalent Creative Commons licence. If you create a translation of this work, you should add the following disclaimer along with the suggested citation: “This translation was not created by the World Health Organization (WHO). WHO is not responsible for the content or accuracy of this translation. The original English edition shall be the binding and authentic edition”. Any mediation relating to disputes arising under the licence shall be conducted in accordance with the mediation rules of the World Intellectual Property Organization. Suggested citation. The use of stems in the selection of International Nonproprietary Names (INN) for pharmaceutical substances. Geneva: World Health Organization; 2018 (WHO/EMP/RHT/TSN/2018.1). Licence: CC BY-NC-SA 3.0 IGO. Cataloguing-in-Publication (CIP) data.
    [Show full text]
  • Discovery of Β-Arrestin-Biased Β2-Adrenoceptor Agonists from 2-Amino-2-Phenylethanol Derivatives
    www.nature.com/aps ARTICLE Discovery of β-arrestin-biased β2-adrenoceptor agonists from 2-amino-2-phenylethanol derivatives Anthony Yiu-Ho Woo1,2, Xin-yue Ge3,4,LiPan3,4, Gang Xing3,4, Yong-mei Mo3,4, Rui-juan Xing3,4,9, Xiao-ran Li1, Yu-yang Zhang1, Irving W. Wainer5,6, Mao-sheng Cheng3,4 and Rui-ping Xiao2,7,8 β-Arrestins are a small family of proteins important for signal transduction at G protein-coupled receptors (GPCRs). β-Arrestins are involved in the desensitization of GPCRs. Recently, biased ligands possessing different efficacies in activating the G protein- versus the β-arrestin-dependent signals downstream of a single GPCR have emerged, which can be used to selectively modulate GPCR signal transduction in such a way that desirable signals are enhanced to produce therapeutic effects while undesirable signals of the same GPCR are suppressed to avoid side effects. In the present study, we evaluated agonist bias for compounds developed along a drug discovery project of β2-adrenoceptor agonists. About 150 compounds, including derivatives of fenoterol, 2-amino-1- phenylethanol and 2-amino-2-phenylethanol, were obtained or synthesized, and initially screened for their β-adrenoceptor- mediated activities in the guinea pig tracheal smooth muscle relaxation assay or the cardiomyocyte contractility assay. Nineteen bioactive compounds were further assessed using both the HTRF cAMP assay and the PathHunter β-arrestin assay. Their concentration-response data in stimulating cAMP synthesis and β-arrestin recruitment were applied to the Black–Leff operational model for ligand bias quantitation. As a result, three compounds (L-2, L-4, and L-12) with the core structure of 5-(1-amino-2- hydroxyethyl)-8-hydroxyquinolin-2(1H)-one were identified as a new series of β-arrestin-biased β2-adrenoceptor agonists, whereas salmeterol was found to be Gs-biased.
    [Show full text]
  • Glucocorticoid Enhancement of Memory Storage Involves
    Proc. Natl. Acad. Sci. USA Vol. 94, pp. 14048–14053, December 1997 Neurobiology Glucocorticoid enhancement of memory storage involves noradrenergic activation in the basolateral amygdala (dexamethasoneyRU 28362yb-adrenergic antagonistsyinhibitory avoidance) GINA L. QUIRARTE*†,BENNO ROOZENDAAL*‡, AND JAMES L. MCGAUGH*§ *Center for the Neurobiology of Learning and Memory and §Department of Psychobiology, University of California, Irvine, CA 92697-3800; and †Centro de Neurobiologı´a, Universitat Nacional Autonome de Mexico, Queretaro, Qro., 76001 Mexico Contributed by James L. McGaugh, October 7, 1997 ABSTRACT Evidence indicates that the modulatory ef- and opioid peptidergic systems influence the training-induced fects of the adrenergic stress hormone epinephrine as well as release of norepinephrine (13, 14). several other neuromodulatory systems on memory storage Findings of a series of recent experiments from our labo- are mediated by activation of b-adrenergic mechanisms in the ratory indicate that the amygdala is involved in mediating the amygdala. In view of our recent findings indicating that the memory-modulating effects of glucocorticoids (15). Excito- amygdala is involved in mediating the effects of glucocorti- toxically induced lesions of the basolateral (BLA), but not the coids on memory storage, the present study examined whether central (CEA), nucleus of the amygdala blocked the enhancing the glucocorticoid-induced effects on memory storage depend effects of systemic posttraining injections of dexamethasone, a on b-adrenergic
    [Show full text]
  • 3- and J82-Adrenergic Receptors in Rat Brain (Norepinephrine/Epinephrine/'2,5-Labeled Pindolol/Ultrofflm)
    Proc. Natl. Acad. Sci. USA Vol. 81, pp. 1585-1589, March 1984 Neurobiology Quantitative autoradiography of !,3- and j82-adrenergic receptors in rat brain (norepinephrine/epinephrine/'2,5-labeled pindolol/Ultrofflm) THOMAS C. RAINBOW, BRUCE PARSONS, AND BARRY B. WOLFE Department of Pharmacology/G3, University of Pennsylvania School of Medicine, Philadelphia, PA 19104 Communicated by Louis B. Flexner, November 21, 1983 ABSTRACT We have used quantitative autoradiography dards, the optical density readings can be quantitatively con- to localize in rat brain /3i- and .82-adrenergic receptors. These verted to amount of radioligand bound per mg of protein receptors were labeled in vitro with 1251-labeled pindolol, an (11). Thus, in the present study we have combined the tech- antagonist of 13-adrenergic receptors that binds nonselectively niques of quantitative autoradiography and quantitative analy- to both .p2 and #2 subtypes. The selective inhibition of 1251_ sis of -adrenergic receptor subtypes to allow determination labeled pindolol binding with specific antagonists of .BI and 132 of subtype densities with a resolution of =100 Am. These receptors allowed the visualization of 18-adrenergic receptor studies, in addition to confirming the previous reports on the subtypes. High levels of ,B1 receptors were observed in the cin- distribution of subtypes in gross areas, such as the entire gulate cortex, layers I and II of the cerebral cortex, the hippo- cerebral cortex or cerebellum, have also disclosed that 381 campus, the Islands of Calleja, and the gelatinosus, mediodor- and 832 receptors are distributed heterogeneously among afa- sal, and ventral nuclei of the thalamus. High levels of #82 recep- tomically discrete nuclei and subregions of rat brain.
    [Show full text]
  • Customs Tariff - Schedule
    CUSTOMS TARIFF - SCHEDULE 99 - i Chapter 99 SPECIAL CLASSIFICATION PROVISIONS - COMMERCIAL Notes. 1. The provisions of this Chapter are not subject to the rule of specificity in General Interpretative Rule 3 (a). 2. Goods which may be classified under the provisions of Chapter 99, if also eligible for classification under the provisions of Chapter 98, shall be classified in Chapter 98. 3. Goods may be classified under a tariff item in this Chapter and be entitled to the Most-Favoured-Nation Tariff or a preferential tariff rate of customs duty under this Chapter that applies to those goods according to the tariff treatment applicable to their country of origin only after classification under a tariff item in Chapters 1 to 97 has been determined and the conditions of any Chapter 99 provision and any applicable regulations or orders in relation thereto have been met. 4. The words and expressions used in this Chapter have the same meaning as in Chapters 1 to 97. Issued January 1, 2020 99 - 1 CUSTOMS TARIFF - SCHEDULE Tariff Unit of MFN Applicable SS Description of Goods Item Meas. Tariff Preferential Tariffs 9901.00.00 Articles and materials for use in the manufacture or repair of the Free CCCT, LDCT, GPT, following to be employed in commercial fishing or the commercial UST, MXT, CIAT, CT, harvesting of marine plants: CRT, IT, NT, SLT, PT, COLT, JT, PAT, HNT, Artificial bait; KRT, CEUT, UAT, CPTPT: Free Carapace measures; Cordage, fishing lines (including marlines), rope and twine, of a circumference not exceeding 38 mm; Devices for keeping nets open; Fish hooks; Fishing nets and netting; Jiggers; Line floats; Lobster traps; Lures; Marker buoys of any material excluding wood; Net floats; Scallop drag nets; Spat collectors and collector holders; Swivels.
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2010/0184806 A1 Barlow Et Al
    US 20100184806A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2010/0184806 A1 Barlow et al. (43) Pub. Date: Jul. 22, 2010 (54) MODULATION OF NEUROGENESIS BY PPAR (60) Provisional application No. 60/826,206, filed on Sep. AGENTS 19, 2006. (75) Inventors: Carrolee Barlow, Del Mar, CA (US); Todd Carter, San Diego, CA Publication Classification (US); Andrew Morse, San Diego, (51) Int. Cl. CA (US); Kai Treuner, San Diego, A6II 3/4433 (2006.01) CA (US); Kym Lorrain, San A6II 3/4439 (2006.01) Diego, CA (US) A6IP 25/00 (2006.01) A6IP 25/28 (2006.01) Correspondence Address: A6IP 25/18 (2006.01) SUGHRUE MION, PLLC A6IP 25/22 (2006.01) 2100 PENNSYLVANIA AVENUE, N.W., SUITE 8OO (52) U.S. Cl. ......................................... 514/337; 514/342 WASHINGTON, DC 20037 (US) (57) ABSTRACT (73) Assignee: BrainCells, Inc., San Diego, CA (US) The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system (21) Appl. No.: 12/690,915 including by stimulating or increasing neurogenesis, neuro proliferation, and/or neurodifferentiation. The disclosure (22) Filed: Jan. 20, 2010 includes compositions and methods based on use of a peroxi some proliferator-activated receptor (PPAR) agent, option Related U.S. Application Data ally in combination with one or more neurogenic agents, to (63) Continuation-in-part of application No. 1 1/857,221, stimulate or increase a neurogenic response and/or to treat a filed on Sep. 18, 2007. nervous system disease or disorder. Patent Application Publication Jul. 22, 2010 Sheet 1 of 9 US 2010/O184806 A1 Figure 1: Human Neurogenesis Assay Ciprofibrate Neuronal Differentiation (TUJ1) 100 8090 Ciprofibrates 10-8.5 10-8.0 10-7.5 10-7.0 10-6.5 10-6.0 10-5.5 10-5.0 10-4.5 Conc(M) Patent Application Publication Jul.
    [Show full text]
  • ( 12 ) United States Patent
    US010493080B2 (12 ) United States Patent (10 ) Patent No.: US 10,493,080 B2 Schultz et al. (45 ) Date of Patent : Dec. 3 , 2019 ( 54 ) DIRECTED DIFFERENTIATION OF (56 ) References Cited OLIGODENDROCYTE PRECURSOR CELLS TO A MYELINATING CELL FATE U.S. PATENT DOCUMENTS 7,301,071 B2 11/2007 Zheng (71 ) Applicants : The Scripps Research Institute , La 7,304,071 B2 12/2007 Cochran et al. Jolla , CA (US ) ; Novartis AG , Basel 9,592,288 B2 3/2017 Schultz et al. 2003/0225072 A1 12/2003 Welsh et al. ( CH ) 2006/0258735 Al 11/2006 Meng et al. 2009/0155207 Al 6/2009 Hariri et al . (72 ) Inventors : Peter Schultz , La Jolla , CA (US ) ; Luke 2010/0189698 A1 7/2010 Willis Lairson , San Diego , CA (US ) ; Vishal 2012/0264719 Al 10/2012 Boulton Deshmukh , La Jolla , CA (US ) ; Costas 2016/0166687 Al 6/2016 Schultz et al. Lyssiotis , Boston , MA (US ) FOREIGN PATENT DOCUMENTS (73 ) Assignees : The Scripps Research Institute , La JP 10-218867 8/1998 Jolla , CA (US ) ; Novartis AG , Basel JP 2008-518896 5/2008 (CH ) JP 2010-533656 A 10/2010 WO 2008/143913 A1 11/2008 WO 2009/068668 Al 6/2009 ( * ) Notice : Subject to any disclaimer , the term of this WO 2009/153291 A1 12/2009 patent is extended or adjusted under 35 WO 2010/075239 Al 7/2010 U.S.C. 154 ( b ) by 0 days . (21 ) Appl. No .: 15 /418,572 OTHER PUBLICATIONS Molin - Holgado et al . “ Regulation of muscarinic receptor function in ( 22 ) Filed : Jan. 27 , 2017 developing oligodendrocytes by agonist exposure ” British Journal of Pharmacology, 2003 , 138 , pp .
    [Show full text]