Rauvolfia Serpentine)

Total Page:16

File Type:pdf, Size:1020Kb

Rauvolfia Serpentine) International Journal of Innovation in Agriculture Sciences and Rural Development Vol.1, NO.1 , P : 13 - 27 Received: 19 Nov 2018 Accepted: 15 Feb 2019 A review of the therapeutic properties of the medical herb ( Rauvolfia serpentine) Seyed Mohammad Reza Soltani introduces botanical aspects, effective Moghadas materials and scientific evaluation of using R. Naturopathic Reseacher, Islamic Azad University serpentine. The author emphasizes on the importance of observing the suitable dose of Abstract using R. serpentine plant and screening the patients to minimize its side-effects and R. serpentina is an evergreen plant as a introduces this plant a good recommendation member of Apocynaceae family and is used to control and treat some diseases such as in the treatment of some of the diseases high systolic hypertension and mental including hypertension. More than 100 diseases such as anxiety and schizophrenia. species are included in the Rauwolfia genus, and they are native to tropical and subtropical Keywords: Rauvolfia serpentina, Asrole, regions around the world, including Europe, Medicinal herbs, Natural treatment, Blood Africa, Asia, Australia, and the Central pressure America and South America. The plant Introduction usually grows to a height 60 - 90 cm with the leaves as elliptical or lanceolate shaped. It Rauwolfia was named in honor of German also has small pink or white flowers, with physician Dr Leonhard Rauwolf, who shiny purple or black and round fruits. The published a report of his travelling in India. root of this plant has been used for a long time The root of this plant has been used for a long in India and the Malay peninsula as an time in India and the Malay peninsula as an antidote to the sting of insects and poisonous antidote to the stings of insects and reptiles. It has also been used to reduce fever, poisonous reptiles. The name of this plant is as a stimulant to uterine contractions, recognized as Sarpgandha in Sanskrit in the diarrhea, for insomnia, and particularly for old Indian books (1000 years before BC) and the treatment of insanity. The present study also in the great works of Charaka (second century, A.D.). This plant also has been used 13 to reduce fever, as a stimulant to uterine useful Rauwolfia species from therapeutical contractions, diarrhea, dysentery, insomnia, aspects is Rauwolfia serpentina growing to and insanity. More than two decades, its the height of 1.5 to 3 foot and it has pink clinical applications were successful in the white flowers (Mia et al., 2009:168). treatment of hypertension. Rauvolfia The history of the application of Rauwolfia in serpentina or Serpentina is a climbing or twin treating diseases shrub belongs to Apocynaceae family and is found in Himalaya, Assam, Pego, Java, R. serpentine has been used for centuries in Tenaserim, Bahar, Deccan and Malay fold medicine in India to treat different Peninsula. Its variety is recognized as diseases such as the sting of snake and Sarpgandha (ancient times), Chandria insects, fever, malaria, abdomen pain and (Sanskrite), Chota-Chand (Indian), Chand dysentery. It was also used as a uterine (Bengal), Danbarova or Pagla-Kadava stimulant, febrifuge, and cure for insanity. (Bihar), Chandra, Chota Chanid, Karavi or The plant was mentioned in Indian Harkaya (Bombay), patalagarud or manuscripts since 1000 bc and is also known Atalaganidi (Telegu), Kumanmeliour as sarpagandha and chandriko. Serpentina is (Tamil), Chovana Vilpouri (Malay) and selected for study due to its long, tapering, Danbarova or DIHAN Barea (Oria). It is said snake-like roots. The Indian political leader, that 130 special species of Rauwolfia grow in Mahatma Gandhi was known to use the root tropical areas as local. Yang can described of Rauwolfia to make a tea that he consumed five species of this plant as follows: to help relax . Rauwolfia serpinta, Rauwolfia cansine, The Indian physician Rustom Jal Vakil Rauwolfia micranta, Rauwolfia densiflora introduced Rauwolfia to western medicine. and Rauwolfia praknis. Based on the origin He collected data on patients undergoing or source of presenting eight species of treatment with Rauwolfia for 10 years, from Rauwolfia growing in India and 1939 to 1949. In 1949, he published a paper Rauwolfia species in Indian market, Bengal, on watershed in a British Medical journal and Bihar, Osma, Dehar and Seylan are presented the antihypertensive properties completely recognized. These species show of R serpentina. He presented his exact considerable difference in the quality and results from treating 50 patients who had high volume of therapeutical alkaloids. The most blood pressure with the root of Rauwolfia. 14 The results were considerable and An alkaloid isolated by the Chemistry significant. By 1949, more than 90% of Department of the tropical school of Indian physicians were using Rauwolfia in Medicine, Calcutta, was investigated by the treatment of high blood pressure. After Chopra, Gupta and Mukherjee (1933). As a Vakil’s original paper, more than 100 result of their pharmacological studies they scientific articles were published around the showed that this alkaloid has a toxic effect on world. After the main article of Vakil, more lower forms of life such as Paramoecia than 100 scientific papers were published all Caudatum in dilution of 1 in 20,000. Its around the world. In recent years, this drug is toxicity on animals was variable. Frogs used for sedative properties and it is also used tolerated completely, whereas the white for curing insanity and is advertised mostly in mouse was very sensitive. The drug was non-allowed press. Its application in the much more toxic, when injected treatment of hypertension is a new source of intravenously or intraperitoneally, than when pharmacological researches about this drug. injected subcutaneously. In the circulatory It is said that the consumption cases of this system, the drug decreased the blood pressure drug is under experiment and any registration of cats under anaesthesia as it has long- of the exact clinical observations is valuable lasting effect. If spine of cats are used, the in real evaluation of this drug in the treatment effect produced is very low, which shows that of hyperpicsia. Chemically, the root contains the fall in blood pressure was due to some alkaloids. Sen and Bose (1931) found vasodilatation as a result of the the depression two alkaloids with different melting points. of the vasomotor center in the medulla Siddiqui and Siddiqui (1931) introduced five oblongata. The fall in blood pressure was also alkaloids including ajmaline, ajmalimine, noticed after the terminations of the vagi ajmalicine, serpentine, serpentinine . Von were paralysed with atropine, showing that Italie and Steenhaur mentioned at least three vagal inhibition is not important in the fall alkaloids that their nature and identity were created. The fall in blood pressure was also similar to the findings of Siddiqui and partly due to decreased cardic output, which Siddiqui. was found on myocardiographic studies. During the injection of the drug through isolated vessels, Chopra and his coworkers found that it definitely decreased the number 15 of drops of the injection per minute, which R. serpentina is an evergreen plant as a means that it causes ‘vasoconstriction’ member of Apocynaceae family and is used though they have erroneously called it in the treatment of some of the diseases vasodilatation. Both, the subjects were intact. including hypertension. More than 100 The drug seemed to have a slight depressant species are included in the Rauwolfia genus, action. The alkaloid has a stimulant action on and they are native to tropical and subtropical the simple muscles of the alimentary canal regions around the world, including Europe, and the uterus. However, its most interesting Africa, Asia, Australia, and the Central action was observed on the central nervous America and South America. system, which it seems to act in the reverse Rauwolfia serpentina is native to the humid order of development of heart congestive forests of Southeast Asia, including India, system. As by affecting the neural centers can Burma, Bangladesh, Sri Lanka, and lead to drowsiness, diminution in motor Malaysia. The plant normally grows to a activity, diminution in the sensory stimuli, height between 60 and 90 cm and has green low performance of the medullary centers leaves as 7 to 10 cm long and 3.5 to 5.0 cm (Bhatia, 1942:2). wide. The leaves are elliptical or lanceolate shaped with 3 to 5 leaves. The plant has The introduction of Rouvolfia serpentine or small pink or white flowers. It has many Indian snake root shiny, black or purple and round fruits that Family : Apocynaceae are about 0.5 cm in diameter. The plant has a prominent, soft taproot with a length between Species : serpentina 30 and 50 cm and a diameter between 1.2 and Genus : Rouvolfia 2.5 cm (Kiran, Jothi Priya & Gayatri Devi, 2018:25 16 Figure 1- Rouvolfia Figure 2-Another view of Rouvolfia 2. Chemical constituents of Rouvolfia system and thereby decreases blood pressure as compared to other blood-pressure Rauvolfia serpentina has been an extensive decreasing agents. It is reported that R. field of research for decades and several serpentina root contains 0.7-3.0% of total individuals have explored this field due to its alkaloids and about 0.1% of the active phytochemical properties. The various principle reserpine which is an indole phytochemical compounds or secondary alkaloid, existing in the root. Thus, root metabolites present in R. serpentina include biomass production of this plant may be of alkaloids, phenols, tannins and flavonoids economic importance. On the basis of the (Rahman, 2018:45). structure, there are three types of alkaloids: Alkaloids Weak basic indole alkaloids, intermediate Alkaloids are large group of organic base alkaloids and strong anhydronium molecules which contain a heterocyclic bases. The various alkaloids identified in nitrogen ring.
Recommended publications
  • Effects of the Putative Antipsychotic Alstonine on Glutamate Uptake in Acute Hippocampal Slices ⇑ Ana P
    Neurochemistry International 61 (2012) 1144–1150 Contents lists available at SciVerse ScienceDirect Neurochemistry International journal homepage: www.elsevier.com/locate/nci Effects of the putative antipsychotic alstonine on glutamate uptake in acute hippocampal slices ⇑ Ana P. Herrmann a,b, , Paula Lunardi b, Luísa Klaus Pilz a, Ana C. Tramontina b, Viviane M. Linck a,b, Christopher O. Okunji c, Carlos A. Gonçalves b, Elaine Elisabetsky a,b a Laboratório de Etnofarmacologia, Departamento de Farmacologia, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Rua Sarmento Leite, 500, 90050-170 Porto Alegre, RS, Brazil b Programa de Pós-graduação em Ciências Biológicas: Bioquímica, Instituto de Ciências Básicas da Saúde, Universidade Federal do Rio Grande do Sul, Rua Ramiro Barcelos, 2600, 90035-000 Porto Alegre, RS, Brazil c International Centre for Ethnomedicine and Drug Development (InterCEDD), Nsukka, Enugu State, Nigeria article info abstract Article history: A dysfunctional glutamatergic system is thought to be central to the negative symptoms and cognitive Received 8 March 2012 deficits recognized as determinant to the poor quality of life of people with schizophrenia. Modulating Received in revised form 13 August 2012 glutamate uptake has, thus, been suggested as a novel target for antipsychotics. Alstonine is an indole Accepted 15 August 2012 alkaloid sharing with atypical antipsychotics the profile in animal models relevant to schizophrenia, Available online 25 August 2012 though divergent in its mechanism of action. The aim of this study was to evaluate the effects of alstonine on glutamate uptake. Additionally, the effects on glutathione content and extracellular S100B levels were Keywords: assessed.
    [Show full text]
  • (12) United States Patent (10) Patent No.: US 9,687,864 B2 Fulton Et Al
    USOO9687864B2 (12) United States Patent (10) Patent No.: US 9,687,864 B2 Fulton et al. (45) Date of Patent: Jun. 27, 2017 (54) SYSTEMAND METHOD FOR ENHANCED 428/25 (2015.01); Y10T 428/31504 (2015.04); ELECTROSTATIC DEPOSITION AND Y10T 428/31507 (2015.04); SURFACE COATINGS (Continued) (58) Field of Classification Search (71) Applicant: Battelle Memorial Institute, USPC .......... 118/620–640; 23.9/690 708; 427/458, Columbus, OH (US) 427/475 4.86 (72) Inventors: John L. Fulton, Richland, WA (US); See application file for complete search history. George S. Deverman, Richland, WA (US); Dean W. Matson, Kennewick, (56) References Cited CA (US); Clement R. Yonker, Kennewick, WA (US); C. Douglas U.S. PATENT DOCUMENTS Taylor, Franklinton, NC (US); James 3,087,860 A 4, 1963 Endicott B. McClain, Raleigh, NC (US); Joseph 3,123,077 A 3, 1964 Alcamo M. Crowley, Cambria, CA (US) (Continued) (73) Assignee: Battelle Memorial Institute, Columbus, OH (US) FOREIGN PATENT DOCUMENTS CA 2589761 12, 2004 (*) Notice: Subject to any disclaimer, the term of this CN 1465410 1, 2004 patent is extended or adjusted under 35 (Continued) U.S.C. 154(b) by 0 days. (21) Appl. No.: 14/310,960 OTHER PUBLICATIONS Abreu Filho et al., “Influence of metal alloy and the profile of (22) Filed: Jun. 20, 2014 coronary stents in patients with multi-vessel coronary disease.” Clinics 66(6):985-989 (2011). (65) Prior Publication Data (Continued) US 2015/OO40827 A1 Feb. 12, 2015 Related U.S. Application Data Primary Examiner — Yewebdar Tadesse (74) Attorney, Agent, or Firm — Lerner, David, (62) Division of application No.
    [Show full text]
  • Fused Tricyclic Dual Inhibitors of Cdk 4/6 and Flt3
    (19) TZZ ¥¥_T (11) EP 2 937 349 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.: 28.10.2015 Bulletin 2015/44 C07D 471/14 (2006.01) C07D 519/00 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01) (2006.01) (21) Application number: 15161337.9 A61P 35/02 (22) Date of filing: 21.03.2012 (84) Designated Contracting States: • Keegan, Kathleen S. AL AT BE BG CH CY CZ DE DK EE ES FI FR GB Bainbridge Island, WA Washington 98110 (US) GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO • LI, Zhihong PL PT RO RS SE SI SK SM TR Millbrae, CA California 94030 (US) Designated Extension States: • Lively, Sarah E. BA ME San Carlos, CA California 94070 (US) • McGee, Lawrence R. (30) Priority: 23.03.2011 US 201161466841 P Pacifica, CA California 94044 (US) •Ragains,Mark L. (62) Document number(s) of the earlier application(s) in Fort Worth, TX Texas 76109 (US) accordance with Art. 76 EPC: • Wang, Xianghong 12711738.0 / 2 688 887 Dublin, CA California 94568 (US) • Weidner, Margaret F. (71) Applicant: AMGEN INC. Woodinville, WA Washington 98072 (US) Thousand Oaks, CA 91320-1799 (US) • Zhang, Jian Foster City, CA California 94404 (US) (72) Inventors: • Chen, Xiaoqi (74) Representative: Hoffmann Eitle Palo Alto, CA California 94303 (US) Patent- und Rechtsanwälte PartmbB •Dai,Kang Arabellastraße 30 Albany, CA California 94706 (US) 81925 München (DE) • Duquette, Jason A. Millbrae, CA California 94030 (US) Remarks: • Gribble, Michael W., Jr. This application was filed on 12-05-2015 as a San Francisco, CA California 94110 (US) divisional application to the application mentioned • Huard, Justin N.
    [Show full text]
  • Exploring New Pharmacology and Toxicological Screening and Safety
    Zaman et al. BMC Complementary and Alternative Medicine (2015) 15:121 DOI 10.1186/s12906-015-0635-2 RESEARCH ARTICLE Open Access Exploring new pharmacology and toxicological screening and safety evaluation of one widely used formulation of Nidrakar Bati from South Asia region Afria Zaman1, Md Shamsuddin Sultan Khan2*, Lucky Akter1, Sharif Hossain Syeed3, Jakia Akter4, Abdullah Al Mamun5, Md Ershad Alam5, Md Ahsan Habib5 and Md Abdul Jalil5 Abstract Background: Nidrakar Bati (NKB) is an herbal remedy consisted with seven medicinal herbs widely used to cure Somnifacient (sleeping aid) in South Asia as Ayurvedic medicinal system. In the present study, pharmacological and toxicological effects of this medicine was investigated in mice to validate the safety and efficacy of the herb. Methods: Organic solvent extracts NKB were prepared using maceration method. Effect of extracts on the central nervous system was evaluated using hypnotic activity assay. Effect of the extracts on metabolic activity, assessing involvement of thyroid was conducted using hypoxia test. analgesic and anti-inflammatory activities were assessed in mice using acetic acid induced writhing, formalin induced paw edema, xylene induced ear edema assays. Anxiolytic activity was performed using plus maze, climbing out and forced swimming tests. Effect of the extracts on psychopharmacological effect was carried out using locomotor activity tests (open field, Hole-board and Hole-cross tests). Neuropharmacological effect of the extracts was performed using motor coordination (rotarod test). Toxicological potential of the extract was evaluated using gastro-intestinal activity (gastric emptying and gastrointestinal motility tests). Results: The studied formulation reduced the CNS stimulant effects dose independently. In the hypoxia test, only a dose of 100 mg/kg of NKB decreased the survival time.
    [Show full text]
  • Antitumor Activities of Rauwolfia Vomitoria Extract and Potentiation Of
    Current Therapeutic Research 75 (2013) 8–14 Contents lists available at ScienceDirect Current Therapeutic Research journal homepage: www.elsevier.com/locate/cuthre Antitumor Activities of Rauwolfia vomitoria Extract and Potentiation of Carboplatin Effects Against Ovarian Cancer☆ Jun Yu, PhD1,2, Yan Ma, PhD1,2, Jeanne Drisko, MD2, Qi Chen, PhD1,2,n 1 Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, Kansas City, Kansas 2 KU Integrative Medicine, University of Kansas Medical Center, Kansas City, Kansas article info abstract Article history: Background: Tumor resistance to platinum-based drugs has been an obstacle to the treatment of ovarian Accepted 26 April 2013 cancer. Extract of the plant Rauwolfia vomitoria has long been used by cancer patients. However, there have not been systematic studies of its anticancer activity. Key words: Objective: In an effort to enhance the effectiveness of platinum-based drugs, we investigated the carboplatin anticancer effect of a Rauwolfia vomitoria extract (Rau), both alone and in combination with ovarian cancer carboplatin (Cp). plant extract Methods: In vitro cytotoxicity and colony formation were evaluated in several ovarian cancer cell lines. fi Rauwol a vomitoria In vivo effects were evaluated in an intraperitoneal ovarian cancer mouse model. The combination of Rau synergy and Cp was assessed using Chou-Talalay’s constant ratio design and median effect analysis based on the isobologram principle to determine the combination index values. Results: Rau decreased cell growth in all 3 tested ovarian cancer cell lines dose dependently and completely inhibited formation of colonies in soft agar. Apoptosis was induced in a time- and dose- dependent manner and was the predominant form of Rau-induced cell death.
    [Show full text]
  • Development of a Pharmacophore for Inhibition of Human Liver Cytochrome P-450 2D6: Molecular Modeling and Inhibition Studies
    1136 J. Med. Chem. 1993,36, 1136-1145 Development of a Pharmacophore for Inhibition of Human Liver Cytochrome P-450 2D6: Molecular Modeling and Inhibition Studies Giinter R. Strob1,'J Stephanie von Kruedener,t Joachim Stockigt; F. Peter Guengerich,O and Thomas Wolfft Znstitut fur Toxikologie, GSF - Forschungszentrum fiir Umwelt und Gesundheit, 8042 Neuherberg, Germany, Znstitut fur Pharmazie, Johannes Gutenberg- Universitiit, 6500 Mainz, Germany, and Center in Molecular Toxicology, Vanderbilt University, Nashville, Tennessee 37232 Received December 31, 1991 To gain insight into the specificity of cytochrome P-450 2D6 toward inhibitors, a preliminary pharmacophore model was built up using strong competitive inhibitors. Ajmalicine (l),the strongest inhibitor known (Ki = 3 nM) was selected as template because of ita rigid structure. The preliminary pharmacophore model was validated by performing inhibition studies with derivatives of ajmalicine (1)and quinidine (9). Bufuralol(18) was chosen as substrate and the metabolite 1'-hydroxybufuralol (19) was separated by high performance liquid chromatography. All incubations were carried out using human liver microsomes after demonstration that the Ki values obtained with microsomes were in accordance with those obtained with a reconstituted monooxygenase system containing purified cytochrome P-4502D6. Large differences of Ki values ranging between 0.005 and 100 pM were observed. Low-energy conformers of tested compounds were fit within the preliminary pharmacophore model. The analysis of steric and electronic properties of these compounds led to the definition of a final pharmacophore model. Characteristic properties are a positive charge on a nitrogen atom and a flat hydrophobic region, the plane of which is almost perpendicular to the N-H axis and maximally extends up to a distance of 7.5 A from the nitrogen atom.
    [Show full text]
  • Handbook of Experimental Pharmacology Volume
    Handbook of Experimental Pharmacology Volume 212 Editor-in-Chief F.B. Hofmann, München Editorial Board J.A. Beavo, Seattle J.E. Barrett, Philadelphia D. Ganten, Berlin P. Geppetti, Florence M.C. Michel, Ingelheim C.P. Page, London W. Rosenthal, Berlin For further volumes: http://www.springer.com/series/164 . Gerhard Gross • Mark A. Geyer Editors Current Antipsychotics Editors Gerhard Gross Mark A. Geyer Abbott, Neuroscience Research, GPRD University of California San Diego Ludwigshafen, Germany Department of Psychiatry Institut fu¨r Pharmakologie La Jolla Universita¨t Duisburg-Essen California Universita¨tsklinikum Essen USA Essen Germany ISSN 0171-2004 ISSN 1865-0325 (electronic) ISBN 978-3-642-25760-5 ISBN 978-3-642-25761-2 (eBook) DOI 10.1007/978-3-642-25761-2 Springer Heidelberg New York Dordrecht London Library of Congress Control Number: 2012952465 # Springer-Verlag Berlin Heidelberg 2012 This work is subject to copyright. All rights are reserved by the Publisher, whether the whole or part of the material is concerned, specifically the rights of translation, reprinting, reuse of illustrations, recitation, broadcasting, reproduction on microfilms or in any other physical way, and transmission or information storage and retrieval, electronic adaptation, computer software, or by similar or dissimilar methodology now known or hereafter developed. Exempted from this legal reservation are brief excerpts in connection with reviews or scholarly analysis or material supplied specifically for the purpose of being entered and executed on a computer system, for exclusive use by the purchaser of the work. Duplication of this publication or parts thereof is permitted only under the provisions of the Copyright Law of the Publisher’s location, in its current version, and permission for use must always be obtained from Springer.
    [Show full text]
  • Handbook of Schizophrenia Spectrum Disorders, Volume III
    Handbook of Schizophrenia Spectrum Disorders, Volume III Michael S. Ritsner Editor Handbook of Schizophrenia Spectrum Disorders, Volume III Therapeutic Approaches, Comorbidity, and Outcomes 123 Editor Michael S. Ritsner Technion – Israel Institute of Technology Rappaport Faculty of Medicine Haifa Israel [email protected] ISBN 978-94-007-0833-4 e-ISBN 978-94-007-0834-1 DOI 10.1007/978-94-007-0834-1 Springer Dordrecht Heidelberg London New York Library of Congress Control Number: 2011924745 © Springer Science+Business Media B.V. 2011 No part of this work may be reproduced, stored in a retrieval system, or transmitted in any form or by any means, electronic, mechanical, photocopying, microfilming, recording or otherwise, without written permission from the Publisher, with the exception of any material supplied specifically for the purpose of being entered and executed on a computer system, for exclusive use by the purchaser of the work. Printed on acid-free paper Springer is part of Springer Science+Business Media (www.springer.com) Foreword Schizophrenia Spectrum Disorders: Insights from Views Across 100 years Schizophrenia spectrum and related disorders such as schizoaffective and mood dis- orders, schizophreniform disorders, brief psychotic disorders, delusional and shared psychotic disorders, and personality (i.e., schizotypal, paranoid, and schizoid per- sonality) disorders are the most debilitating forms of mental illness, worldwide. There are 89,377 citations (including 10,760 reviews) related to “schizophrenia” and 2118 (including 296 reviews) related to “schizophrenia spectrum” in PubMed (accessed on August 12, 2010). The classification of these disorders, in particular, of schizophrenia, schizoaf- fective and mood disorders (referred to as functional psychoses), has been debated for decades, and its validity remains controversial.
    [Show full text]
  • Negative Allosteric Modulators of Mglu7 Receptor As Putative Antipsychotic Drugs
    fnmol-11-00316 September 18, 2018 Time: 19:5 # 1 ORIGINAL RESEARCH published: 20 September 2018 doi: 10.3389/fnmol.2018.00316 Negative Allosteric Modulators of mGlu7 Receptor as Putative Antipsychotic Drugs Paulina Cieslik,´ Monika Wo´zniak,Katarzyna Kaczorowska, Piotr Branski,´ Grzegorz Burnat, Agnieszka Chocyk, Bartosz Bobula, Piotr Gruca, Ewa Litwa, Agnieszka Pałucha-Poniewiera, Agnieszka W ˛asik,Andrzej Pilc and Joanna Wieronska´ * Institute of Pharmacology, Polish Academy of Sciences, Krakow, Poland The data concerning antipsychotic-like activity of negative allosteric modulators (NAMs)/antagonists of mGlu7 receptors are limited. The only available ligands for this receptor are MMPIP and ADX71743. In the present studies, we used stable cell line expressing mGlu7 receptor and it was shown that both compounds dose-dependently potentiated forskolin elevated cAMP concentration in the T-REx 293 cells, showing their inverse agonist properties. Subsequently, pharmacokinetic studies were performed. Both compounds were given intraperitoneally (i.p.) at the dose of 10 mg/kg and reached Cmax 0.25–0.5 h after administration, and then they declined rapidly, ADX71743 being almost undetectable 2 h after administration, while the concentration of MMPIP was still observed, suggesting that the concentration of MMPIP was more stable. Finally, we investigated the role of both mGlu7 receptor NAMs in animal models of schizophrenia. Behavioral tests commonly used in antipsychotic drug discovery were conducted. Both Edited by: tested compounds dose-dependently inhibited MK-801-induced hyperactivity (MMPIP Enza Palazzo, Università degli Studi della Campania at 15 mg/kg; ADX at 5 and 15 mg/kg) and DOI-induced head twitches (MMPIP at 5, Luigi Vanvitelli Naples, Italy 10, 15 mg/kg; ADX at 2.5, 5, 10 mg/kg).
    [Show full text]
  • WO 2012/166819 Al 6 December 2012 (06.12.2012) P O P C T
    (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (10) International Publication Number (43) International Publication Date WO 2012/166819 Al 6 December 2012 (06.12.2012) P O P C T (51) International Patent Classification: (71) Applicants (for all designated States except US): MI- A61F 2/02 (2006.01) CELL TECHNOLOGIES, INC. [US/US]; 801 Capitola Drive, Suite 1, Durham, NC 2771 3 (US). BATTELLE (21) International Application Number: MEMORIAL INSTITUTE [US/US]; P. O. Box 999. Kl- PCT/US20 12/040040 53, Richland, WA 99352 (US). (22) International Filing Date: (72) Inventors; and 30 May 20 12 (30.05.2012) (75) Inventors/Applicants (for US only): MATSON, Dean, W. (25) Filing Language: English [US/US]; 4104 W. 17th Avenue, Kennewick, WA 99338 (US). YONKER, Clement, R. [US/US]; P. O. Box M, 19 (26) Publication Language: English Char Lane, Sandpoint, ID 83864 (US). FULTON, John, (30) Priority Data: L. [US/US]; 1809 Hunt, Richland, WA 99354 (US). DE- 61/491,847 31 May 201 1 (3 1.05.201 1) US VERMAN, George, S. [US/US]; 1573 Foxglove Avenue, 61/649,585 2 1 May 2012 (21.05.2012) US Richland, WA 99352 (US). TARASEVICH, Barbara, J. [US/US]; c/o Battelle Memorial Institute, P. O. Box 999, Kl-53, Richland, WA 99352 (US). SHAW, Wendy, J. [Continued on nextpage] (54) Title: SYSTEM AND PROCESS FOR FORMATION OF A TIME-RELEASED, DRUG-ELUTING TRANSFERABLE COATING (57) Abstract: A system and method are disclosed for coating surfaces of F!G. 5 expandable medical devices with composite coatings.
    [Show full text]
  • United States Patent (19) 11 Patent Number: 6,077,850 Carter Et Al
    USOO607785OA United States Patent (19) 11 Patent Number: 6,077,850 Carter et al. (45) Date of Patent: Jun. 20, 2000 54 SUBSTITUTED BENZOPYRAN ANALOGS 59-29681 2/1984 Japan. FOR THE TREATMENT OF 2-22272 1/1990 Japan. NFLAMMATION WO88/04654 6/1988 WIPO .......................... CO7D 311/58 WO94/13659 6/1994 WIPO ... ... CO7D 319/18 WO95/07274 3/1995 WIPO .......................... CO7D 405/12 75 Inventors: SG"SEE,Mark G WO96/4O110 12A 1996 WIPO ............................ A61K 31/35 Devadas, Chesterfield;s sJohn J Talley, WO98/34115 8/1998 WIPO. St. Louis; David L. Brown; Matthew J OTHER PUBLICATIONS Graneto, both of Chesterfield, all of Mo.; Stephen R Bertenshaw, Cheshire, Sabbaramaiah et al., Proc. Soc. Exp. Biol. Med., 216, Conn.; Donald J. Rogier, Jr.; 201: 1997. Srinivasan Raj Nagarajan, both of Hida et al., Anticancer Res., 19, 775-82:1998. Chesterfield, Mo.; Cathleen E. Hanau, Wison, Cancer Res., 58, 2929–34:1998. St. Louis, Mo.; Susan J. Hartmann, Buckman et al., Carcinogensis, 19, 729-29:1998. Kirkwood, Mo.; Cindy L. Ludwig, St. Barnes et al., Lung Biol. Health Dis., 114, 11-27:1998. Louis, Mo.; Suzanne Metz, M. Tsujii et al., Cell, 93, 705–16:1998. Chesterfield, Mo.; Donald E Korte, Bustos, J. Clin. Inverst., 100, 1150–58:1997. Mundelein, Ill. Bagetta et al., Biochem, BiophyS. Res. Commun., 244, 73 Assignee: G.D. Searle & Co., Skokie, Ill. 819-24:1998. Sandhya et al., Brain Res., 788, 233–31:1998. 21 Appl. No.: 09/175,584 Singer et al., Gastroenterology, 115, 297-306:1998. Nogawa et al., Proc. Natl. Acad. Sci., 95, 10966–71:1998.
    [Show full text]
  • The Ambit of Phytotherapy in Psychotic Care
    DOI: 10.5772/intechopen.79547 ProvisionalChapter chapter 4 The Ambit of Phytotherapy in Psychotic Care AbdulwakeelAbdulwakeel Ayokun-nun Ajao, Ayokun-nun Ajao, Saheed Sabiu, FataiSaheed Sabiu, Oladunni Fatai Oladunni Balogun, Balogun, DamilareDamilare Adedayo Adekomi Adedayo Adekomi and SefiuSefiu Adekilekun Saheed Adekilekun Saheed Additional information is available at the end of the chapter http://dx.doi.org/10.5772/intechopen.79547 Abstract The rate of psychosis has drastically increased in recent years and the number of prescrip- tions for psychiatric medications has made an even bigger jump. With the worrisome side effects of the medications, which can pose serious health risks and make medica- tion compliance difficult, coupled with the prohibitive cost for many patients, there is an obvious need for alternative solutions. This review presents the ambit of phytotherapy in psychotic care. Interestingly, the review revealed that, plant-based medicines are rich in phytonutrients of antipsychotic importance and may be effective as stand-alone treat- ments or supplementary to conventional interventions. Despite the emerging interest in phytotherapy for mental disorders, the majority of the formulations are yet to be clinically certified. However, simply disregarding them for this reason might be consequential and as such, for better and improved mental health, research into phytotherapeutic care for psychosis must remain to be continuously explored as a promising niche. Keywords: hallucination, mental health, phytonutrient, phytotherapy, psychosis 1. Introduction Feelings and perceptions like paranoia/hearing voices may be highly discomforting, worry- ing, and necessitate people to seek definitive aid. Generally, help have been offered medi- cally, and mental illnesses or psychosis have always been diagnosed for such feelings.
    [Show full text]