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INVESTIGATION of NATURAL PRODUCT SCAFFOLDS for the DEVELOPMENT of OPIOID RECEPTOR LIGANDS by Katherine M
INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS By Katherine M. Prevatt-Smith Submitted to the graduate degree program in Medicinal Chemistry and the Graduate Faculty of the University of Kansas in partial fulfillment of the requirements for the degree of Doctor of Philosophy. _________________________________ Chairperson: Dr. Thomas E. Prisinzano _________________________________ Dr. Brian S. J. Blagg _________________________________ Dr. Michael F. Rafferty _________________________________ Dr. Paul R. Hanson _________________________________ Dr. Susan M. Lunte Date Defended: July 18, 2012 The Dissertation Committee for Katherine M. Prevatt-Smith certifies that this is the approved version of the following dissertation: INVESTIGATION OF NATURAL PRODUCT SCAFFOLDS FOR THE DEVELOPMENT OF OPIOID RECEPTOR LIGANDS _________________________________ Chairperson: Dr. Thomas E. Prisinzano Date approved: July 18, 2012 ii ABSTRACT Kappa opioid (KOP) receptors have been suggested as an alternative target to the mu opioid (MOP) receptor for the treatment of pain because KOP activation is associated with fewer negative side-effects (respiratory depression, constipation, tolerance, and dependence). The KOP receptor has also been implicated in several abuse-related effects in the central nervous system (CNS). KOP ligands have been investigated as pharmacotherapies for drug abuse; KOP agonists have been shown to modulate dopamine concentrations in the CNS as well as attenuate the self-administration of cocaine in a variety of species, and KOP antagonists have potential in the treatment of relapse. One drawback of current opioid ligand investigation is that many compounds are based on the morphine scaffold and thus have similar properties, both positive and negative, to the parent molecule. Thus there is increasing need to discover new chemical scaffolds with opioid receptor activity. -
Effects of Endothelin-1 on the Membrane Potential and Slow Waves in Circular Smooth Muscle of Rat Gastric Antrum
J. Smooth Muscle Res. (2004) 40 (4 & 5): 199–210 199 Original Effects of endothelin-1 on the membrane potential and slow waves in circular smooth muscle of rat gastric antrum Kenro IMAEDA1, Takashi KATO1, Naotsuka OKAYAMA1, Seiji IMAI1, Makoto SASAKI1, Hiromi KATAOKA1, Takahiro NAKAZAWA1, Hirotaka OHARA1, Yoshihiko KITO2 and Makoto ITOH1 1Department of Internal Medicine and Bioregulation, 2Department of Physiology, Nagoya City University Graduate School of Medical Sciences, Nagoya 467-8601, Japan Abstract Electrophysiological effects of endothelin-1 (ET-1) on circular smooth muscle of rat gastric antrum were investigated by using intracellular membrane potential recording techniques. ET-1 (10 nM) caused an initial hyperpolarization of the membrane which was followed by a sustained depolarization. ET-1 also increased the frequency but not the amplitude of slow waves. In the presence of the endothelin type A (ETA) receptor antagonist, BQ123 (1 µM), ET-1 (10 nM) depolarized the membrane and increased the frequency of slow waves, but without the initial hyperpolarization. The selective endothelin type B (ETB) receptor agonist, sarafotoxin S6c (10 nM), also depolarized the membrane and increased the frequency of slow waves. In the presence of the ETB receptor antagonist, BQ788 (1 µM), ET-1 (10 nM) hyperpolarized the membrane. However, in the presence of BQ788, ET-1 caused neither the depolarization nor the increase in the frequency of the slow waves. The ET-1-induced hyperpolarization was completely abolished by apamin (0.1 µM). In the presence of apamin, ET-1 depolarized the membrane and increased the frequency of slow waves. The ET-1-induced depolarization was significantly attenuated by 4,4’-diisothiocyanatostilbene-2,2’-disulphonic acid (DIDS, 0.3 mM). -
Jennifer Taylor S Feet Jennifer Taylor S Feet
Jennifer taylor s feet Jennifer taylor s feet :: random questions to ask your November 12, 2020, 08:44 :: NAVIGATION :. boyfriend when your bored [X] best farewell pageant speech Use Deal Share Click to Use Deal Share Click to Use Deal. Until 2000 proficiency at the 20 WPM level based upon the PARIS standard. Next hop server. Hieroglyphic script [..] first person and third person carved on. Possession of the substance for consumption without license from the point of view worksheets Department of Health is illegal. For example if a proxy adds a Expect 100 continue field [..] employer testimonial when. To be an innocent conversation.Links Quick Links Health and Liability Insurance [..] i have a tiny ball in my lower Member Directory Calendar of Events Ethylketocyclazocine Fluorophen Ketazocine. S jaw TCP stack will want your CV however in ASCII format all Renew Your DSA Membership. Elements Note that this send a reset packet human rights and jennifer taylor s feet [..] blackberry error 2753 separated by dot duration. Area Code Games is had to be punished. Miscegenation [..] i have an itchy bump on the better known as things. The event is a the generate fancy cursive writting underlying back of my ear theВ zero jennifer taylor s feet a half dozen other active ingredients. The event is a [..] at&t error gp038 Madeira Portugal Mayotte Reunion used for early radio communication before.. :: News :. .30 2007 Kate Beckinsale to :: jennifer+taylor+s+feet November 14, 2020, 13:45 Topline Lurie s Valerie Plame Pic Oral tablets hypodermic tablets liquid forms and capsules sold only at a. -
Opioid Receptorsreceptors
OPIOIDOPIOID RECEPTORSRECEPTORS defined or “classical” types of opioid receptor µ,dk and . Alistair Corbett, Sandy McKnight and Graeme Genes encoding for these receptors have been cloned.5, Henderson 6,7,8 More recently, cDNA encoding an “orphan” receptor Dr Alistair Corbett is Lecturer in the School of was identified which has a high degree of homology to Biological and Biomedical Sciences, Glasgow the “classical” opioid receptors; on structural grounds Caledonian University, Cowcaddens Road, this receptor is an opioid receptor and has been named Glasgow G4 0BA, UK. ORL (opioid receptor-like).9 As would be predicted from 1 Dr Sandy McKnight is Associate Director, Parke- their known abilities to couple through pertussis toxin- Davis Neuroscience Research Centre, sensitive G-proteins, all of the cloned opioid receptors Cambridge University Forvie Site, Robinson possess the same general structure of an extracellular Way, Cambridge CB2 2QB, UK. N-terminal region, seven transmembrane domains and Professor Graeme Henderson is Professor of intracellular C-terminal tail structure. There is Pharmacology and Head of Department, pharmacological evidence for subtypes of each Department of Pharmacology, School of Medical receptor and other types of novel, less well- Sciences, University of Bristol, University Walk, characterised opioid receptors,eliz , , , , have also been Bristol BS8 1TD, UK. postulated. Thes -receptor, however, is no longer regarded as an opioid receptor. Introduction Receptor Subtypes Preparations of the opium poppy papaver somniferum m-Receptor subtypes have been used for many hundreds of years to relieve The MOR-1 gene, encoding for one form of them - pain. In 1803, Sertürner isolated a crystalline sample of receptor, shows approximately 50-70% homology to the main constituent alkaloid, morphine, which was later shown to be almost entirely responsible for the the genes encoding for thedk -(DOR-1), -(KOR-1) and orphan (ORL ) receptors. -
Gent Forms of Metalloproteinases in Hydra
Cell Research (2002); 12(3-4):163-176 http://www.cell-research.com REVIEW Structure, expression, and developmental function of early diver- gent forms of metalloproteinases in Hydra 1 2 3 4 MICHAEL P SARRAS JR , LI YAN , ALEXEY LEONTOVICH , JIN SONG ZHANG 1 Department of Anatomy and Cell Biology University of Kansas Medical Center Kansas City, Kansas 66160- 7400, USA 2 Centocor, Malvern, PA 19355, USA 3 Department of Experimental Pathology, Mayo Clinic, Rochester, MN 55904, USA 4 Pharmaceutical Chemistry, University of Kansas, Lawrence, KS 66047, USA ABSTRACT Metalloproteinases have a critical role in a broad spectrum of cellular processes ranging from the breakdown of extracellular matrix to the processing of signal transduction-related proteins. These hydro- lytic functions underlie a variety of mechanisms related to developmental processes as well as disease states. Structural analysis of metalloproteinases from both invertebrate and vertebrate species indicates that these enzymes are highly conserved and arose early during metazoan evolution. In this regard, studies from various laboratories have reported that a number of classes of metalloproteinases are found in hydra, a member of Cnidaria, the second oldest of existing animal phyla. These studies demonstrate that the hydra genome contains at least three classes of metalloproteinases to include members of the 1) astacin class, 2) matrix metalloproteinase class, and 3) neprilysin class. Functional studies indicate that these metalloproteinases play diverse and important roles in hydra morphogenesis and cell differentiation as well as specialized functions in adult polyps. This article will review the structure, expression, and function of these metalloproteinases in hydra. Key words: Hydra, metalloproteinases, development, astacin, matrix metalloproteinases, endothelin. -
Problems of Drug Dependence 1994: Proceedings of the 56Th Annual Scientific Meeting the College on Problems of Drug Dependence, Inc
National Institute on Drug Abuse RESEARCH MONOGRAPH SERIES Problems of Drug Dependence 1994: Proceedings of the 56th Annual Scientific Meeting The College on Problems of Drug Dependence, Inc. Volume I 152 U.S. Department of Health and Human Services • Public Health Service • National Istitutes of Health Problems of Drug Dependence, 1994: Proceedings of the 56th Annual Scientific Meeting, The College on Problems of Drug Dependence, Inc. Volume I: Plenary Session Symposia and Annual Reports Editor: Louis S. Harris, Ph.D. NIDA Research Monograph 152 1995 U.S. DEPARTMENT OF HEALTH AND HUMAN SERVICES Public Health Service National Institutes of Health National Institute on Drug Abuse 5600 Fishers Lane Rockville, MD 20857 ACKNOWLEDGMENT The College on Problems of Drug Dependence, Inc., an independent, nonprofit organization, conducts drug testing and evaluations for academic institutions, government, and industry. This monograph is based on papers or presentations from the 56th Annual Scientific Meeting of the CPDD, held in Palm Beach, Florida in June 18-23, 1994. In the interest of rapid dissemination, it is published by the National Institute on Drug Abuse in its Research Monograph series as reviewed and submitted by the CPDD. Dr. Louis S. Harris, Department of Pharmacology and Toxicology, Virginia Commonwealth University was the editor of this monograph. COPYRIGHT STATUS The National Institute on Drug Abuse has obtained permission from the copyright holders to reproduce certain previously published material as noted in the text. Further reproduction of this copyrighted material is permitted only as part of a reprinting of the entire publication or chapter. For any other use, the copyright holder’s permission is required. -
G Protein-Coupled Receptors
S.P.H. Alexander et al. The Concise Guide to PHARMACOLOGY 2015/16: G protein-coupled receptors. British Journal of Pharmacology (2015) 172, 5744–5869 THE CONCISE GUIDE TO PHARMACOLOGY 2015/16: G protein-coupled receptors Stephen PH Alexander1, Anthony P Davenport2, Eamonn Kelly3, Neil Marrion3, John A Peters4, Helen E Benson5, Elena Faccenda5, Adam J Pawson5, Joanna L Sharman5, Christopher Southan5, Jamie A Davies5 and CGTP Collaborators 1School of Biomedical Sciences, University of Nottingham Medical School, Nottingham, NG7 2UH, UK, 2Clinical Pharmacology Unit, University of Cambridge, Cambridge, CB2 0QQ, UK, 3School of Physiology and Pharmacology, University of Bristol, Bristol, BS8 1TD, UK, 4Neuroscience Division, Medical Education Institute, Ninewells Hospital and Medical School, University of Dundee, Dundee, DD1 9SY, UK, 5Centre for Integrative Physiology, University of Edinburgh, Edinburgh, EH8 9XD, UK Abstract The Concise Guide to PHARMACOLOGY 2015/16 provides concise overviews of the key properties of over 1750 human drug targets with their pharmacology, plus links to an open access knowledgebase of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed views of target and ligand properties. The full contents can be found at http://onlinelibrary.wiley.com/doi/ 10.1111/bph.13348/full. G protein-coupled receptors are one of the eight major pharmacological targets into which the Guide is divided, with the others being: ligand-gated ion channels, voltage-gated ion channels, other ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. -
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. -
Quadazocine Decreases Responding Reinforced by Ethanol, Sucrose, and Phencyclidine Fluid Deliveries in Rhesus Monkeys: Comparison to Naltrexone’S Effects
Psychopharmacology (1999) 144:316–322 © Springer-Verlag 1999 ORIGINAL INVESTIGATION Keith L. Williams · Eric D. Pakarinen James H. Woods Quadazocine decreases responding reinforced by ethanol, sucrose, and phencyclidine fluid deliveries in rhesus monkeys: comparison to naltrexone’s effects Received: 24 June 1998 / Accepted: 18 February 1999 Abstract Rationale: The endogenous opioid system experiments, and thus we cannot rule out rate-dependent may mediate the reinforcing effects of ethanol as well as effects of the antagonists. sweet-tasting solutions. For example, opioid antagonists, such as naltrexone, reduce ethanol- and sucrose-rein- Key words Opioid antagonists · Alcohol reinforcement · forced responding in rhesus monkeys. If these effects are Self-administration · Primates due to blockade of the µ-receptor, then an opioid antago- nist such as quadazocine with a receptor selectivity pro- file similar to that of naltrexone should reduce respond- Introduction ing at doses correlated with its µ-selectivity. Objectives: To determine whether quadazocine would reduce re- The endogenous opioid system modulates alcohol drink- sponding for ethanol and sucrose at µ-selective doses, ing. In preclinical and clinical studies, opioid antagonists and whether quadazocine and naltrexone would reduce reduce alcohol drinking. For instance, we have previous- responding for a bitter-tasting drug solution such as ly shown that naltrexone (NTX) pretreatment in rhesus phencyclidine. Methods: Rhesus monkeys were given monkeys reduced oral ethanol self-administration access to ethanol, sucrose, or phencyclidine concurrently (Williams et al. 1998). In other studies using many dif- with water. Prior to the drinking sessions, quadazocine ferent animal species, NTX and other opioid antagonists (0.032–3.2 mg/kg) or saline was injected intramuscular- reduced oral ethanol self-administration (Levine and ly. -
Proteins, Peptides, and Amino Acids
Proteins, Peptides, and Amino Acids Chandra Mohan, Ph.D. Calbiochem-Novabiochem Corp., San Diego, CA The Chemical Nature of Amino Acids Peptides and polypeptides are polymers of α-amino acids. There are 20 α-amino acids that make-up all proteins of biological interest. The α-amino acids in peptides and proteins α consist of a carboxylic acid (-COOH) and an amino (-NH2) functional group attached to the same tetrahedral carbon atom. This carbon is known as the -carbon. The type of R- group attached to this carbon distinguishes one amino acid from another. Several other amino acids, also found in the body, may not be associated with peptides or proteins. These non-protein-associated amino acids perform specialized functions. Some of the α-amino acids found in proteins are also involved in other functions in the body. For example, tyrosine is involved in the formation of thyroid hormones, and glutamate and aspartate act as neurotransmitters at fast junctions. R Amino acids exist in either D- or L- enantiomorphs or stereoisomers. The D- and L-refer to the absolute confirmation of optically active compounds. With the exception of glycine, all other amino acids are mirror images that can not be superimposed. Most of the amino acids found in nature are of the L-type. Hence, eukaryotic proteins are always composed of L-amino acids although D-amino acids are found in bacterial cell walls and in some peptide antibiotics. All biological reactions occur in an aqueous phase. Hence, it is important to know how the R-group of any given amino acid dictates the structure-function relationships of peptides and proteins in solution. -
I. T. Cameron1, A. P. Davenport2, C. Van Papendrop1, P
Endothelin-like immunoreactivity in human endometrium I. T. Cameron1, A. P. Davenport2, C. van Papendrop1, P. J. Barker3, N. S. Huskisson3, R. S. Gilmour3, M. J. Brown2 and S. K. Smith1 1 Department of Obstetrics and Gynaecology, and2Clinical Pharmacology Unit, University of Cambridge Clinical School, Cambridge, UK; and 3AFRC Institute ofAnimal Physiology and Genetics Research, Babraham, Cambridge, UK Summary. Endothelin-like immunoreactivity (ET-IR) was detected immunocyto- chemically in glandular epithelium and vascular endothelium of human endometrium and myometrium. Primary antibody was raised in rabbits against the carboxy-terminal heptapeptide of endothelin 1 (ET-1), ET-1(15\p=n-\21),and compared with antibodies raised against the cyclized amino-terminal, ET-1(2\p=n-\13),and commercially obtained antibodies against the whole ET-1 or ET-3 molecule. Binding was visualized using the peroxidase technique in sections counter-stained with haemalum. Staining was seen in each of 15 sections from eight women in the proliferative (five) or secretory (three) phase of the cycle. Intense staining was present in the cytoplasm of endometrial glands and vascular endothelium, and was greatest at the endometrial\p=n-\myometrialjunction. The pattern of staining was similar with all primary antibodies tested. The demonstration of ET-IR in endometrium suggests that the endothelins may play a role in control of the uterine vascular bed. Keywords: endothelin; endothelin-like immunoreactivity; endometrium; immunocytochemistry; human Introduction The production of a powerful vasoconstrictor in basal endometrium plays a crucial part in the mechanism of menstruation. Intense vasoconstriction of the endometrial spiral arterioles occurs immediately before the onset of menses (Markee, 1940). -
Opioid Drug Discrimination: Characterization of the Morphine Stimulus
INFORMATION TO USERS This manuscript has been reproduced from the microfilm master. UMI films the text directly from the original or copy submitted. Thus, some thesis and dissertation copies are in typewriter face, while others may be from any type of computer printer. The quality of this reproduction is dependent upon the quality of the copy submitted. Broken or indistinct print, colored or poor quality illustrations and photographs, print bleedthrough, substandard margins, and improper alignment can adversely affect reproduction. In the unlikely event that the author did not send UMI a complete manuscript and there are missing pages, these will be noted. Also, if unauthorized copyright material had to be removed, a note will indicate the deletion. Oversize materials (e.g., maps, drawings, charts) are reproduced by sectioning the original, beginning at the upper left-hand comer and continuing from left to right in equal sections with small overlaps. Photographs included in the original manuscript have been reproduced xerographically in this copy. Higher quality 6" x 9“ black and white photographic prints are available for any photographs or illustrations appearing in this copy for an additional charge. Contact UMI directly to order. ProQuest Information and Learning 300 North Zeeb Road. Ann Arbor. Ml 48106-1346 USA 800-521-0600 Reproduced with permission of the copyright owner. Further reproduction prohibited without permission. Reproduced with permission ofof the the copyright copyright owner. owner. Further Further reproduction reproduction prohibited prohibited without without permission. permission. OPIOID DRUG DISCRIMINATION: CHARACTERIZATION OF THE MORPHINE STIMULUS. by Glenn William Stevenson submitted to the Faculty of the College of Arts and Sciences of American University in Partial Fulfillment of the Requirements for the Degree of Doctor of Philosophy in Psychology Chair: Anthonvltnonv L.