Characterization of Putative 5-HT7 Receptors Mediating Tachycardia in the Cat
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TABLE 1 Studies of Antagonist Activity in Constitutively Active
TABLE 1 Studies of antagonist activity in constitutively active receptors systems shown to demonstrate inverse agonism for at least one ligand Targets are natural Gs and constitutively active mutants (CAM) of GPCRs. Of 380 antagonists, 85% of the ligands demonstrate inverse agonism. Receptor Neutral Antagonist Inverse Agonist Reference Human β2-adrenergic Dichloroisoproterenol, pindolol, labetolol, timolol, Chidiac et al., 1996; Azzi et alprenolol, propranolol, ICI 118,551, cyanopindolol al., 2001 Turkey erythrocyte β-adrenergic Propranolol, pindolol Gotze et al., 1994 Human β2-adrenergic (CAM) Propranolol Betaxolol, ICI 118,551, sotalol, timolol Samama et al., 1994; Stevens and Milligan, 1998 Human/guinea pig β1-adrenergic Atenolol, propranolol Mewes et al., 1993 Human β1-adrenergic Carvedilol CGP20712A, metoprolol, bisoprolol Engelhardt et al., 2001 Rat α2D-adrenergic Rauwolscine, yohimbine, WB 4101, idazoxan, Tian et al., 1994 phentolamine, Human α2A-adrenergic Napthazoline, Rauwolscine, idazoxan, altipamezole, levomedetomidine, Jansson et al., 1998; Pauwels MPV-2088 (–)RX811059, RX 831003 et al., 2002 Human α2C-adrenergic RX821002, yohimbine Cayla et al., 1999 Human α2D-adrenergic Prazosin McCune et al., 2000 Rat α2-adrenoceptor MK912 RX821002 Murrin et al., 2000 Porcine α2A adrenoceptor (CAM- Idazoxan Rauwolscine, yohimbine, RX821002, MK912, Wade et al., 2001 T373K) phentolamine Human α2A-adrenoceptor (CAM) Dexefaroxan, (+)RX811059, (–)RX811059, RS15385, yohimbine, Pauwels et al., 2000 atipamezole fluparoxan, WB 4101 Hamster α1B-adrenergic -
Anti-Migraine Agents Reference Number: OH.PHAR.PPA.34 Effective Date: 01.01.21 Last Review Date: 11.20 Line of Business: Medicaid
Clinical Policy: Anti-Migraine Agents Reference Number: OH.PHAR.PPA.34 Effective Date: 01.01.21 Last Review Date: 11.20 Line of Business: Medicaid See Important Reminder at the end of this policy for important regulatory and legal information. Description • When using a preferred agent where applicable, the number of tablets/doses allowed per month will be restricted based on the manufacturer’s package insert and/or Buckeye Health plans quantity limits. CNS AGENTS: ANTI-MIGRAINE AGENTS – ACUTE MIGRANE TREATMENT NO PA REQUIRED “PREFERRED” STEP THERAPY REQUIRED PA REQUIRED “NON-PREFERRED” “PREFERRED” NARATRIPTAN (GENERIC OF AMERGE®) NURTEC™ ODT (rimegepant) ALMOTRIPTAN (generic of Axert®) RIZATRIPTAN TABLETS (GENERIC OF CAFERGOT® (ergotamine w/caffeine) MAXALT®) ELETRIPTAN (generic of Relpax®) RIZATRIPTAN ODT (GENERIC OF ERGOMAR® (ergotamine) MAXALT-MLT®) FROVA® (frovatriptan) SUMATRIPTAN TABLETS, NASAL SPRAY, MIGERGOT® (ergotamine w/caffeine) INJECTION (GENERIC OF MIGRANAL® (dihydroergotamine) IMITREX®) ONZETRA™ XSAIL™ (sumatriptan) REYVOW™ (lasmiditan) SUMAVEL DOSEPRO® (sumatriptan) TOSYMRA® (sumatriptan) TREXIMET® (sumatriptan/naproxen) UBRELVY™ (ubrogepant)* ZOLMITRIPTAN (generic of Zomig®) ZOLMITRIPTAN ODT (generic of Zomig ZMT®) ZOMIG® NASAL SPRAY (zolmitriptan) CNS AGENTS: ANTI-MIGRAINE AGENTS – CLUSTER HEADACHE TREATMENT NO PA REQUIRED “PREFERRED” PA REQUIRED “NON-PREFERRED” VERAPAMIL (Generic of Calan®) EMGALITY™ (galcanezumab) VERAPAMIL SR/ER (Generic of Calan SR®, Isoptin SR®, Verelan®) CNS AGENTS: ANTI-MIGRAINE AGENTS – PROPHYLAXIS TREATMENT NO PA REQUIRED “PREFERRED” STEP THERAPY REQUIRED PA REQUIRED “NON-PREFERRED” (Trials of at least 3 controller “PREFERRED” medications) Cardiovascular Agents: Beta-blockers AIMOVIG™ (erenumab-aooe) † EMGALITY™ (galcanezumab) CNS Agents: Anticonvulsants AJOVY™ (fremanezumab-vfrm) * CNS Agents: Serotonin-norepinephrine reuptake inhibitors CNS Agents: Tricyclic antidepressants †Initial Dose is limited to 70mg once monthly; may request dose increase if 70mg fails to provide adequate relief over two consecutive months. -
Evidence That Mcpp May Have Behavioural Effects Mediated by Central 5-Ht1c Receptors 1G.A
Br. J. Pharmacol. (1988), 94, 137-147 Evidence that mCPP may have behavioural effects mediated by central 5-HT1c receptors 1G.A. Kennett & G. Curzon Department of Neurochemistry, Institute of Neurology, Queen Square, London WC1N 3BG 1 The effects of 1-(3-chlorophenyl)piperazine (mCPP) and 1-[3-(trifluoromethyl)phenyl] piperazine (TFMPP) on activity of rats in a novel cage, and on the rotorod and elevated bar co-ordination tests was examined. 2 Peripherally administered mCPP and TFMPP dose-dependently reduced locomotion, rearing, and feeding scores but not grooming of freely fed rats placed in a novel observation cage. Yawning behaviour was increased. Similar effects were also observed after injection of mCPP into the 3rd ventricle. 3 Co-ordination on a rotating drum of both untrained and trained rats was impaired following mCPP but co-ordination on an elevated bar was not. 4 The hypoactivity induced by mCPP was opposed by three antagonists with high affinity for the 5-hydroxytryptamine (5-HT1c) site; metergoline, mianserin, cyproheptadine and possibly also by a fourth antagonist mesulergine. Metergoline, mianserin and cyproheptadine also opposed the reduction in feeding scores. However, neither effect of mCPP was antagonized by the 5-HT2-receptor antagonists ketanserin or ritanserin, the 5-HT3-receptor antagonist ICS 205-930, the 5-HTlA and 5-HTIB-receptor antagonists (-)-pindolol, (-)-propranolol and (±)-cyanopindolol or the 5-HTIA-, 5-HT2- and dopamine receptor antagonist spiperone. The specific a2-adrenoceptor antagonist idazoxan was also without effect. 5 Hypoactivity induced by TFMPP was similarly antagonized by mianserin but unaffected by (±+-cyanopindolol. 6 These results suggest that the hypoactivity is mediated by central 5-HT1c-receptors and that mCPP and possibly TFMPP may be 5-HT1c-receptor agonists. -
Vascular Effects of Nitric Oxide the Relation to Migraine ISBN 90-9009713-9 NUGI 7411746
Vascular effects of nitric oxide the relation to migraine ISBN 90-9009713-9 NUGI 7411746 Printing by: WRidderprint Offsetdrnkkerij b.v., Ridderkerk, The Netherlands © E.M. van Gelderen 1996 All rights reserved. Save exceptions by the law, no patt of this publication may be reproduced, stored in a retrieval system of any nature, or transmitted in any form or by means, electronic, mechanical, photocopying, recording or othenvise, including a complete or pattial transcription, without the prior written permission of the author, or where appropriate, of the publishers of the atticles. Vascular Effects of Nitric Oxide The Relation to Migraine De vasculaire effecten van stikstof oxide de relatie met migraine Proefschrift ter verkrijging van de graad van Doctor aan de Erasmus Universiteit Rotterdam op gezag van de Rector Magnificus Prof. Dr. P.W.C. AKKERMANS MA en volgens het besluit van het College van Promoties De openbare verdediging zal plaats vinden op woensdag 18 september 1996 om 11.45 uur door Eduard Marcel van Gelderen geboren te Rotterdam Promotiecommissie Promotor: Prof. Dr. P.R. Saxena Overige leden: Prof. Dr. AJ. Man in 't Veld Prof. Dr. F.P. Nijkamp Prof. Dr. P.D. Verdouw Prof. Dr. P.A. van Zwieten Dr. M.D. Ferrari Dr. P.l Koudstaal This thesis was prepared at the Department of Pharmacology of the Erasmus University Rotterdam, P.O.Box 1738, 3000 DR Rotterdam, The Netherlands Tel' nagedachtenis aan mijn vader Vaal' Saskia, Kimberley en Felix Table of contents page Chapter 1. General introduction 11 1.1 Pathophysiology of migraine 1.2 Local regulation of vascular tone; endothelium-derived factors 1.3 Aims of the thesis Chapter 2. -
Biased Ligands Differentially Shape the Conformation of The
International Journal of Molecular Sciences Article Biased Ligands Differentially Shape the Conformation of the Extracellular Loop Region in 5-HT2B Receptors Katrin Denzinger, Trung Ngoc Nguyen, Theresa Noonan, Gerhard Wolber and Marcel Bermudez * Institute of Pharmacy, Freie Universität Berlin, Königin-Luise-Strasse 2-4, 14195 Berlin, Germany; [email protected] (K.D.); [email protected] (T.N.N.); [email protected] (T.N.); [email protected] (G.W.) * Correspondence: [email protected] Received: 22 November 2020; Accepted: 18 December 2020; Published: 20 December 2020 Abstract: G protein-coupled receptors are linked to various intracellular transducers, each pathway associated with different physiological effects. Biased ligands, capable of activating one pathway over another, are gaining attention for their therapeutic potential, as they could selectively activate beneficial pathways whilst avoiding those responsible for adverse effects. We performed molecular dynamics simulations with known β-arrestin-biased ligands like lysergic acid diethylamide and ergotamine in complex with the 5-HT2B receptor and discovered that the extent of ligand bias is directly connected with the degree of closure of the extracellular loop region. Given a loose allosteric coupling of extracellular and intracellular receptor regions, we delineate a concept for biased signaling at serotonin receptors, by which conformational interference with binding pocket closure restricts the signaling repertoire of the receptor. Molecular docking studies of biased ligands gathered from the BiasDB demonstrate that larger ligands only show plausible docking poses in the ergotamine-bound structure, highlighting the conformational constraints associated with bias. This emphasizes the importance of selecting the appropriate receptor conformation on which to base virtual screening workflows in structure-based drug design of biased ligands. -
Skim - a Generalized Literature-Based Discovery System For
bioRxiv preprint doi: https://doi.org/10.1101/2020.10.16.343012; this version posted October 17, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. SKiM - A generalized literature-based discovery system for uncovering novel biomedical knowledge from PubMed Kalpana Raja1, John Steill1, Ian Ross2, Lam C Tsoi3,4,5, Finn Kuusisto1, Zijian Ni6, Miron Livny2, James Thomson1,7 and Ron Stewart1* 1Regenerative Biology, Morgridge Institute for Research, Madison, WI, USA 2Center for High Throughput Computing, Computer Sciences Department, University of Wisconsin, Madison, WI, USA 3Department of Dermatology, University of Michigan Medical School, Ann Arbor, MI, USA 4Department of Computational Medicine & Bioinformatics, University of Michigan, Ann Arbor, MI, USA 5Department of Biostatistics, University of Michigan, Ann Arbor, MI, USA 6Department of Statistics, University of Wisconsin, Madison, WI, USA 7Department of Cell and Regenerative Biology, University of Wisconsin, Madison, WI, USA *Corresponding author Email: [email protected] Phone: (608) 316-4349 Home page: https://morgridge.org/profile/ron-stewart/ bioRxiv preprint doi: https://doi.org/10.1101/2020.10.16.343012; this version posted October 17, 2020. The copyright holder for this preprint (which was not certified by peer review) is the author/funder. All rights reserved. No reuse allowed without permission. Abstract Literature-based discovery (LBD) uncovers undiscovered public knowledge by linking terms A to C via a B intermediate. Existing LBD systems are limited to process certain A, B, and C terms, and many are not maintained. We present SKiM (Serial KinderMiner), a generalized LBD system for processing any combination of A, Bs, and Cs. -
Wednesday, July 10, 2019 4:00Pm
Wednesday, July 10, 2019 4:00pm Oklahoma Health Care Authority 4345 N. Lincoln Blvd. Oklahoma City, OK 73105 The University of Oklahoma Health Sciences Center COLLEGE OF PHARMACY PHARMACY MANAGEMENT CONSULTANTS MEMORANDUM TO: Drug Utilization Review (DUR) Board Members FROM: Melissa Abbott, Pharm.D. SUBJECT: Packet Contents for DUR Board Meeting – July 10, 2019 DATE: July 3, 2019 NOTE: The DUR Board will meet at 4:00pm. The meeting will be held at 4345 N. Lincoln Blvd. Enclosed are the following items related to the July meeting. Material is arranged in order of the agenda. Call to Order Public Comment Forum Action Item – Approval of DUR Board Meeting Minutes – Appendix A Update on Medication Coverage Authorization Unit/SoonerPsych Program Update – Appendix B Action Item – Vote to Prior Authorize Jornay PM™ [Methylphenidate Extended-Release (ER) Capsule], Evekeo ODT™ [Amphetamine Orally Disintegrating Tablet (ODT)], Adhansia XR™ (Methylphenidate ER Capsule), and Sunosi™ (Solriamfetol Tablet) – Appendix C Action Item – Vote to Prior Authorize Balversa™ (Erdafitinib) – Appendix D Action Item – Vote to Prior Authorize Annovera™ (Segesterone Acetate/Ethinyl Estradiol Vaginal System), Bijuva™ (Estradiol/Progesterone Capsule), Cequa™ (Cyclosporine 0.09% Ophthalmic Solution), Corlanor® (Ivabradine Oral Solution), Crotan™ (Crotamiton 10% Lotion), Gloperba® (Colchicine Oral Solution), Glycate® (Glycopyrrolate Tablet), Khapzory™ (Levoleucovorin Injection), Qmiiz™ ODT [Meloxicam Orally Disintegrating Tablet (ODT)], Seconal Sodium™ (Secobarbital -
Ergotamine | Memorial Sloan Kettering Cancer Center
PATIENT & CAREGIVER EDUCATION Ergotamine This information from Lexicomp® explains what you need to know about this medication, including what it’s used for, how to take it, its side effects, and when to call your healthcare provider. Brand Names: US Ergomar Warning Poor blood flow to the hands, feet, or brain has happened when this drug was taken with certain other drugs like clarithromycin, erythromycin, indinavir, itraconazole, ketoconazole, nelfinavir, ritonavir, and troleandomycin. This may be very bad or even deadly. Do not take this drug if you are taking any of these drugs. There are many drugs that can do this. Check to make sure that it is safe for you to take this drug with all of your drugs. What is this drug used for? It is used to treat migraine headaches. What do I need to tell my doctor BEFORE I take this drug? If you are allergic to this drug; any part of this drug; or any other drugs, foods, or substances. Tell your doctor about the allergy and what signs you had. If you have any of these health problems: Blood vessel disease, heart disease, high blood pressure, kidney disease, liver disease, or a very bad infection. If you have taken almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, Ergotamine 1/6 sumatriptan, or zolmitriptan in the last 24 hours. If you are pregnant or may be pregnant. Do not take this drug if you are pregnant. If you are breast-feeding or plan to breast-feed. This is not a list of all drugs or health problems that interact with this drug. -
PRESCRIBED DRUGS and NEUROLOGICAL COMPLICATIONS K a Grosset, D G Grosset Iii2
J Neurol Neurosurg Psychiatry: first published as 10.1136/jnnp.2004.045757 on 16 August 2004. Downloaded from PRESCRIBED DRUGS AND NEUROLOGICAL COMPLICATIONS K A Grosset, D G Grosset iii2 J Neurol Neurosurg Psychiatry 2004;75(Suppl III):iii2–iii8. doi: 10.1136/jnnp.2004.045757 treatment history is a fundamental part of the healthcare consultation. Current drugs (prescribed, over the counter, herbal remedies, drugs of misuse) and how they are taken A(frequency, timing, missed and extra doses), drugs tried previously and reason for discontinuation, treatment response, adverse effects, allergies, and intolerances should be taken into account. Recent immunisations may also be of importance. This article examines the particular relevance of medication in patients presenting with neurological symptoms. Drugs and their interactions may contribute in part or fully to the neurological syndrome, and treatment response may assist diagnostically or in future management plans. Knowledge of medicine taking behaviour may clarify clinical presentations such as analgesic overuse causing chronic daily headache, or severe dyskinesia resulting from obsessive use of dopamine replacement treatment. In most cases, iatrogenic symptoms are best managed by withdrawal of the offending drug. Indirect mechanisms whereby drugs could cause neurological problems are beyond the scope of the current article—for example, drugs which raise blood pressure or which worsen glycaemic control and consequently increase the risk of cerebrovascular disease, or immunosupressants -
Package Leaflet: Information for the Patient Dostinex® 0.5 Mg Tablets
Package leaflet: Information for the patient Dostinex® 0.5 mg Tablets cabergoline Read all of this leaflet carefully before you start taking this medicine because it contains important information for you. - Keep this leaflet. You may need to read it again. - If you have any further questions, ask your doctor or pharmacist. - This medicine has been prescribed for you only. Do not pass it on to others. It may harm them, even if their signs of illness are the same as yours. - If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. See section 4. What is in this leaflet 1. What Dostinex is and what it is used for 2. What you need to know before you take Dostinex 3. How to take Dostinex 4. Possible side effects 5 How to store Dostinex 6. Contents of the pack and other information 1. What Dostinex is and what it is used for - Dostinex contains the active ingredient cabergoline. This medicine belongs to a class of medicines called ‘dopamine agonists’. Dopamine is produced naturally in the body and helps to transmit messages to the brain. - Dostinex is used to stop breast milk production (lactation) soon after childbirth, stillbirth, abortion or miscarriage. It can also be used if you do not want to continue to breast-feed your baby once you have started. - Dostinex can also be used to treat other conditions caused by hormonal disturbance which can result in high levels of prolactin being produced. This includes lack of periods, infrequent and very light menstruation, periods in which ovulation does not occur and secretion of milk from your breast without breast-feeding. -
Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans
molecules Review Molecular and Functional Imaging Studies of Psychedelic Drug Action in Animals and Humans Paul Cumming 1,2,* , Milan Scheidegger 3 , Dario Dornbierer 3, Mikael Palner 4,5,6 , Boris B. Quednow 3,7 and Chantal Martin-Soelch 8 1 Department of Nuclear Medicine, Bern University Hospital, CH-3010 Bern, Switzerland 2 School of Psychology and Counselling, Queensland University of Technology, Brisbane 4059, Australia 3 Department of Psychiatry, Psychotherapy and Psychosomatics, Psychiatric Hospital of the University of Zurich, CH-8032 Zurich, Switzerland; [email protected] (M.S.); [email protected] (D.D.); [email protected] (B.B.Q.) 4 Odense Department of Clinical Research, University of Southern Denmark, DK-5000 Odense, Denmark; [email protected] 5 Department of Nuclear Medicine, Odense University Hospital, DK-5000 Odense, Denmark 6 Neurobiology Research Unit, Copenhagen University Hospital, DK-2100 Copenhagen, Denmark 7 Neuroscience Center Zurich, University of Zurich and Swiss Federal Institute of Technology Zurich, CH-8058 Zurich, Switzerland 8 Department of Psychology, University of Fribourg, CH-1700 Fribourg, Switzerland; [email protected] * Correspondence: [email protected] or [email protected] Abstract: Hallucinogens are a loosely defined group of compounds including LSD, N,N- dimethyltryptamines, mescaline, psilocybin/psilocin, and 2,5-dimethoxy-4-methamphetamine (DOM), Citation: Cumming, P.; Scheidegger, which can evoke intense visual and emotional experiences. We are witnessing a renaissance of re- M.; Dornbierer, D.; Palner, M.; search interest in hallucinogens, driven by increasing awareness of their psychotherapeutic potential. Quednow, B.B.; Martin-Soelch, C. As such, we now present a narrative review of the literature on hallucinogen binding in vitro and Molecular and Functional Imaging ex vivo, and the various molecular imaging studies with positron emission tomography (PET) or Studies of Psychedelic Drug Action in single photon emission computer tomography (SPECT). -
The 5-HT1-Like Receptors Mediating Inhibition of Sympathetic Vasopressor Out¯Ow in the Pithed Rat: Operational Correlation with the 5-HT1A, 5-HT1B and 5-HT1D Subtypes
British Journal of Pharmacology (1998) 124, 1001 ± 1011 1998 Stockton Press All rights reserved 0007 ± 1188/98 $12.00 http://www.stockton-press.co.uk/bjp The 5-HT1-like receptors mediating inhibition of sympathetic vasopressor out¯ow in the pithed rat: operational correlation with the 5-HT1A, 5-HT1B and 5-HT1D subtypes 1,3Carlos M. Villalo n, 1David Centurio n, 1Gonzalo Rabelo, 2Peter de Vries, 2Pramod R. Saxena & 1Araceli Sa nchez-Lo pez 1Seccio n de Terape utica Experimental, Departamento de Farmacologõ a y Toxicologõ a, CINVESTAV, I.P.N., Apdo. Postal 22026, 14000 Me xico D.F., Me xico and 2Department of Pharmacology, Faculty of Medicine and Health Sciences, Erasmus University Rotterdam, P.O. Box 1738, 3000 DR Rotterdam, The Netherlands 1 It has been suggested that the inhibition of sympathetically-induced vasopressor responses produced by 5-hydroxytryptamine (5-HT) in pithed rats is mediated by 5-HT1-like receptors. The present study has re-analysed this suggestion with regard to the classi®cation schemes recently proposed by the NC- IUPHAR subcommittee on 5-HT receptors. 2 Intravenous (i.v.) continuous infusions of 5-HT and the 5-HT1 receptor agonists, 8-OH-DPAT (5-HT1A), indorenate (5-HT1A), CP 93,129 (5-HT1B) and sumatriptan (5-HT1B/1D), resulted in a dose- dependent inhibition of sympathetically-induced vasopressor responses. 3 The sympatho-inhibitory responses induced by 5-HT, 8-OH-DPAT, indorenate, CP 93,129 or sumatriptan were analysed before and after i.v. treatment with blocking doses of the putative 5-HT receptor antagonists, WAY 100635 (5-HT1A), cyanopindolol (5-HT1A/1B) or GR 127935 (5-HT1B/1D).