Tachykinin Receptors (Version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database
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Nitrate Prodrugs Able to Release Nitric Oxide in a Controlled and Selective
Europäisches Patentamt *EP001336602A1* (19) European Patent Office Office européen des brevets (11) EP 1 336 602 A1 (12) EUROPEAN PATENT APPLICATION (43) Date of publication: (51) Int Cl.7: C07C 205/00, A61K 31/00 20.08.2003 Bulletin 2003/34 (21) Application number: 02425075.5 (22) Date of filing: 13.02.2002 (84) Designated Contracting States: (71) Applicant: Scaramuzzino, Giovanni AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU 20052 Monza (Milano) (IT) MC NL PT SE TR Designated Extension States: (72) Inventor: Scaramuzzino, Giovanni AL LT LV MK RO SI 20052 Monza (Milano) (IT) (54) Nitrate prodrugs able to release nitric oxide in a controlled and selective way and their use for prevention and treatment of inflammatory, ischemic and proliferative diseases (57) New pharmaceutical compounds of general effects and for this reason they are useful for the prep- formula (I): F-(X)q where q is an integer from 1 to 5, pref- aration of medicines for prevention and treatment of in- erably 1; -F is chosen among drugs described in the text, flammatory, ischemic, degenerative and proliferative -X is chosen among 4 groups -M, -T, -V and -Y as de- diseases of musculoskeletal, tegumental, respiratory, scribed in the text. gastrointestinal, genito-urinary and central nervous sys- The compounds of general formula (I) are nitrate tems. prodrugs which can release nitric oxide in vivo in a con- trolled and selective way and without hypotensive side EP 1 336 602 A1 Printed by Jouve, 75001 PARIS (FR) EP 1 336 602 A1 Description [0001] The present invention relates to new nitrate prodrugs which can release nitric oxide in vivo in a controlled and selective way and without the side effects typical of nitrate vasodilators drugs. -
Use and Cardiovascular Safety of Transdermal and Other Granisetron Preparations in Cancer Management
Cancer Management and Research Dovepress open access to scientific and medical research Open Access Full Text Article REVIEW Use and cardiovascular safety of transdermal and other granisetron preparations in cancer management 1 Jay W Mason Abstract: 5-HT3 antagonists have been available as oral and intravenous preparations for Thomas E Moon2 decades. The availability more recently of transdermal granisetron and the anticipated availability of a subcutaneous granisetron preparation have provided helpful alternatives to patients, and 1School of Medicine, University of Utah, Salt Lake City, UT, these preparations have been shown to have less potential to prolong QT than other drugs in 2Tarizona eHealth Services, Inc, the class. Emeryville, CA, USA Keywords: chemotherapy-induced nausea, vomiting, granisetron, QT prolongation Introduction Problem of chemotherapy-induced nausea and vomiting For personal use only. Chemotherapy-induced nausea and vomiting (CINV) occurs in 10%–90% of patients, depending on the emetic risk of the chemotherapeutic agent.1,2 There is a consider- able cost involved, not only for the expense of hospitalization and the direct treatment of CINV, but also because of the loss of workdays and the consequences of delayed 3–7 chemotherapy administration. There is consistent evidence that 5-HT3 antagonist antiemetic therapy has improved this problem without increasing the cost.3–7 Unmet needs in CINV treatment Delayed nausea and vomiting occurring hours or days after chemotherapy, either as a result of reduced plasma concentrations -
Tachykinins and Airway Microvascular Leakage Induced by Hcl Intra-Oesophageal Instillation
Copyright #ERS Journals Ltd 2002 Eur Respir J 2002; 20: 268–273 European Respiratory Journal DOI: 10.1183/09031936.02.00250902 ISSN 0903-1936 Printed in UK – all rights reserved Tachykinins and airway microvascular leakage induced by HCl intra-oesophageal instillation S. Daoui*,B.D9Agostino#, L. Gallelli#, X. Emonds Alt}, F. Rossi#, C. Advenier* Tachykinins and airway microvascular leakage induced by HCl intra-oesophageal *Dept of Pharmacology, University instillation. S. Daoui, B. D9Agostino, L. Gallelli, X. Emonds Alt, F. Rossi, C. Advenier. Paris V, Paris, France, #Dept of #ERS Journals Ltd 2002. Experimental Medicine, Faculty of ABSTRACT: Gastro-oesophageal reflux is a common clinical disorder associated with Medicine and Surgery, Naples, Italy, }Sanofi Synthelabo Research, Montpel- a variety of respiratory symptoms, including chronic cough and exacerbation of asthma. lier, France. In this study, the potential role of acid-induced tachykinin release was examined in guinea pigs and rabbits, by examining the effects of the tachykinin NK1 and NK3 Correspondence: C. Advenier receptors antagonists (SR 140333 and SR 142801, respectively) (1–10 mg?kg-1)on Universite´ Paris V plasma protein extravasation induced in airways by hydrochloric acid (HCl) infusion in UPRES EA220, Pharmacologie the oesophagus. 45 rue des Saints Pe`res Guinea pigs were anaesthetised with urethane, while rabbits were subject to F-75006 Paris neuroleptoanalgesia with hypnorm. Airway vascular leakage was evaluated by France Fax: 33 142863810 measuring extravasation of Evans blue dye. All animals were pretreated with atropine E-mail: [email protected] (1 mg?kg-1 i.p.), propranolol (1 mg?kg-1 i.p.), phosphoramidon (2.5 mg?kg-1 i.v.) and -1 saline or tachykinin receptor antagonists (1–10 mg?kg i.p.). -
In February 2013, Glaxosmithkline (GSK) Announced a Commitment To
In February 2013, GlaxoSmithKline (GSK) announced a commitment to further clinical transparency through the public disclosure of GSK Clinical Study Reports (CSRs) on the GSK Clinical Study Register. The following guiding principles have been applied to the disclosure: Information will be excluded in order to protect the privacy of patients and all named persons associated with the study Patient data listings will be completely removed* to protect patient privacy. Anonymized data from each patient may be made available subject to an approved research proposal. For further information please see the Patient Level Data section of the GSK Clinical Study Register. Aggregate data will be included; with any direct reference to individual patients excluded *Complete removal of patient data listings may mean that page numbers are no longer consecutively numbered CONFIDENTIAL HM2009/00361/00HM2009/00361/00 TheThe GlaxoSmithKline GlaxoSmithKline group group of companies of companies NKP106254 Division: Worldwide Development Retention Category: GRS019 Information Type: Clinical Pharmacology Study Report Title: Randomised, double-blind, placebo controlled, cross-over study comparing the effects of both single dose and repeated dosing treatment for 14 days of vestipitant or vestipitant + paroxetine combination in an enriched population of subjects with tinnitus & hearing loss. Phase: II Compound Number: GW597599 Effective Date: 10-DEC-2009 Description: Tinnitus associated with hearing loss is a high prevalent audiologic disorder with important unmet needs as far as therapy is concerned. The present study explored the possible beneficial effects on tinnitus loudness or annoyance of a combination drug treatment aimed to increase the local inhibitory activity of neural circuitries involved in sound perception and generation. -
( 12 ) United States Patent
US009974742B2 (12 ) United States Patent (10 ) Patent No. : US 9 , 974 , 742 B2 Ottoboni et al. (45 ) Date of Patent: * May 22, 2018 ( 54 ) EMULSION FORMULATIONS OF AN NK - 1 2013 /0236501 A1 * 9 /2013 Booth . .. .. .. A61K 9 /0019 424 / 400 RECEPTOR ANTAGONIST AND USES 2013 /0317016 AL 11 /2013 Hingorani et al. THEREOF 2016 / 0024092 Al 1 / 2016 Wan et al. 2016 / 0082013 Al 3 / 2016 Ottoboni et al . @(71 ) Applicant : Heron Therapeutics , Inc. , Redwood 2016 /0206622 A1 3 / 2016 Ottoboni et al . City , CA (US ) 2017 / 0112847 AL 4 /2017 Ottoboni et al. @(72 ) Inventors : Thomas B . Ottoboni, Belmont, CA (US ) ; Han Han , Mountain View , CA FOREIGN PATENT DOCUMENTS (US ) CN 102379 * 3 / 2012 CN 102379845 A 3 / 2012 @(73 ) Assignee : Heron Therapeutics, Inc. , San Diego , WO WO 2005 /016308 AL 2 / 2005 WO WO 2009 / 124756 AL 10 / 2009 CA (US ) WO WO 2011 / 158053 AL 12 / 2011 WO WO 2013 / 177501 A2 11 / 2013 @( * ) Notice : Subject to any disclaimer , the term of this WO WO 2014 /0209962 AL 12 /2014 patent is extended or adjusted under 35 WO WO 2014 /005606 AL 3 / 2016 U . S . C . 154 ( b ) by 0 days . days . WO WO 2016 /044784 Al 3 / 2016 This patent is subject to a terminal dis claimer . OTHER PUBLICATIONS (21 ) Appl. No. : 15 /012 , 532 Cassileth et al. in Arch . Intern Med . 1983 ; 143 ( 7 ) : 1347 - 1349 ( Abstract ) . * Dexamethasone Hydrogen Phosphate at web .archive . org/ web / ( 22 ) Filed : Feb . 1 , 2016 20141224130045 /http :/ /www . drugs . com / pro / dexamethasone -so dium -phosphate .html ( retrieved on the internet Mar. -
Selective Blockade of NK2 Or NK3 Receptors Produces Anxiolytic- and Antidepressant-Like Effects in Gerbils ⁎ N
Pharmacology, Biochemistry and Behavior 83 (2006) 533–539 www.elsevier.com/locate/pharmbiochembeh Selective blockade of NK2 or NK3 receptors produces anxiolytic- and antidepressant-like effects in gerbils ⁎ N. Salomé, J. Stemmelin, C. Cohen , G. Griebel Sanofi-Aventis, Department of Psychopharmacology, 31 av Paul Vaillant-Couturier, 92220 Bagneux, France Received 17 October 2005; received in revised form 1 March 2006; accepted 9 March 2006 Available online 19 April 2006 Abstract There is a growing interest in the potential anxiolytic- and antidepressant-like effects of compounds that target neurokinin receptors. Since the structure and the pharmacology of the human neurokinin receptor resembles that of gerbils, rather than that of mice or rats, we decided to investigate the anxiolytic- and /or antidepressant-like effects of NK1 (SSR240600), NK2 (saredutant) and NK3 (osanetant) receptor antagonists in gerbils. It was found that saredutant (3–10 mg/kg, p.o.) and osanetant (3–10 mg/kg, p.o.) produced anxiolytic-like effects in the gerbil social interaction test. These effects were similar to those obtained with the V1b receptor antagonist SSR149415 (3–10 mg/kg, p.o.), diazepam (1 mg/kg, p.o.) and buspirone (10 mg/kg, p.o.). Fluoxetine and SSR240600 were devoid of effects in this test. In the tonic immobility test in gerbils, saredutant (5–10 mg/kg, i.p.) and osanetant (5–10 mg/kg, i.p.) produced similar effects to those observed with fluoxetine (7.5–15 mg/kg, i.p.), SSR149415 (10–30 mg/kg, p.o.) and buspirone (3 mg/kg, i.p.). Diazepam and SSR240600 were inactive in this paradigm. -
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. -
CDR Clinical Review Report for Akynzeo
CADTH COMMON DRUG REVIEW Clinical Review Report Netupitant/Palonosetron 300 mg/0.5 mg (Akynzeo) (Purdue Pharma) Indication: In combination with dexamethasone, once- per-cycle treatment for the prevention of acute and delayed nausea and vomiting associated with highly emetogenic cancer chemotherapy, or with moderately emetogenic cancer chemotherapy that is uncontrolled by a 5-hydroxytryptamine-3 receptor antagonist alone. Service Line: CADTH Common Drug Review Version: Final Publication Date: June 2018 Report Length: 96 Pages Disclaimer: The information in this document is intended to help Canadian health care decision-makers, health care professionals, health systems leaders, and policy-makers make well-informed decisions and thereby improve the quality of health care services. While patients and others may access this document, the document is made available for informational purposes only and no representations or warranties are made with respect to its fitness for any particular purpose. The information in this document should not be used as a substitute for professional medical advice or as a substitute for the application of clinical judgment in respect of the care of a particular patient or other professional judgment in any decision-making process. The Canadian Agency for Drugs and Technologies in Health (CADTH) does not endorse any information, drugs, therapies, treatments, products, processes, or services. While care has been taken to ensure that the information prepared by CADTH in this document is accurate, complete, and up-to-date as at the applicable date the material was first published by CADTH, CADTH does not make any guarantees to that effect. CADTH does not guarantee and is not responsible for the quality, currency, propriety, accuracy, or reasonableness of any statements, information, or conclusions contained in any third-party materials used in preparing this document. -
Neurokinin Receptor NK Receptor
Neurokinin Receptor NK receptor There are three main classes of neurokinin receptors: NK1R (the substance P preferring receptor), NK2R, and NK3R. These tachykinin receptors belong to the class I (rhodopsin-like) G-protein coupled receptor (GPCR) family. The various tachykinins have different binding affinities to the neurokinin receptors: NK1R, NK2R, and NK3R. These neurokinin receptors are in the superfamily of transmembrane G-protein coupled receptors (GPCR) and contain seven transmembrane loops. Neurokinin-1 receptor interacts with the Gαq-protein and induces activation of phospholipase C followed by production of inositol triphosphate (IP3) leading to elevation of intracellular calcium as a second messenger. Further, cyclic AMP (cAMP) is stimulated by NK1R coupled to the Gαs-protein. The neurokinin receptors are expressed on many cell types and tissues. www.MedChemExpress.com 1 Neurokinin Receptor Antagonists, Agonists, Inhibitors, Modulators & Activators Aprepitant Befetupitant (MK-0869; MK-869; L-754030) Cat. No.: HY-10052 (Ro67-5930) Cat. No.: HY-19670 Aprepitant (MK-0869) is a selective and Befetupitant is a high-affinity, nonpeptide, high-affinity neurokinin 1 receptor antagonist competitive tachykinin 1 receptor (NK1R) with a Kd of 86 pM. antagonist. Purity: 99.67% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg Size: 1 mg, 5 mg Biotin-Substance P Casopitant mesylate Cat. No.: HY-P2546 (GW679769B) Cat. No.: HY-14405A Biotin-Substance P is the biotin tagged Substance Casopitant mesylate (GW679769B) is a potent, P. Substance P (Neurokinin P) is a neuropeptide, selective, brain permeable and orally active acting as a neurotransmitter and as a neurokinin 1 (NK1) receptor antagonist. -
(12) United States Patent (10) Patent No.: US 9.446,029 B2 Boscan Et Al
USOO9446O29B2 (12) United States Patent (10) Patent No.: US 9.446,029 B2 BOScan et al. (45) Date of Patent: Sep. 20, 2016 (54) USE OF NK-1 RECEPTOR ANTAGONISTS IN GB 2216529 10, 1989 MANAGEMENT OF VISCERAL PAIN WO 9102745 A1 3, 1991 WO 911226.6 A1 8, 1991 (75) Inventors: Pedro Boscan, Bellvue, CO (US); WO O11801.6 A1 3, 2001 David Twedt, Fort Collins, CO (US) OTHER PUBLICATIONS (73) Assignee: Colorado State University Research Glerum et al. (Veterinary Surgery, 30, 351-358, 2001).* Foundation, Fort Collins, CO (US) Devitt et al. (JAVMA, 227, 6, Sep. 15, 2005).* Papich (Veterinary Pharmacology and Therapeutics, Ninth Edition, (*) Notice: Subject to any disclaimer, the term of this 2009, p. 1247-1272, editors: Jim E. Riviere Mark G. Papich).* patent is extended or adjusted under 35 Bradesi et al. (Gastroenterology, 2006, 130, 1729-1742).* U.S.C. 154(b) by 452 days. Heard, D.J. et al. Effect of acepromazine on the anesthetic require ment of halothane in the dog, AJVR, 1986, pp. 2113-2115, vol. 47. (21) Appl. No.: 13/192.283 No. 10. Hellyer, P.W. et al. Effects of diazepam and flumazenil on minimum alveolar concentrations for dogs anesthetized with isoflurane or a (22) Filed: Jul. 27, 2011 combination of isoflurane and fentanyl, AJVR, 2001, pp. 555-560, (65) Prior Publication Data vol. 62, No. 4. Muir, W.W. III, et al. Effects of morphine, lidocaine, ketamine, and US 2012/002898O A1 Feb. 2, 2012 morphine-lidocaine-ketamine drug combination on minimum alveolar concentration in dogs anesthetized with isoflurane, AJVR, Related U.S. -
Use and Cardiovascular Safety of Transdermal and Other Granisetron Preparations in Cancer Management
Cancer Management and Research Dovepress open access to scientific and medical research Open Access Full Text Article REVIEW Use and cardiovascular safety of transdermal and other granisetron preparations in cancer management 1 Jay W Mason Abstract: 5-HT3 antagonists have been available as oral and intravenous preparations for Thomas E Moon2 decades. The availability more recently of transdermal granisetron and the anticipated availability of a subcutaneous granisetron preparation have provided helpful alternatives to patients, and 1School of Medicine, University of Utah, Salt Lake City, UT, these preparations have been shown to have less potential to prolong QT than other drugs in 2Tarizona eHealth Services, Inc, the class. Emeryville, CA, USA Keywords: chemotherapy-induced nausea, vomiting, granisetron, QT prolongation Introduction Problem of chemotherapy-induced nausea and vomiting For personal use only. Chemotherapy-induced nausea and vomiting (CINV) occurs in 10%–90% of patients, depending on the emetic risk of the chemotherapeutic agent.1,2 There is a consider- able cost involved, not only for the expense of hospitalization and the direct treatment of CINV, but also because of the loss of workdays and the consequences of delayed 3–7 chemotherapy administration. There is consistent evidence that 5-HT3 antagonist antiemetic therapy has improved this problem without increasing the cost.3–7 Unmet needs in CINV treatment Delayed nausea and vomiting occurring hours or days after chemotherapy, either as a result of reduced plasma concentrations