DOCSLIB.ORG

A New Specific Histamine-H2-Receptor Agonist R L Mcisaac,* B J JOHNSTON, and L P FIELDING from the Academic Surgical Unit, St

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
A New Specific Histamine-H2-Receptor Agonist R L Mcisaac,* B J JOHNSTON, and L P FIELDING from the Academic Surgical Unit, St Gut: first published as 10.1136/gut.22.7.529 on 1 July 1981. Downloaded from Gut, 1981. 22, 529-533 Gastric mucosal blood flow and acid secretory changes in man with impromidine: a new specific histamine-H2-receptor agonist R L McISAAC,* B J JOHNSTON, AND L P FIELDING From The Academic Surgical Unit, St. Mary's Hospital Medical School, London SUMMARY The effect of impromidine, a new histamine-H2-receptor agonist, on gastric mucosal blood flow (neutral red clearance) and acid secretion was studied in nine volunteers. Impromidine stimulated a dose-dependent increase in neutral red clearance and acid secretion. Simultaneous cimetidine in three doses caused a parallel shift to the right for both acid output and clearance with unchanged maxima compatible with simple surmountable antagonism. There were small cardio- vascular changes: an increased heart rate with a decreased diastolic pressure during infusion of impromidine. These changes were antagonised by cimetidine. The involvement of histamine in the control of was approved by the local ethical committee and gastric acid secretion was supported by the informed written consent was obtained from each discovery of the specific inhibitors of H2-receptors volunteer in accordance with the Declaration of on the parietal cell.' Studies in animals have also Helsinki. Gastric mucosal blood flow was shown that the gastric vasculature is sensitive to measured by the neutral red clearance technique.8 http://gut.bmj.com/ histamine through a combination of Hl- and H2- receptors although with different relative contri- GASTRIC FUNCTION TESTS AND butions.2 3In man histamine stimulates a dose- E S T I M A T I ON O F M U C O S A L B L OO1) dependent increase in both acid secretion and F L O W mucosal blood flow but the blood flow component After an overnight fast each volunteer was is relatively resistant to inhibition by cimetidine.4 intubated with a double lumen nasogastric tube A specific histamine-H,-receptor agonist would be (Sherwood 12-14 French gauge), the position on September 26, 2021 by guest. Protected copyright. of value in the investigation of the role of being determined by a water recovery test.' histamine in the control of gastric acid secretion Overnight secretion was aspirated and discarded. and blood flow in both healthy man and in A 15 minute basal sample was collected as a patients with peptic ulcer disease. Recent studies reference for neutral red standards (see below). have indicated that impromidine is a potent Winged needles were inserted into a vein in each stimulant of gastric secretion in man with forearm; one for drug infusion and the other for relatively fewer side-effects than histamine." 6 blood sampling. A 15 ml venous sample was taken The purpose of the present investigation was to for processing of neutral red standards in whole study the stimulation of acid secretion and blood blood and then a loading dose of neutral red (NR, flow in healthy volunteers using increasing doses 125 gg/kg) was given followed by a constant in- of impromidine and to compare these effects with fusion (250 ,g/kg per h). Blood samples were taken our previous results using histamine.4 at 15 minute intervals for 45 minutes and then at 30 minute intervals thereafter. After a basal Methods period (45 minutes) gastric acid secretion was stimulated by an infusion of impromidine. Dose- In the study group there were nine volunteers, response curves were constructed on two separate mean age 22 years (range 21-26 years). The study days at least one week apart. On day one, *Address for correspondence: Dr R L Mcisaac, Academic Surgical impromidine was given in four sequential doses Unit, St. Mary's Hospital Medical School, London W2 1 PG. (125, 2.5, 5*0, and 10 ig/kg per h) each for one Received for publication 11 December 1980 hour (Fig. 1). Two volunteers received impromi- 529 Gut: first published as 10.1136/gut.22.7.529 on 1 July 1981. Downloaded from 53 Mc!saac, Johnston, and Fielding 600 60 .E a-- mm -- - - - - - m- - - - -- -------- . *~ f E- 500 00. 50 T ,o n =2) E 0 400 40 0 1 z E (n-2) 0 300 I- ° 30 U 200 /1 0 OK I- 20 t z T11T2;(=s 100 1 i itn=S) 10 [ -L 'F , I 0 -," . 0 B 1.25 2.5 5.0 10 20 40 80 B 1.25 2.5 5.0 10 20 40 80 Impromidine pjg/kg.h Impromidine pg/kg-h Fig. I Mean (: S E M ) a(id output ini volunteers durinig infiision ol graded doses of inpromidine ( 125-20 Fig. 2 Mean ( t S E M) neutral red clearance in the pg/kgper h). Baval secretion (B) 5444;13 3 pmpioll/nin has same volunteers as in Fig. 1. Basal NRC (B) 20 :t4*3 been subtracted. Tte theoretical maximunm was mIl/min has been subtracted. The calculated maximum calculated to be 530 4 -605 pmol/min and is shown by was 56 1 9-6 ml/min and is shown by the dotted line. the dotted line. (ED,,) and an inhibitory dose,,, (ID,,,) for cime- dine in the dose range 2-5-20 gg/kg per h. On day tidine. Standard errors for these calculations were two, the test was repeated with cimetidine (0 25, also derived from the least squares fit. 0.5, or 1[0 mg/kg) which was randomised among Blood pressure and heart rate were measured three groups of the volunteers (three, three, and electronically by inflating a cuff around the arm two volunteers respectively). The infusion of over the brachial artery (Digital 8000, Ueda cimetidine was begun 30 minutes before Electronics Ltd) and changes were analysed by impromidine (dose-range 5-80 gg/kg per h). means of Student's paired t test. http://gut.bmj.com/ Gastric juice was collected every 10 minutes. The volume of the aspirate was recorded and the Results concentration of H' measured by titration of 3 ml gastric juice to pH 7.0 with 0 1M NaOH using an I M P R O M I I) I N E 1) 0 S E - R E S P O N S E automatic titrator (Radiometer, Copenhagen). S T U I) I E S Acid secretion was expressed as gmol H+/min. Impromidine (1-25-10 Mg/kg per h) caused a NR concentration was determined in 3 ml blood dcse-dependent increase in both acid output and on September 26, 2021 by guest. Protected copyright. and 1 ml gastric juice after alkalinisation and NRC (Figs t and 2). In the two volunteers who extraction into diethyl ether (10 ml Analar grade, received an infusion of impromidine 20 ag/kg BDH Ltd) with further extraction into 0-1M per h, this dose caused a small increase in acid HCI. The aqueous layer was read in a spectro- output above that induced by 10 1Mg/kg per h, photometer (Pye-Unicam SP 1800) at 540 nm but NRC at the high dose began to decrease. against serial standards of NR made up in whole The best fit curves for these data give the follow- blood or gastric juice and processed along with ing calculated values (omitting the data for 20 the samples. Neutral red clearance (NRC) in Mg/kg per h). Maximal acid ouput was 530+60.5 mI/min was calculated from the equation NCR= (SEM) gumol H+/min and the ED>,, 2.3±0.26 (NR). xxV/(NR)h, where (NR). and (NR)b are M£g/kg per h. For NRC the calculated maximal gastric and whole blood concentrations of NR rate was 56+9-6 ml/min and the ED5,,, 1l7+0.34 and V is the volume of gastric aspirate in ml/min. Mg/kg per h. Dose-response curves were constructed using the mean of the last two 10 minute periods at EFFECT OF CIM ETI DINE ON each dose level of impromidine. The data were I M P R 0 M II) I N E- I N I) L' C E I) A C II) used to fit non-linear curves by the method of SECRETION AND NRC: COMk1PARISON least squares"' so as to calculate a best fit maxi- WITH PREVIOUS H ISTAMI NE DATA mum for acid secretion and NCR as well as In a previous study. cimetidine (06 mg/kg per obtaining calculated values for the dose of h) reduced acid secretion induced by histanmine imnromidine lroducing a half-maximal response but had no effect on neutral red clearance.4 Gut: first published as 10.1136/gut.22.7.529 on 1 July 1981. Downloaded from Impromidine and gastric blood flow 531 600 150 ._E E impromidline -. 500 r2= .57 0 E Y -.14X * 23 400 100 [ C * E 30 : ' * ' A A 0. E 300 1, A U C A CA a A C &* ,AA z 0 200 so g, 6A AA * histamine A An, #A A .61 AAA r2yy~ .1ox - 1g AA A 100 A A 0 0 1.25 2.5 5.0 10 20 40 500 1000 Impromidine pg/kg h ACID output pmol/min Fig. 3 The effect or cimetidine given in three doses Fig. 4 Comparison of the acid secretory and NRC 025(E),05( A), and 1-0( *) mg/kgperh on impromidine- responses during infusion ofgraded doses ofhistamine induced gastric acid secretion. The calculated ID50 for (A) and impromidine (*). The calculated regression cimetidine inhibition was 0-10 0014 mg/kg per h. line for histamine was Y=0 IOX - 19, r2=0-61, n=38 (p < 0001) andfor impromidine Y=0-14X -23, In the present study cimetidine caused a parallel, r2-0-57, n =44 (p <0O00J).
Load more

Recommended publications
  • )&F1y3x PHARMACEUTICAL APPENDIX to THE
    )&f1y3X PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE )&f1y3X PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 3 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. Product CAS No. Product CAS No. ABAMECTIN 65195-55-3 ACTODIGIN 36983-69-4 ABANOQUIL 90402-40-7 ADAFENOXATE 82168-26-1 ABCIXIMAB 143653-53-6 ADAMEXINE 54785-02-3 ABECARNIL 111841-85-1 ADAPALENE 106685-40-9 ABITESARTAN 137882-98-5 ADAPROLOL 101479-70-3 ABLUKAST 96566-25-5 ADATANSERIN 127266-56-2 ABUNIDAZOLE 91017-58-2 ADEFOVIR 106941-25-7 ACADESINE 2627-69-2 ADELMIDROL 1675-66-7 ACAMPROSATE 77337-76-9 ADEMETIONINE 17176-17-9 ACAPRAZINE 55485-20-6 ADENOSINE PHOSPHATE 61-19-8 ACARBOSE 56180-94-0 ADIBENDAN 100510-33-6 ACEBROCHOL 514-50-1 ADICILLIN 525-94-0 ACEBURIC ACID 26976-72-7 ADIMOLOL 78459-19-5 ACEBUTOLOL 37517-30-9 ADINAZOLAM 37115-32-5 ACECAINIDE 32795-44-1 ADIPHENINE 64-95-9 ACECARBROMAL 77-66-7 ADIPIODONE 606-17-7 ACECLIDINE 827-61-2 ADITEREN 56066-19-4 ACECLOFENAC 89796-99-6 ADITOPRIM 56066-63-8 ACEDAPSONE 77-46-3 ADOSOPINE 88124-26-9 ACEDIASULFONE SODIUM 127-60-6 ADOZELESIN 110314-48-2 ACEDOBEN 556-08-1 ADRAFINIL 63547-13-7 ACEFLURANOL 80595-73-9 ADRENALONE
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2012/0115729 A1 Qin Et Al
    US 201201.15729A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2012/0115729 A1 Qin et al. (43) Pub. Date: May 10, 2012 (54) PROCESS FOR FORMING FILMS, FIBERS, Publication Classification AND BEADS FROM CHITNOUS BOMASS (51) Int. Cl (75) Inventors: Ying Qin, Tuscaloosa, AL (US); AOIN 25/00 (2006.01) Robin D. Rogers, Tuscaloosa, AL A6II 47/36 (2006.01) AL(US); (US) Daniel T. Daly, Tuscaloosa, tish 9.8 (2006.01)C (52) U.S. Cl. ............ 504/358:536/20: 514/777; 426/658 (73) Assignee: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF 57 ABSTRACT ALABAMA, Tuscaloosa, AL (US) (57) Disclosed is a process for forming films, fibers, and beads (21) Appl. No.: 13/375,245 comprising a chitinous mass, for example, chitin, chitosan obtained from one or more biomasses. The disclosed process (22) PCT Filed: Jun. 1, 2010 can be used to prepare films, fibers, and beads comprising only polymers, i.e., chitin, obtained from a suitable biomass, (86). PCT No.: PCT/US 10/36904 or the films, fibers, and beads can comprise a mixture of polymers obtained from a suitable biomass and a naturally S3712). (4) (c)(1), Date: Jan. 26, 2012 occurring and/or synthetic polymer. Disclosed herein are the (2), (4) Date: an. AO. films, fibers, and beads obtained from the disclosed process. O O This Abstract is presented solely to aid in searching the sub Related U.S. Application Data ject matter disclosed herein and is not intended to define, (60)60) Provisional applicationpp No. 61/182,833,sy- - - s filed on Jun.
    [Show full text]
  • Proceedings of the British Pharmacological Society Clinical Pharmacology Section
    PROCEEDINGS OF THE BRITISH PHARMACOLOGICAL SOCIETY CLINICAL PHARMACOLOGY SECTION 9-11 September 1987 UNIVERSITY OF OXFORD For oral communications with more than one author, an asterisk(*) denotes the one who presented the work. 90P Proceedings of the BPS, 9-11 September 1987 COMMUNICATIONS Low dose angiotensin II enhances proximal min clearance period (CP). Urine was collected tubular sodium reabsorption in man for this and a further CP after the infusion. Absolute Na+ excretion (UNa + V) (,mol J. McMURRAY*, P. H. SEIDELIN & min-' ± s.e. mean) for the baseline preinfusion A. D. STRUTHERS CP, the infusion CP and post infusion recovery Department of Clinical Pharmacology, Ninewells CPwas: (a) 119 ± 15; 112 ± 14; 108 ± 14. (b) 108 Hospital and Medical School, Dundee DD1 9SY + 13; 82 + 10; 101 ± 14 (P < 0.01 vs control). Fractional Na+ excretion (FENa+) (% s.e. The renin-angiotensin-aldosterone system mean) for the equivalent CP was (a) 0.84 ± 0.1; (RAAS) is crucial in the maintenance of Na+ 0.75 ± 0.1; 0.72 ± 0.09 (b) 0.82 ± 0.09; 0.56 + balance in man. The role of aldosterone in Na+ 0.07; 0.69 ± 0.09 (P < 0.02 vs control). Fractional homeostasis is well known (Laragh, 1985). In Li+ excretion (FEL,-) (% + s.e. mean) was: (a) addition, however, there are now animal data to 31 ±2;30+2;34+3. (b)29±2;23±2;27±3. suggest that angiotensin II (All) plays a direct (P < 0.01 vs control). Distal Na+ reabsorption role, independent of aldosterone, in controlling (RDNa+) (% ± s.e. mean) was: (a) 34 ± 2; 34 + renal Na+ reabsorption.
    [Show full text]
  • Back Matter (PDF)
    INDEX Volume 250, July-September, 1989 Acad, B.-A. and Weiss, H. R: Regional modification of status, obesity (dogs), inhalational, hepatobiliary clearance, 02 consumption and coronary flow 1061 cholephilic xenobiotics (rats), 421 during Beta adrenoceptor stimula- postjunctional, anococcygeus muscle local, induced injury to sciatic nerve, his- tion in reperfused canine myocar- (rats), 492 tologic analysis (rats), 406 dium, 611 beta Angiotensin II Acetaminophen, -induced necrosis, hepato- basal activity, phosphatidic acid phos- -adenosine interactions protective effects, cystathionine phatase (rats), 236 heart rate changes, aldosterone release (rats), 667 02 consumption and coronary flow, (rats), 442 Acetylcholine myocardium (dogs), 611 noradrenergic neurotransmission, a-aminobutyric acid outflow, morphine Adrenocorticotropin, acute and chronic vasoconstriction (rats), 433 withdrawal, alpha receptors (guinea phencyclidine administration (rats), antihypertensive mechanism of captopril, pigs), 682 534 renal hypertension (rats), 515 endogenous release, muscarinic modula- Aging, defective modulation, noradrenergic defective modulation, noradrenergic neu- tion, neostriatal slices (rats), 617 neurotransmission, prostaglandins rotransmission, prostaglandins preclinical studies of quinelorane (rats), (rats), 9 (rats), 9 227 Ahlers, S. T., see Barrett, J. E., 788 minimal receptor domains (rabbits), 31 Acetylcholinesterase Ahiers, S. T., see Gleeson, S., 809 nonpeptide receptor antagonists, struc- changes in drinking activity, electrolyte Albelda,
    [Show full text]
  • International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors
    1521-0081/67/3/601–655$25.00 http://dx.doi.org/10.1124/pr.114.010249 PHARMACOLOGICAL REVIEWS Pharmacol Rev 67:601–655, July 2015 Copyright © 2015 by The American Society for Pharmacology and Experimental Therapeutics ASSOCIATE EDITOR: ELIOT H. OHLSTEIN International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors Pertti Panula, Paul L. Chazot, Marlon Cowart, Ralf Gutzmer, Rob Leurs, Wai L. S. Liu, Holger Stark, Robin L. Thurmond, and Helmut L. Haas Department of Anatomy, and Neuroscience Center, University of Helsinki, Finland (P.P.); School of Biological and Biomedical Sciences, University of Durham, United Kingdom (P.L.C.); AbbVie, Inc. North Chicago, Illinois (M.C.); Department of Dermatology and Allergy, Hannover Medical School, Hannover, Germany (R.G.); Department of Medicinal Chemistry, Amsterdam Institute of Molecules, Medicines and Systems, VU University Amsterdam, The Netherlands (R.L.); Ziarco Pharma Limited, Canterbury, United Kingdom (W.L.S.L.); Institute of Pharmaceutical and Medical Chemistry (H.S.) and Institute of Neurophysiology, Medical Faculty (H.L.H.), Heinrich-Heine-University Duesseldorf, Germany; and Janssen Research & Development, LLC, San Diego, California (R.L.T.) Abstract ....................................................................................602 Downloaded from I. Introduction and Historical Perspective .....................................................602 II. Histamine H1 Receptor . ..................................................................604 A. Receptor Structure
    [Show full text]
  • Pharmaceutical Appendix to the Tariff Schedule 2
    Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE HARMONIZED TARIFF SCHEDULE Harmonized Tariff Schedule of the United States (2007) (Rev. 2) Annotated for Statistical Reporting Purposes PHARMACEUTICAL APPENDIX TO THE TARIFF SCHEDULE 2 Table 1. This table enumerates products described by International Non-proprietary Names (INN) which shall be entered free of duty under general note 13 to the tariff schedule. The Chemical Abstracts Service (CAS) registry numbers also set forth in this table are included to assist in the identification of the products concerned. For purposes of the tariff schedule, any references to a product enumerated in this table includes such product by whatever name known. ABACAVIR 136470-78-5 ACIDUM LIDADRONICUM 63132-38-7 ABAFUNGIN 129639-79-8 ACIDUM SALCAPROZICUM 183990-46-7 ABAMECTIN 65195-55-3 ACIDUM SALCLOBUZICUM 387825-03-8 ABANOQUIL 90402-40-7 ACIFRAN 72420-38-3 ABAPERIDONUM 183849-43-6 ACIPIMOX 51037-30-0 ABARELIX 183552-38-7 ACITAZANOLAST 114607-46-4 ABATACEPTUM 332348-12-6 ACITEMATE 101197-99-3 ABCIXIMAB 143653-53-6 ACITRETIN 55079-83-9 ABECARNIL 111841-85-1 ACIVICIN 42228-92-2 ABETIMUSUM 167362-48-3 ACLANTATE 39633-62-0 ABIRATERONE 154229-19-3 ACLARUBICIN 57576-44-0 ABITESARTAN 137882-98-5 ACLATONIUM NAPADISILATE 55077-30-0 ABLUKAST 96566-25-5 ACODAZOLE 79152-85-5 ABRINEURINUM 178535-93-8 ACOLBIFENUM 182167-02-8 ABUNIDAZOLE 91017-58-2 ACONIAZIDE 13410-86-1 ACADESINE 2627-69-2 ACOTIAMIDUM 185106-16-5 ACAMPROSATE 77337-76-9
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2002/0102215 A1 100 Ol
    US 2002O102215A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2002/0102215 A1 Klaveness et al. (43) Pub. Date: Aug. 1, 2002 (54) DIAGNOSTIC/THERAPEUTICAGENTS (60) Provisional application No. 60/049.264, filed on Jun. 6, 1997. Provisional application No. 60/049,265, filed (75) Inventors: Jo Klaveness, Oslo (NO); Pal on Jun. 6, 1997. Provisional application No. 60/049, Rongved, Oslo (NO); Anders Hogset, 268, filed on Jun. 7, 1997. Oslo (NO); Helge Tolleshaug, Oslo (NO); Anne Naevestad, Oslo (NO); (30) Foreign Application Priority Data Halldis Hellebust, Oslo (NO); Lars Hoff, Oslo (NO); Alan Cuthbertson, Oct. 28, 1996 (GB)......................................... 9622.366.4 Oslo (NO); Dagfinn Lovhaug, Oslo Oct. 28, 1996 (GB). ... 96223672 (NO); Magne Solbakken, Oslo (NO) Oct. 28, 1996 (GB). 9622368.0 Jan. 15, 1997 (GB). ... 97OO699.3 Correspondence Address: Apr. 24, 1997 (GB). ... 9708265.5 BACON & THOMAS, PLLC Jun. 6, 1997 (GB). ... 9711842.6 4th Floor Jun. 6, 1997 (GB)......................................... 97.11846.7 625 Slaters Lane Alexandria, VA 22314-1176 (US) Publication Classification (73) Assignee: NYCOMED IMAGING AS (51) Int. Cl." .......................... A61K 49/00; A61K 48/00 (52) U.S. Cl. ............................................. 424/9.52; 514/44 (21) Appl. No.: 09/765,614 (22) Filed: Jan. 22, 2001 (57) ABSTRACT Related U.S. Application Data Targetable diagnostic and/or therapeutically active agents, (63) Continuation of application No. 08/960,054, filed on e.g. ultrasound contrast agents, having reporters comprising Oct. 29, 1997, now patented, which is a continuation gas-filled microbubbles stabilized by monolayers of film in-part of application No. 08/958,993, filed on Oct.
    [Show full text]
  • Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DIX to the HTSUS—Continued
    20558 Federal Register / Vol. 60, No. 80 / Wednesday, April 26, 1995 / Notices DEPARMENT OF THE TREASURY Services, U.S. Customs Service, 1301 TABLE 1.ÐPHARMACEUTICAL APPEN- Constitution Avenue NW, Washington, DIX TO THE HTSUSÐContinued Customs Service D.C. 20229 at (202) 927±1060. CAS No. Pharmaceutical [T.D. 95±33] Dated: April 14, 1995. 52±78±8 ..................... NORETHANDROLONE. A. W. Tennant, 52±86±8 ..................... HALOPERIDOL. Pharmaceutical Tables 1 and 3 of the Director, Office of Laboratories and Scientific 52±88±0 ..................... ATROPINE METHONITRATE. HTSUS 52±90±4 ..................... CYSTEINE. Services. 53±03±2 ..................... PREDNISONE. 53±06±5 ..................... CORTISONE. AGENCY: Customs Service, Department TABLE 1.ÐPHARMACEUTICAL 53±10±1 ..................... HYDROXYDIONE SODIUM SUCCI- of the Treasury. NATE. APPENDIX TO THE HTSUS 53±16±7 ..................... ESTRONE. ACTION: Listing of the products found in 53±18±9 ..................... BIETASERPINE. Table 1 and Table 3 of the CAS No. Pharmaceutical 53±19±0 ..................... MITOTANE. 53±31±6 ..................... MEDIBAZINE. Pharmaceutical Appendix to the N/A ............................. ACTAGARDIN. 53±33±8 ..................... PARAMETHASONE. Harmonized Tariff Schedule of the N/A ............................. ARDACIN. 53±34±9 ..................... FLUPREDNISOLONE. N/A ............................. BICIROMAB. 53±39±4 ..................... OXANDROLONE. United States of America in Chemical N/A ............................. CELUCLORAL. 53±43±0
    [Show full text]
  • Eosinophil Chemotaxis and Anterior Uveitis from Topical Dimoprit and Nordimoprit
    Eosinophil Chemotaxis and Anterior Uveitis From Topical Dimoprit and Nordimoprit Joel S. Mindel*tt Alan H. Friedmaat Tali Haimov,f Alex D. Kharlamb,*t and Jonathan M. Freilichj- Topical application of the H2-histamine receptor agonist, dimaprit (S-[4-N,N-dimethylaminopro- pyl]isothiourea), produced eosinophil chemotaxis into the anterior segment of rabbit eyes only when an H2-antagonist was co-administered. Nordimaprit (S-[4-N,N-dimethylaminoethyl]isothiourea), a structural homologue of dimaprit that lacked activity at histamine receptors, produced eosinophil chemotaxis whether or not an H2-antagonist was co-administered. Onset of eosinophil chemotaxis began after 2 or more days of treatment, and was accompanied by corneal edema, opacifkation, and ocular inflammation. There was no concurrent eosinophilia in the peripheral blood or in the conjunctiva. The response occurred in pigmented and albino rabbit eyes, and was facilitated by prior co-administration of proparacaine eye drops. Another dimaprit homologue without activity at histamine receptors, homodimaprit (S-[4-N,N- dimethylaminobutyl]isothiourea), did not produce eosinophil chemotaxis when applied topically, nor did the H2-agonists impromidine, histamine, or 4-methylhistamine, whether co-administered with an H2- antagonist or not. It was concluded that dimaprit and nordimaprit produced a selective eosinophil che- motaxis unrelated to H,- and H2-histamine receptor activity. However, the H2-agonist activity of dimaprit appeared to inhibit this response unless neutralized by an H2-antagonist. Topical application of dimaprit with an H2-antagonist or nordimaprit alone may allow large numbers of non-degranulated eosinophils, free of other cell types, to be harvested from the aqueous humor. Invest Ophthalmol Vis Sci 27:1504- 1511,1986 Histamine is both an Hr and H2-receptor agonist.
    [Show full text]
  • Histamine, Histamine Receptors, and Their Role in Immunomodulation: an Updated Systematic Review
    The Open Immunology Journal, 2009, 2, 9-41 9 Open Access Histamine, Histamine Receptors, and their Role in Immunomodulation: An Updated Systematic Review Mohammad Shahid*,1, Trivendra Tripathi2, Farrukh Sobia1, Shagufta Moin2, Mashiatullah Siddiqui2 and Rahat Ali Khan3 1Section of Immunology and Molecular Biology, Department of Microbiology, 2Department of Biochemistry, and 3Department of Pharmacology, Faculty of Medicine, Jawaharlal Nehru Medical College & Hospital, Aligarh Muslim University, Aligarh-202002, U.P., India Abstract: Histamine, a biological amine, is considered as a principle mediator of many pathological processes regulating several essential events in allergies and autoimmune diseases. It stimulates different biological activities through differen- tial expression of four types of histamine receptors (H1R, H2R, H3R and H4R) on secretion by effector cells (mast cells and basophils) through various immunological or non-immunological stimuli. Since H4R has been discovered very re- cently and there is paucity of comprehensive literature covering new histamine receptors, their antagonists/agonists, and role in immune regulation and immunomodulation, we tried to update the current aspects and fill the gap in existing litera- ture. This review will highlight the biological and pharmacological characterization of histamine, histamine receptors, their antagonists/agonists, and implications in immune regulation and immunomodulation. Keywords: Histamine, histamine receptors, H4-receptor, antagonists, agonists, immunomodulation. I.
    [Show full text]
  • Histamine Receptors
    HISTAMINE RECEPTORS Rob Leurs and Henk Timmerman Based on these observations histamine is Leiden/Amsterdam Centre for Drug Research considered as one of the most important Division of Medicinal Chemistry mediators of allergy and inflammation. Vrije Universiteit Amsterdam, The Netherlands Pharmacology of the Histamine Receptor Subtypes Introduction The advent of molecular biology techniques has greatly increased the number of Histamine is one of the aminergic pharmacologically distinct receptor subtypes in neurotransmitters, playing an important role in the the biogenic amine field, yet the pharmacological regulation of several (patho)physiological definition of the three distinct histamine receptor processes. In the mammalian brain histamine is subtypes by the pioneering work of Ash and synthesized in a restricted population of neurons Schild,34 Blacket al and Arrang et al 5 has still not located in the tuberomammillary nucleus of the been challenged by gene cloning approaches. posterior hypothalamus.1 These neurons project diffusely to most cerebral areas and have been Until the seventies, histamine research implicated in several brain functions (e.g. completely focused on the role of histamine in sleep/wakefulness, hormonal secretion, allergic diseases. This intensive research resulted cardiovascular control, thermoregulation, food in the development of several potent 1 intake, and memory formation). In peripheral “antihistamines” (e.g. mepyramine), which were tissues histamine is stored in mast cells, useful in inhibiting certain symptoms of allergic basophils, enterochromaffin cells and probably conditions.6 The observation that these also in some specific neurons. Mast cell histamine “antihistamines” did not antagonise all histamine- plays an important role in the pathogenesis of induced effects (e.g.
    [Show full text]
  • ( 12 ) United States Patent
    US010493080B2 (12 ) United States Patent (10 ) Patent No.: US 10,493,080 B2 Schultz et al. (45 ) Date of Patent : Dec. 3 , 2019 ( 54 ) DIRECTED DIFFERENTIATION OF (56 ) References Cited OLIGODENDROCYTE PRECURSOR CELLS TO A MYELINATING CELL FATE U.S. PATENT DOCUMENTS 7,301,071 B2 11/2007 Zheng (71 ) Applicants : The Scripps Research Institute , La 7,304,071 B2 12/2007 Cochran et al. Jolla , CA (US ) ; Novartis AG , Basel 9,592,288 B2 3/2017 Schultz et al. 2003/0225072 A1 12/2003 Welsh et al. ( CH ) 2006/0258735 Al 11/2006 Meng et al. 2009/0155207 Al 6/2009 Hariri et al . (72 ) Inventors : Peter Schultz , La Jolla , CA (US ) ; Luke 2010/0189698 A1 7/2010 Willis Lairson , San Diego , CA (US ) ; Vishal 2012/0264719 Al 10/2012 Boulton Deshmukh , La Jolla , CA (US ) ; Costas 2016/0166687 Al 6/2016 Schultz et al. Lyssiotis , Boston , MA (US ) FOREIGN PATENT DOCUMENTS (73 ) Assignees : The Scripps Research Institute , La JP 10-218867 8/1998 Jolla , CA (US ) ; Novartis AG , Basel JP 2008-518896 5/2008 (CH ) JP 2010-533656 A 10/2010 WO 2008/143913 A1 11/2008 WO 2009/068668 Al 6/2009 ( * ) Notice : Subject to any disclaimer , the term of this WO 2009/153291 A1 12/2009 patent is extended or adjusted under 35 WO 2010/075239 Al 7/2010 U.S.C. 154 ( b ) by 0 days . (21 ) Appl. No .: 15 /418,572 OTHER PUBLICATIONS Molin - Holgado et al . “ Regulation of muscarinic receptor function in ( 22 ) Filed : Jan. 27 , 2017 developing oligodendrocytes by agonist exposure ” British Journal of Pharmacology, 2003 , 138 , pp .
    [Show full text]