The Structure and Function of V1b Vasopressin Receptor
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(1982), 24(4), 329—337 Pineal Response to Lithium1
Indian J. Psychiat. (1982), 24(4), 329—337 PINEAL RESPONSE TO LITHIUM1 S. PARVATHI DEVI* A. VENKOBA RAO> PINEAL FUNCTION AND BEHAVIOUR—A until Crowther demonstrated from his REVIEW autopsy studies that pineal calcification The pineal gland in ma.i is an active had nothing to do with mental derange endocrine gland throughout life (Wurtman ment. et al., 1964 ; Tapp & Huxley, 1972 ; Interest in the pineal gland lay dormant Cardinali, 1974 ; Reiter et al., 1975 ; Reiter, and the gland was relegated to be a ves- 1978). It elaborates several hormones with tigeal organ until the endocrine nature precise rhythmicity. The chronobiological of the gland was suggested following des aspects of the mammalian pineal gland have criptions of pineal tumours associated with been clearly brought out by Reiler (198!) precocious puberty (Kitay, 1954). The defining the circadian rhythms in indole idea of a special relation of pineal gland to metabolism within the pineal of mammals. mind was revived in reports of experiments The two major classes of pineal hormones— with pineal extracts in the treatment of pineal indoles (melatonin, serotonin and schizophrenia (Becker, 1920 ; Eldered et the tryptophols) and the polypeptides are al., 196U; Kitay & Altschule, 1954). The known to influence several physiological isolation and characterisation of the pineal systems including the central nervous system hormone melatonin was a turning point (Cardinali, 1974 and Anton Tay, 1974). in pineal research (Lerner et al., 1958). The association of pineal gland with be Since then the pineal gland has been a haviour and mental illness can be traced to focus of intense scientific enquiry revealing Alexandrian school of thought (Herophilus it to be an endocrine gland capable of c. -
DDAVP Nasal Spray Is Provided As an Aqueous Solution for Intranasal Use
DDAVP® Nasal Spray (desmopressin acetate) Rx only DESCRIPTION DDAVP® Nasal Spray (desmopressin acetate) is a synthetic analogue of the natural pituitary hormone 8-arginine vasopressin (ADH), an antidiuretic hormone affecting renal water conservation. It is chemically defined as follows: Mol. wt. 1183.34 Empirical formula: C46H64N14O12S2•C2H4O2•3H2O 1-(3-mercaptopropionic acid)-8-D-arginine vasopressin monoacetate (salt) trihydrate. DDAVP Nasal Spray is provided as an aqueous solution for intranasal use. Each mL contains: Desmopressin acetate 0.1 mg Sodium Chloride 7.5 mg Citric acid monohydrate 1.7 mg Disodium phosphate dihydrate 3.0 mg Benzalkonium chloride solution (50%) 0.2 mg The DDAVP Nasal Spray compression pump delivers 0.1 mL (10 mcg) of DDAVP (desmopressin acetate) per spray. CLINICAL PHARMACOLOGY DDAVP contains as active substance desmopressin acetate, a synthetic analogue of the natural hormone arginine vasopressin. One mL (0.1 mg) of intranasal DDAVP has an antidiuretic activity of about 400 IU; 10 mcg of desmopressin acetate is equivalent to 40 IU. 1. The biphasic half-lives for intranasal DDAVP were 7.8 and 75.5 minutes for the fast and slow phases, compared with 2.5 and 14.5 minutes for lysine vasopressin, another form of the hormone used in this condition. As a result, intranasal DDAVP provides a prompt onset of antidiuretic action with a long duration after each administration. 1 2. The change in structure of arginine vasopressin to DDAVP has resulted in a decreased vasopressor action and decreased actions on visceral smooth muscle relative to the enhanced antidiuretic activity, so that clinically effective antidiuretic doses are usually below threshold levels for effects on vascular or visceral smooth muscle. -
Histamine Receptors
Tocris Scientific Review Series Tocri-lu-2945 Histamine Receptors Iwan de Esch and Rob Leurs Introduction Leiden/Amsterdam Center for Drug Research (LACDR), Division Histamine is one of the aminergic neurotransmitters and plays of Medicinal Chemistry, Faculty of Sciences, Vrije Universiteit an important role in the regulation of several (patho)physiological Amsterdam, De Boelelaan 1083, 1081 HV, Amsterdam, The processes. In the mammalian brain histamine is synthesised in Netherlands restricted populations of neurons that are located in the tuberomammillary nucleus of the posterior hypothalamus.1 Dr. Iwan de Esch is an assistant professor and Prof. Rob Leurs is These neurons project diffusely to most cerebral areas and have full professor and head of the Division of Medicinal Chemistry of been implicated in several brain functions (e.g. sleep/ the Leiden/Amsterdam Center of Drug Research (LACDR), VU wakefulness, hormonal secretion, cardiovascular control, University Amsterdam, The Netherlands. Since the seventies, thermoregulation, food intake, and memory formation).2 In histamine receptor research has been one of the traditional peripheral tissues, histamine is stored in mast cells, eosinophils, themes of the division. Molecular understanding of ligand- basophils, enterochromaffin cells and probably also in some receptor interaction is obtained by combining pharmacology specific neurons. Mast cell histamine plays an important role in (signal transduction, proliferation), molecular biology, receptor the pathogenesis of various allergic conditions. After mast cell modelling and the synthesis and identification of new ligands. degranulation, release of histamine leads to various well-known symptoms of allergic conditions in the skin and the airway system. In 1937, Bovet and Staub discovered compounds that antagonise the effect of histamine on these allergic reactions.3 Ever since, there has been intense research devoted towards finding novel ligands with (anti-) histaminergic activity. -
Receptor Antagonist (H RA) Shortages | May 25, 2020 2 2 2 GERD4,5 • Take This Opportunity to Determine If Continued Treatment Is Necessary
H2-receptor antagonist (H2RA) Shortages Background . 2 H2RA Alternatives . 2 Therapeutic Alternatives . 2 Adults . 2 GERD . 3 PUD . 3 Pediatrics . 3 GERD . 3 PUD . 4 Tables Table 1: Health Canada–Approved Indications of H2RAs . 2 Table 2: Oral Adult Doses of H2RAs and PPIs for GERD . 4 Table 3: Oral Adult Doses of H2RAs and PPIs for PUD . 5 Table 4: Oral Pediatric Doses of H2RAs and PPIs for GERD . 6 Table 5: Oral Pediatric Doses of H2RAs and PPIs for PUD . 7 References . 8 H2-receptor antagonist (H2RA) Shortages | May 25, 2020 1 H2-receptor antagonist (H2RA) Shortages BACKGROUND Health Canada recalls1 and manufacturer supply disruptions may be causing shortages of commonly used acid-reducing medications called histamine H2-receptor antagonists (H2RAs) . H2RAs include cimetidine, famotidine, nizatidine and ranitidine . 2 There are several Health Canada–approved indications of H2RAs (see Table 1); this document addresses the most common: gastroesophageal reflux disease (GERD) and peptic ulcer disease (PUD) . 2 TABLE 1: HEALTH CANADA–APPROVED INDICATIONS OF H2RAs H -Receptor Antagonists (H RAs) Health Canada–Approved Indications 2 2 Cimetidine Famotidine Nizatidine Ranitidine Duodenal ulcer, treatment ü ü ü ü Duodenal ulcer, prophylaxis — ü ü ü Benign gastric ulcer, treatment ü ü ü ü Gastric ulcer, prophylaxis — — — ü GERD, treatment ü ü ü ü GERD, maintenance of remission — ü — — Gastric hypersecretion,* treatment ü ü — ü Self-medication of acid indigestion, treatment and prophylaxis — ü† — ü† Acid aspiration syndrome, prophylaxis — — — ü Hemorrhage from stress ulceration or recurrent bleeding, — — — ü prophylaxis ü = Health Canada–approved indication; GERD = gastroesophageal reflux disease *For example, Zollinger-Ellison syndrome . -
Design and Synthesis of Functionally Selective Kappa Opioid Receptor Ligands
Design and Synthesis of Functionally Selective Kappa Opioid Receptor Ligands By Stephanie Nicole Johnson 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 Masters in Science. Chairperson: Dr. Thomas E. Prisinzano Dr. Apurba Dutta Dr. Jeffrey P. Krise Date Defended: May 2, 2017 The Thesis Committee for Stephanie Nicole Johnson certifies that this is the approved version of the following thesis: Design and Synthesis of Functionally Selective Kappa Opioid Receptor Ligands Chairperson: Dr. Thomas E. Prisinzano Date approved: May 4, 2017 ii Abstract The ability of ligands to differentially regulate the activity of signaling pathways coupled to a receptor potentially enables researchers to optimize therapeutically relevant efficacies, while minimizing activity at pathways that lead to adverse effects. Recent studies have demonstrated the functional selectivity of kappa opioid receptor (KOR) ligands acting at KOR expressed by rat peripheral pain sensing neurons. In addition, KOR signaling leading to antinociception and dysphoria occur via different pathways. Based on this information, it can be hypothesized that a functionally selective KOR agonist would allow researchers to optimize signaling pathways leading to antinociception while simultaneously minimizing activity towards pathways that result in dysphoria. In this study, our goal was to alter the structure of U50,488 such that efficacy was maintained for signaling pathways important for antinociception (inhibition of cAMP accumulation) and minimized for signaling pathways that reduce antinociception. Thus, several compounds based on the U50,488 scaffold were designed, synthesized, and evaluated at KORs. Selected analogues were further evaluated for inhibition of cAMP accumulation, activation of extracellular signal-regulated kinase (ERK), and inhibition of calcitonin gene- related peptide release (CGRP). -
Histamine in the Control of Gastric Acid Secretion: a Topic Review
Pharmacological Research 47 (2003) 299–304 Histamine in the control of gastric acid secretion: a topic review Elisabetta Barocelli∗, Vigilio Ballabeni Dipartimento di Scienze Farmacologiche, Biologiche e Chimiche Applicate, Università di Parma, Parco Area delle Scienze, 27/A, Parma 43100, Italy Accepted 30 December 2002 Abstract In this paper, the current knowledge about the role of histamine in the control of gastric acid secretion is reviewed. In particular, we focus this topic into three sections considering the recent insights on: histamine receptor subtypes involved in gastric acid secretion, the interplay between neuronal–hormonal–paracrine pathways and the cerebral histaminergic control of gastric secretion. From the careful perusal of scientific literature, the fundamental role of histamine as local stimulator of gastric acid secretion via H2 receptors is fairly confirmed while for the H3 receptor only a minor modulating role is hypothesized. An undisputed function of ECL cells as controllable source of histamine within the so-called gastrin–ECL cell–parietal cell axis is generally proposed and the intriguing possibility of a remote control of gastric secretion via H3 receptors is also suggested. © 2003 Elsevier Science Ltd. All rights reserved. Keywords: Secretagogue; Histaminergic system; Gastric acid secretion 1. Introduction the central and in the peripheral neuronal networks [7] and its cloning [8] major attention was devoted by researchers Although histamine has been found to be a potent secret- mainly to the re-examination of apparently anomalous ef- agogue of acid secretion since 1920 [1], its physiologic role fects exerted by histamine. Also for gastric acid secretion, in the stomach is again a subject of debate as also acetyl- although here histamine plays an undisputed central role choline and gastrin are of prime importance in the stimula- through H2 receptors activation [9], the possible involvement tion of gastric acid production. -
Therapeutic Potential of Vasopressin-Receptor Antagonists in Heart Failure
J Pharmacol Sci 124, 1 – 6 (2014) Journal of Pharmacological Sciences © The Japanese Pharmacological Society Current Perspective Therapeutic Potential of Vasopressin-Receptor Antagonists in Heart Failure Yasukatsu Izumi1,*, Katsuyuki Miura2, and Hiroshi Iwao1 1Department of Pharmacology, 2Applied Pharmacology and Therapeutics, Osaka City University Medical School, Osaka 545-8585, Japan Received October 2, 2013; Accepted November 17, 2013 Abstract. Arginine vasopressin (AVP) is a 9-amino acid peptide that is secreted from the posterior pituitary in response to high plasma osmolality and hypotension. AVP has important roles in circulatory and water homoeostasis, which are mediated by oxytocin receptors and by AVP receptor subtypes: V1a (mainly vascular), V1b (pituitary), and V2 (renal). Vaptans are orally and intravenously active nonpeptide vasopressin-receptor antagonists. Recently, subtype-selective nonpeptide vasopressin-receptor agonists have been developed. A selective V1a-receptor antago- nist, relcovaptan, has shown initial positive results in the treatment of Raynaud’s disease, dysmen- orrhea, and tocolysis. A selective V1b-receptor antagonist, nelivaptan, has beneficial effects in the treatment of psychiatric disorders. Selective V2-receptor antagonists including mozavaptan, lixivaptan, satavaptan, and tolvaptan induce highly hypotonic diuresis without substantially affecting the excretion of electrolytes. A nonselective V1a/V2-receptor antagonist, conivaptan, is used in the treatment for euvolaemic or hypervolemic hyponatremia. Recent basic and clinical studies have shown that AVP-receptor antagonists, especially V2-receptor antagonists, may have therapeutic potential for heart failure. This review presents current information about AVP and its antagonists. Keywords: arginine vasopressin, diuretic, heart failure, vasopressin receptor antagonist 1. Introduction receptor blockers, diuretics, b-adrenoceptor blockers, digitalis glycosides, and inotropic agents (4). -
Article Efficacy and Tolerance of Urea Compared with Vaptans for Long
Article Efficacy and Tolerance of Urea Compared with Vaptans for Long-Term Treatment of Patients with SIADH Alain Soupart,*† Michel Coffernils,* Bruno Couturier,† Fabrice Gankam-Kengne,† and Guy Decaux† Summary Background and objectives Vaptans (vasopressin V2-receptor antagonists) are a new approach for the treatment of hyponatremia. However, their indications remain to be determined, and their benefit compared with that of the usual treatments for the syndrome of inappropriate antidiuretic hormone secretion (SIADH) have not been *Department of fi Internal Medicine, evaluated. This prospective, long-term study compared the ef cacy, tolerability, and safety of two oral vaptans Jolimont/Tubize with those of oral urea in patients with SIADH. Hospital, Tubize, Brabant, Belgium; and † Design, setting, participants, & measurements Patients with chronic SIADH of various origins were treated first Research Unit for the Study of Hydromineral with vaptans for 1 year. After an 8-day holiday period, they received oral urea for an additional 1-year follow-up. Metabolism, Serum sodium was measured every 2 months, and drug doses were adjusted accordingly. Department of General Internal Results Thirteen participants were initially included in the study (serum sodium, 12563 mEq/L); 12 completed Medicine, Erasmus the 2-year treatment period. Treatment with vaptans (satavaptan, 5–50 mg/d, n=10; tolvaptan, 30–60 mg/day, University Hospital, Brussels, Belgium n=2) increased natremia (serum sodium, 13563 mEq/L) during the 1-year vaptan period without escape. Hyponatremia recurred in the 12 participants when vaptans were stopped (holiday period). Urea improved the Correspondence: natremia with the same efficacy (serum sodium, 13562 mEq/L) as vaptans during the 1-year urea treatment Dr. -
Histamine H2-Receptor Antagonists Improve Non-Steroidal Anti-Inflammatory Drug-Induced Intestinal Dysbiosis
International Journal of Molecular Sciences Article Histamine H2-Receptor Antagonists Improve Non-Steroidal Anti-Inflammatory Drug-Induced Intestinal Dysbiosis Rei Kawashima, Shun Tamaki, Fumitaka Kawakami, Tatsunori Maekawa and Takafumi Ichikawa * Department of Regulation Biochemistry, Kitasato University Graduate School of Medical Sciences, Kanagawa 252-0374, Japan; [email protected] (R.K.); [email protected] (S.T.); [email protected] (F.K.); [email protected] (T.M.) * Correspondence: [email protected]; Tel.: +81-42-778-8863 Received: 8 October 2020; Accepted: 30 October 2020; Published: 31 October 2020 Abstract: Dysbiosis, an imbalance of intestinal flora, can cause serious conditions such as obesity, cancer, and psychoneurological disorders. One cause of dysbiosis is inflammation. Ulcerative enteritis is a side effect of non-steroidal anti-inflammatory drugs (NSAIDs). To counteract this side effect, we proposed the concurrent use of histamine H2 receptor antagonists (H2RA), and we examined the effect on the intestinal flora. We generated a murine model of NSAID-induced intestinal mucosal injury, and we administered oral H2RA to the mice. We collected stool samples, compared the composition of intestinal flora using terminal restriction fragment length polymorphism, and performed organic acid analysis using high-performance liquid chromatography. The intestinal flora analysis revealed that NSAID [indomethacin (IDM)] administration increased Erysipelotrichaceae and decreased Clostridiales but that both had improved with the concurrent administration of H2RA. Fecal levels of acetic, propionic, and n-butyric acids increased with IDM administration and decreased with the concurrent administration of H2RA. Although in NSAID-induced gastroenteritis the proportion of intestinal microorganisms changes, leading to the deterioration of the intestinal environment, concurrent administration of H2RA can normalize the intestinal flora. -
The Oxytocin/Vasopressin Receptor Family Has at Least Five Members in the Gnathostome Lineage, Including Two Distinct V2 Subtypes
The oxytocin/vasopressin receptor family has at least five members in the gnathostome lineage, including two distinct V2 subtypes General and Comparative Endocrinology 175(1): 135-143 doi:10.1016/j.ygcen.2011.10.011 Accepted October 20, 2011 E-pub October 28, 2012 Published January 1, 2012 Figshare doi:10.6084/m9.figshare.811860. Shared October 1, 2013 Daniel Ocampo Daza*, Michalina Lewicka¹, Dan Larhammar Department of Neuroscience, Science for Life Laboratory, Uppsala Universitet, Box 593, SE-751 24 Uppsala, Sweden * Corresponding author. E-mail address: [email protected] ¹ Current address: Department of Neuroscience, Karolinska Institutet, SE-171 77 Stockholm, Sweden Cite as D. Ocampo Daza, M. Lewicka and D. Larhammar. The oxytocin/vasopressin family has at least five members in the gnathostome lineage, including two distinct V2 subtypes. General and Comparative Endocrinology, 175 (1) (2012) 135-143. This document corresponds to the article as it appeared upon acceptance. You are free to download, print and distribute it for any purposes under a Creative Commons Attribution 3.0 Unported License (http://creativecommons.org/licenses/by/3.0/), provided the original work is cited as specified. Errata: The introduction incorrectly states that “the V2 receptor inhibits adenylyl cyclase, thereby reducing the production of cAMP” on page 3. In fact the V2-type vasopressin receptors stimulate adenylyl cyclase and increase the cytosolic cyclic AMP release, see for instance Schöneberg et al., Molecular aspects of vasopressin receptor function, Advances in experimental medicine and biology 449 (1998) 347–58. This mistake was reported in the proofreading phase of pre-publication, but the correction was not carried to the final version of the article. -
G Protein-Coupled Receptors: What a Difference a ‘Partner’ Makes
Int. J. Mol. Sci. 2014, 15, 1112-1142; doi:10.3390/ijms15011112 OPEN ACCESS International Journal of Molecular Sciences ISSN 1422-0067 www.mdpi.com/journal/ijms Review G Protein-Coupled Receptors: What a Difference a ‘Partner’ Makes Benoît T. Roux 1 and Graeme S. Cottrell 2,* 1 Department of Pharmacy and Pharmacology, University of Bath, Bath BA2 7AY, UK; E-Mail: [email protected] 2 Reading School of Pharmacy, University of Reading, Reading RG6 6UB, UK * Author to whom correspondence should be addressed; E-Mail: [email protected]; Tel.: +44-118-378-7027; Fax: +44-118-378-4703. Received: 4 December 2013; in revised form: 20 December 2013 / Accepted: 8 January 2014 / Published: 16 January 2014 Abstract: G protein-coupled receptors (GPCRs) are important cell signaling mediators, involved in essential physiological processes. GPCRs respond to a wide variety of ligands from light to large macromolecules, including hormones and small peptides. Unfortunately, mutations and dysregulation of GPCRs that induce a loss of function or alter expression can lead to disorders that are sometimes lethal. Therefore, the expression, trafficking, signaling and desensitization of GPCRs must be tightly regulated by different cellular systems to prevent disease. Although there is substantial knowledge regarding the mechanisms that regulate the desensitization and down-regulation of GPCRs, less is known about the mechanisms that regulate the trafficking and cell-surface expression of newly synthesized GPCRs. More recently, there is accumulating evidence that suggests certain GPCRs are able to interact with specific proteins that can completely change their fate and function. These interactions add on another level of regulation and flexibility between different tissue/cell-types. -
Corticotropin-Releasing Activity of Lysine Vasopressin Evelyn Joyce Weber Iowa State University
Iowa State University Capstones, Theses and Retrospective Theses and Dissertations Dissertations 1961 Corticotropin-releasing activity of lysine vasopressin Evelyn Joyce Weber Iowa State University Follow this and additional works at: https://lib.dr.iastate.edu/rtd Part of the Biochemistry Commons Recommended Citation Weber, Evelyn Joyce, "Corticotropin-releasing activity of lysine vasopressin " (1961). Retrospective Theses and Dissertations. 1990. https://lib.dr.iastate.edu/rtd/1990 This Dissertation is brought to you for free and open access by the Iowa State University Capstones, Theses and Dissertations at Iowa State University Digital Repository. It has been accepted for inclusion in Retrospective Theses and Dissertations by an authorized administrator of Iowa State University Digital Repository. For more information, please contact [email protected]. This dissertation has been 62-1374 microfilmed exactly as received WEBER, Evelyn Joyce, 1928- CORTICOTRO PIN-RE LEASING ACTIVITY OF LYSINE VASOPRESSIN. Iowa State University of Science and Technology Ph.D., 1961 Chemistry, biological University Microfilms, Inc., Ann Arbor, Michigan CORTICO TROPIN-RELEASING ACTIVITY OF LYSINE 7AS0PRESSII Evelyn Joyce Weber A Dissertation Submitted, to the Graduate Faculty in Partial Fulfillment of The Requirements for the Degree of DOCTOR OF PHILOSOPHY . kajor Subject: Biochemistry Approved: Signature was redacted for privacy. In Charge of l-.ejor V,rork Signature was redacted for privacy. Head, of kajor Department Signature was redacted for privacy. Deacf of Gradu/ue College Iowa State University Of Science and Technology Ames, loua 1961 il TABLE OF CONTENTS Page HISTORICAL . ; 1 Biological Activities of Vasopressin. ...... -3 Pressor activity 3 Antidiuretic activity 5 Oxytocic activity. £ Corticotropin releasing activity 10 Other activities of vasopressin.