IUPHAR Research Articles

Receptor Nomenclature Guidelines

Receptors are typically characterized via two distinct approaches: (1) the identification and pharmacological characterization of a receptor-mediated response using classical pharmacological and/or radioligand approaches in tissues and animal models using selective agonist and antagonist ligands, and; (2) the cloning and expression of proteins with structural homology to known receptors, the function of which is subsequently established by studying the structure activity relationship (SAR) of receptor-mediated responses. An additional means to characterize receptors proceeded, and evolved, with the structural approach, namely classification in terms of signal transduction mechanisms. The International Union of Pharmacology (IUPHAR) created guidelines and selected working groups for each receptor family to establish a common nomenclature system. Reports from those groups that have reached some degree of consensus have been summarized in this appendix.

Receptors for cysteinyl-leukotrienes in human cells.

It is widely accepted that leukotrienes (LTs) exert their actions through high-affmity specific receptors, although none of these receptors has been cloned so far. Recently, the classification and nomenclature of LT receptors has been proposed by an ad hoc committee appointed by the International Union of Pharmacology (IUPHAR), and has been officially approved by the latter (Coleman et al., 1995; TiPS supplement, 1996). According to this nomenclature (Figure 1), the receptors for LTB4 have been termed BLT receptors (where B refers to LTB), while the receptors for the cysteine-containing LTs (Cys-LTs, i.e. LTC4, LTD4 and LTE4) have been named CysLT receptors. Figure 1 also indicates that, so far, only one class of BLT receptors has been identified with sufficient certainty (although the existence of more than one class has been suggested) (Goldman et ah., 1987), while it is recognized that CysLT receptors are heterogeneous.

IUPHAR in Germany

Trustees 1998Professor James W. Black, London, UKProfessor William C. Bowman, Glasgow, UKProfessor Alfred Gilman, Dallas, USAProfessor Thophile Godfraind, Brussels, BelgiumProfessor John Vane, London, UKProfessor Setsuro Ebashi, Okazaki, Japan

Proposed Update of Angiotensin Receptor Nomenclature

Angiotensin II exerts a wide range of actions on the heart, blood vessels, adrenals, kidneys, and nervous system and plays a major role in blood pressure maintenance and volume homeostasis. Its effects are mediated mainly by plasma membrane receptors. Efforts to elucidate the nature and distribution of these receptors have involved intensive research on the part of pharmacologists, molecular biologists, and clinicians, and to avoid confusion it is therefore important that a uniform nomenclature be adopted by all disciplines concerned. The International Union of Pharmacology (IUPHAR) Nomenclature Subcommittee for Angiotensin Receptors met in Oxnard, Calif, in February 1994. At this meeting, scientists working in the field were invited to exchange views on new issues relating to angiotensin receptor subtypes, their functions, and appropriate amendments to the nomenclature proposed in 1991.1 The committee has not yet been able to put forward a definitive recommendation in this fast-moving area, but the simple and workable guidelines suggested in this article reflect the opinion of many specialists. Comments from the scientific community are welcome to help in formulating a proposal that could be endorsed by the IUPHAR. To avoid any ambiguity, it is recommended that Ang should be used as the standard abbreviation for the hormone angiotensin, in conformity with a previous report2 from the Joint Nomenclature and Standardization Committee of the International Society of Hypertension, American Heart Association, and the …

Neural-immune-effector (NIE) cross-talk in vascular trophobiology: proposal for new and not yet exploited purinergic regulatory mechanisms

In a state-of-the-art approach, Dr. Hasséssian presents purinoceptor-mediated vasoconstriction/vasodilation mechanisms of the pulmonary circulation. He focuses on P2 purinoceptors of smooth muscle cells, endothelial cells, platelets and mast cells, without addressing P1 (adenosine) purinoceptors. Recently, the Burnstock's purinoceptorology is "arborizing" into a variety of members of P1 and P2 purinoceptor families classified by the International Union of Pharmacology. Here we would like to add some possible, new and not yet exploited, purinergic regulatory mechanisms to the Hasséssian's work. Accordingly, we shall briefly focus on the involvement of connective tissue (adventitial) mast cells and their interactions with perivascular nerves and medial smooth muscle cells. Biomedical Reviews 1994; 3: 81-86.

Receptor classification and nomenclature: the revolution and the resolution

Ever since Raymond Ahlquisrs landmark observations ~, which led to the now well-accepted concept that cellmembrane receptors for noradrenaline exist in distinct types mediating different functions, pharmacologists have been interested in the characterization of receptors for neurotransmitters and hormones. This approach not only provides explanation of the mechanisms of actions of many drugs but, through the pioneering work of Sir James Black, it is now obvious that rigorous attention to receptor characterization and the identification of selective synthetic ligands can lead to major therapeutic advances. This is exemplified by the introduction of drugs that block f~-adrenoceptors and histamine He receptors 2& Nevertheless, until the advent of modern molecular biology techniques, pharmacologists were sceptical when data from functional studies in whole tissues suggested a multiplicity of receptor types for a given mediator. However, it is now apparent that there are as many as three ~-adrenoceptor types, seven c~-adrenoceptor types, eight prostanoid receptor types and 14 types of receptor for 5-HT (Refs 4-7). This potential for receptor diversity for all neurotransmitters and hormones has now been confirmed by the cloning of many receptor genes and the study of the function of the recombinant receptor proteins for which they code. The speed at which receptor cDNAs are now being cloned has led to a revolutionary situation where new receptor types are being identified before their function in whole tissues, if any, is known. This creates problems for those interested in the classification and nomenclature of receptors. As a consequence of a strong international desire amongst pharmacologists to rationalize the information provided by techniques of molecular biology in relation to drug-related data on receptor function, the Receptor Nomenclature and Drug Classification Committee (NC-IUPHAR) was inaugurated in 1987, under the auspices of the International Union of Pharmacology (IUPHAR). The NC-IUPHAR is now established and endeavouring to provide an open forum for debate on approaches to receptor characterization and to develop guidelines and recommendations for classification and nomenclature. Initial efforts are focused largely on membrane-bound receptors for the common neurotransmitters, but ion channels and other cellular systems involving recognition sites are being considered. Some views on receptor characterization and classification have already been published by the committee s but further effort is being devoted to this by a technical subcommittee, which is also working towards the standardization of terms and symbols used in pharmacology. The technical subcommittee invites input from anyone interested in ligand-receptor theory and works through a panel of distinguished corresponding experts to ensure all views are considered. At the XIIth International Congress of Pharmacology in Montr6al this July, a symposium will be dedicated to the principles of receptor characterization, which will highlight many of the issues for debate. In particular, an integrated pharmacological approach to classification is proposed for appraisal and discussion, which relies on three essential criteria for receptor characterization. These comprise essential data from studies providing structural, operational and transductional T

Reports from IUPHAR

Reports from IUPHAR

IUPHAR announcement

IUPHAR announcement

Challenges for receptor theory as a tool for drug and drug receptor classification

Increased understanding in the field of receptor pharmacology, born of the sophisticated techniques now available to us, has confounded rather than simplified the problem of receptor classification. The International Union of Pharmacology (IUPHAR) is currently sponsoring a Receptor Nomenclature Committee whose aims are to recommend a rational system of classification, a formidable task given the complexity and volume of data in the literature (agonist/antagonist potencies, coupling mechanisms, primary structures, etc.) that will need to be incorporated. The Committee's chairman, Terry Kenakin, outlines here the limitations of classical receptor theory for drug receptor classification and suggests that any functional classification system must take into account not only affinity and intrinsic efficacy but also, at the very least, parameters relating to the transducing properties of receptors. If this is not done, then receptor classification data obtained from studies with agonists and antagonists may be different and lead to confusion.

Cannabimimetic activity of cannabinol in rats and pigeons

The present experiments examined the cannabimimetic potential of cannabinol on its own as well as its interaction with Δ 9-tetrahydrocannabinol ( Δ 9-THC) in vivo. Thus, cannabinol, as evaluated by repeated test procedures using drug-discrimination methodology (Hiltunen and Järbe, 1986; Järbe, Swedberg and Mechoulam, 1981) was found to substitute for the stimulus effects induced by Δ 9-THC in both rats ( Δ 9-THC cue = 3 mg/kg) and pigeons ( Δ 9-THC cue = 0.56 mg/kg), though, relatively larger doses were required in the latter species (ED 50 for cannabinol being 8.4 mg/kg, and 14.1 mg/kg at the time of maximum effect in rats and pigeons, respectively). When administered together, cannabinol added to the cue effects of Δ 9-THC as shown by an increase in the percentage of responding appropriate to the drug, the effect appearing more pronounced in rats than in pigeons; no apparent change in the duration of the effect was indicated by the results obtained. Unconditioned effects of drug, as defined by rectal temperature recordings and open-field activity (ambulation, rearing, latency, circling, grooming, defecation and urination), as well as assessment of vocalization in rats were in keeping with the suggestion that the pharmacological profile of cannabinol is similar, though not necessarily identical, to that of tetrahydrocannabinols, such as Δ 9-THC. Part of these data were presented at the International Union of Pharmacology, IUPHAR, 9th International Congress of Pharmacology Satellite Meeting: European Study Group for Internal Stimulus Control by Electrical Stimulation, Drugs and Other Means, ESISC, London, 29 July to 3 August, 1984 (Järbe, 1984) and at the XVIII Nordic Congress for Physiology and Pharmacology, Uppsala, 10–13 June, 1985 (Järbe, Swedberg, Hiltunen and Mechoulam, 1985).

Australia Hosts 10th IUPHAR Congress

Australia Hosts 10th IUPHAR Congress

IUPHAR Fellowship 1978–1979

IUPHAR Fellowship 1978–1979

IUPHAR fellowship 1977–1978

IUPHAR fellowship 1977–1978

IUPHAR fellowship 1977–1978

IUPHAR fellowship 1977–1978

Hypersensitivity to Drugs.

This book is one of a projected 250-volume encyclopedia of pharmacology published under the sponsorship of the International Union of Pharmacology. One is hard-pressed to think of a more ambitious venture in medical publishing. As might be expected of such an undertaking, those chosen to edit individual volumes and those selected to contribute chapters are all highly expert. Unlike a usual encyclopedia, each volume (or in this case, pair of volumes) is concerned with a major topical area with chapters covering special categories. Each chapter is essentially an expert review paper. The first seven in this book are concerned with basic principles and mechanisms of hypersensitivity to drugs; the next four are concerned with reactions involving specific organs (blood, skin, kidney, liver); the last chapter is concerned with diagnostic techniques. One assumes that the next volume will focus on other organ systems, on the epidemiology of these reactions, and

International Encyclopedia of Pharmacology and TherapeuticsInternational Encyclopedia of Pharmacology and Therapeutics.Section 78, Vols. 1 and 2:Radionuclides in Pharmacology. Section Editor: CohenY.. Contributors: AppelgrenL.-E.,et al.Sponsored by the International Union of Pharmacology (IUPHAR) (Chairman: B. Uvnäs, Stockholm). Cloth, $47.00; £ 17.50 (2-vol. set). Pp. 962, with figures. Oxford, England, Pergamon Press, 1971.

HomeRadiologyVol. 103, No. 2 PreviousNext Book ReviewInternational Encyclopedia of Pharmacology and TherapeuticsMilo M. WebberMilo M. WebberMilo M. WebberPublished Online:May 1 1972https://doi.org/10.1148/103.2.288MoreSectionsPDF ToolsImage ViewerAdd to favoritesCiteTrack CitationsPermissionsReprints ShareShare onFacebookTwitterLinked In Article HistoryPublished in print: May 1972 FiguresReferencesRelatedDetailsRecommended Articles RSNA Education Exhibits RSNA Case Collection Vol. 103, No. 2 Metrics Altmetric Score PDF download

International Encyclopedia of Pharmacology and TherapeuticsInternational Encyclopedia of Pharmacology and Therapeutics. Section 76, Vols. 1 and 2: Radiocontrast Agents. Section Editor: KnoefelP. K.. Sponsored by the International Union of Pharmacology. Cloth, $53.50; Pp. 692, with figures. Oxford, Per-gamon Press, 1971.

HomeRadiologyVol. 102, No. 3 PreviousNext Book ReviewInternational Encyclopedia of Pharmacology and TherapeuticsElliott C. LasserElliott C. LasserElliott C. LasserPublished Online:Mar 1 1972https://doi.org/10.1148/102.3.574MoreSectionsPDF ToolsImage ViewerAdd to favoritesCiteTrack CitationsPermissionsReprints ShareShare onFacebookTwitterLinked In Article HistoryPublished in print: Mar 1972 FiguresReferencesRelatedDetailsRecommended Articles RSNA Education Exhibits RSNA Case Collection Vol. 102, No. 3 Metrics Altmetric Score PDF download