Molecular pharmacology of G protein-coupled receptors. Editorial.

Abstract:

:G protein-coupled receptors are the largest group of membrane proteins and are the targets for approximately 30% of drugs currently used therapeutically. These 7-transmembrane-spanning proteins continue to provide new opportunities to develop therapeutics based on emerging knowledge of their structure, signalling properties and interactions with other proteins. This themed issue of the British Journal of Pharmacology contains a series of papers that cover these issues and identify approaches that may determine future directions. Many of these papers contain material that was presented at the 5th International Molecular Pharmacology of G Protein-Coupled Receptors meeting held in Sydney Australia in late 2008.

journal_name

Br J Pharmacol

authors

Summers RJ

doi

10.1111/j.1476-5381.2010.00695.x

subject

Has Abstract

pub_date

2010-03-01 00:00:00

pages

983-5

issue

5

eissn

0007-1188

issn

1476-5381

pii

BPH695

journal_volume

159

pub_type

社论
  • The irreversible binding of acetylcholine mustard to muscarinic receptors in intestinal smooth muscle of the guinea-pig.

    abstract::1. Acetylcholine mustard (N-2-chloroethyl-N-methyl-2-acetoxyethylamine), a potent muscarinic agonist, binds virtually irreversibly to muscarinic receptors in longitudinal muscle strips from guinea-pig small intesting, as shown by the inhibition of the binding of E13-H]-propylbenzilycholine mustard ([3-H-PrBCM), an aff...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1975.tb07372.x

    authors: Robinson DA,Taylor JG,Young JM

    更新日期:1975-03-01 00:00:00

  • Systemic ETA receptor antagonism with BQ-123 blocks ET-1 induced forearm vasoconstriction and decreases peripheral vascular resistance in healthy men.

    abstract::1. The effect on systemic haemodynamics of BQ-123, a selective endothelin A (ETA) receptor antagonist, was investigated in healthy men by giving, on separate occasions, ascending intravenous doses of 100, 300, 1000 and 3000 nmol min(-1) BQ-123, each for 15 min, in a randomized, placebo-controlled, double-blind study. ...

    journal_title:British journal of pharmacology

    pub_type: 临床试验,杂志文章,随机对照试验

    doi:10.1038/sj.bjp.0704304

    authors: Spratt JC,Goddard J,Patel N,Strachan FE,Rankin AJ,Webb DJ

    更新日期:2001-10-01 00:00:00

  • Activation of PAC(1) and VPAC receptor subtypes elicits differential physiological responses from sympathetic preganglionic neurons in the anaesthetized rat.

    abstract:BACKGROUND AND PURPOSE:Pituitary adenylate cyclase-activating polypeptide (PACAP) is an excitatory neuropeptide with central and peripheral cardiovascular actions. Intrathecal PACAP increases splanchnic sympathetic nerve activity and heart rate, but not mean arterial pressure (MAP). We hypothesize that the three PACAP ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2012.02045.x

    authors: Inglott MA,Lerner EA,Pilowsky PM,Farnham MM

    更新日期:2012-11-01 00:00:00

  • Role of nitric oxide in the induction and expression of morphine tolerance and dependence in mice.

    abstract::1. The possible involvement of nitric oxide (NO) in the induction and expression of morphine tolerance and dependence was studied in mice. A two-day repeated injection regimen was used to induce morphine tolerance and dependence. Tolerance was assessed by the tail flick test and physical dependence by naloxone challen...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb15280.x

    authors: Dambisya YM,Lee TL

    更新日期:1996-03-01 00:00:00

  • The effects of amfonelic acid and some other central stimulants on mouse striatal tyramine, dopamine and homovanillic acid.

    abstract::1 The concentrations of p- and m-tyramine, dopamine and homovanillic acid were measured in the mouse striatum following the subcutaneous administration of amfonelic acid, (+)-amphetamine or nomifensine.2 The administration of 2.5-25 mg/kg of amfonelic acid produced a reduction in p-tyramine that lasted at least 8 h. m...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1982.tb09325.x

    authors: Juorio AV

    更新日期:1982-11-01 00:00:00

  • Inhibition of poly(ADP-ribose) synthetase (PARS) and protection against peroxynitrite-induced cytotoxicity by zinc chelation.

    abstract::Peroxynitrite, a potent oxidant formed by the reaction of nitric oxide and superoxide causes thymocyte necrosis, in part, via activation of the nuclear enzyme poly(ADP-ribose) synthetase (PARS). The cytotoxic PARS pathway initiated by DNA strand breaks and excessive PARS activation has been shown to deplete cellular e...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702332

    authors: Virág L,Szabó C

    更新日期:1999-02-01 00:00:00

  • Acetal phosphatidic acids: novel platelet aggregating agents.

    abstract::1 Palmitaldehyde, olealdehyde and linolealdehyde acetal phosphatidic acids induced rapid shape change and dose-dependent biphasic aggregation of human platelets in platelet-rich plasma; aggregation was reversible at low doses and irreversible at high doses of the acetal phosphatidic acids. The palmitaldehyde congener ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1983.tb10508.x

    authors: Brammer JP,Maguire MH,Walaszek EJ,Wiley RA

    更新日期:1983-05-01 00:00:00

  • A monobromobimane-based assay to measure the pharmacokinetic profile of reactive sulphide species in blood.

    abstract:BACKGROUND AND PURPOSE:Hydrogen sulphide (H(2)S) is a labile, endogenous metabolite of cysteine, with multiple biological roles. The development of sulphide-based therapies for human diseases will benefit from a reliable method of quantifying H(2)S in blood and tissues. EXPERIMENTAL APPROACH:Concentrations of reactive...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.2010.00704.x

    authors: Wintner EA,Deckwerth TL,Langston W,Bengtsson A,Leviten D,Hill P,Insko MA,Dumpit R,VandenEkart E,Toombs CF,Szabo C

    更新日期:2010-06-01 00:00:00

  • Persistent nicotinic blockade by chlorisondamine of noradrenergic neurons in rat brain and cultured PC12 cells.

    abstract::Chlorisondamine (CHL) blocks behavioural responses to nicotine for several weeks or months in rats. Persistent blockade has also been demonstrated ex vivo, in assays of nicotine-evoked striatal dopamine release. Central administration of [3H]-CHL leads to long-term retention of radiolabel in nigrostriatal dopaminergic...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702215

    authors: Reuben M,Louis M,Clarke PB

    更新日期:1998-11-01 00:00:00

  • Rat pineal alpha 1-adrenoceptor subtypes: studies using radioligand binding and reverse transcription-polymerase chain reaction analysis.

    abstract::1. The pharmacological characteristics of alpha 1-adrenoceptor binding sites in rat pineal gland membranes, detected by use of a selective alpha 1-adrenoceptor antagonist ([125I]-iodo-2-[beta-(4-hydroxyphenyl) ethylaminomethyl]tetralone, [125I]-HEAT), were investigated with the alkylating agent, chloroethylclonidine (...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb15530.x

    authors: Sugden D,Anwar N,Klein DC

    更新日期:1996-07-01 00:00:00

  • Pharmacological characterization of the metabotropic glutamate receptor inhibiting D-[3H]-aspartate output in rat striatum.

    abstract::1. The effects of several agonists of the metabotropic glutamate receptor (mGluR) were studied in adult rat striatal slices by measuring (i) KCl (30 mM)-induced output of previously taken up D-[3H]-aspartate (Asp), (ii) forskolin (30 microM)-induced adenosine 3':5'-cyclic monophosphate (cyclic AMP) accumulation and (i...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1993.tb13977.x

    authors: Lombardi G,Alesiani M,Leonardi P,Cherici G,Pellicciari R,Moroni F

    更新日期:1993-12-01 00:00:00

  • Inhibition of nitric oxide synthase by 1-(2-trifluoromethylphenyl) imidazole (TRIM) in vitro: antinociceptive and cardiovascular effects.

    abstract::1. The ability of a range of substituted imidazole compounds to inhibit mouse cerebellar neuronal nitric oxide synthase (nNOS), bovine aortic endothelial NOS (eNOS) and inducible NOS (iNOS) from lungs of endotoxin-pretreated rats was investigated. In each case the substrate (L-arginine) concentration employed was 120 ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb16003.x

    authors: Handy RL,Harb HL,Wallace P,Gaffen Z,Whitehead KJ,Moore PK

    更新日期:1996-09-01 00:00:00

  • Time-dose relationships for locomotor activity effects of morphine after acute or repeated treatment.

    abstract::1. Effects of morphine sulphate (1.25, 2.5, 5, 10, 20 and 40 mg/kg i.p.) on locomotor activity of male rats were observed for 8 h after single doses in non-tolerant rats. The lower three doses had only an excitatory effect, whereas the higher three doses caused initial depression followed by a delayed excitatory effec...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1972.tb06866.x

    authors: Babbini M,Davis WM

    更新日期:1972-10-01 00:00:00

  • Different contributions of chemokine N-terminal features attest to a different ligand binding mode and a bias towards activation of ACKR3/CXCR7 compared with CXCR4 and CXCR3.

    abstract:BACKGROUND AND PURPOSE:Chemokines and their receptors form an intricate interaction and signalling network that plays critical roles in various physiological and pathological cellular processes. The high promiscuity and apparent redundancy of this network makes probing individual chemokine/receptor interactions and fun...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.14132

    authors: Szpakowska M,Nevins AM,Meyrath M,Rhainds D,D'huys T,Guité-Vinet F,Dupuis N,Gauthier PA,Counson M,Kleist A,St-Onge G,Hanson J,Schols D,Volkman BF,Heveker N,Chevigné A

    更新日期:2018-05-01 00:00:00

  • Determinants involved in subtype-specific functions of rat trace amine-associated receptors 1 and 4.

    abstract:AIMS:The trace amine-associated receptor (Taar) family displays high species- and subtype-specific pharmacology. Several trace amines such as β-phenylethylamine (β-PEA), p-tyramine and tryptamine are agonists at TA(1) but poorly activate rat and mouse Taar4. PRINCIPAL RESULTS:Using rat TA(1) and Taar4 chimera, we id...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12020

    authors: Stäubert C,Bohnekamp J,Schöneberg T

    更新日期:2013-03-01 00:00:00

  • Long-lasting activation of cation current by low concentration of endothelin-1 in mouse fibroblasts and smooth muscle cells of rabbit aorta.

    abstract::1. Recombinant human ETA receptors were expressed in a mouse fibroblast cell line (Ltk- cell) and functional coupling of the receptors with Ca2+ permeable channels at low concentrations of endothelin-1 (ET-1) was investigated using whole-cell recordings and monitoring the changes in intracellular free Ca2+ concentrati...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1995.tb16358.x

    authors: Enoki T,Miwa S,Sakamoto A,Minowa T,Komuro T,Kobayashi S,Ninomiya H,Masaki T

    更新日期:1995-06-01 00:00:00

  • Studies on the behavioural pharmacology of a cyclic analogue of dopamine following its injection into the brains of conscious rats.

    abstract::1. The cyclic analogue of dopamine, 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (ADTN) was injected into the lateral ventricle or bilaterally into the nucleus accumbens or caudate nucleus of conscious rats and its effect on locomotor activity was investigated. 2. When given intraventricularly, ADTN produced so...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1975.tb07416.x

    authors: Elkhawad AO,Woodruff GN

    更新日期:1975-05-01 00:00:00

  • Intrinsic defence capacity and therapeutic potential of natriuretic peptides in pulmonary hypertension associated with lung fibrosis.

    abstract:BACKGROUND AND PURPOSE:Idiopathic pulmonary fibrosis (IPF) is a progressive fibro-proliferative disorder refractory to current therapy commonly complicated by the development of pulmonary hypertension (PH); the associated morbidity and mortality are substantial. Natriuretic peptides possess vasodilator and anti-fibroti...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12694

    authors: Baliga RS,Scotton CJ,Trinder SL,Chambers RC,MacAllister RJ,Hobbs AJ

    更新日期:2014-07-01 00:00:00

  • Novel putative pharmacological therapies to protect the right ventricle in pulmonary hypertension: a review of current literature.

    abstract::Pulmonary hypertension (PH) is defined by elevated mean pulmonary artery pressure following the pathological remodelling of small pulmonary arteries. An increase in right ventricular (RV) afterload results in RV hypertrophy and RV failure. The pathophysiology of PH, and RV remodelling in particular, is not well unders...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.13721

    authors: Maarman GJ,Schulz R,Sliwa K,Schermuly RT,Lecour S

    更新日期:2017-04-01 00:00:00

  • Selectivity and potency of 2-alkyl analogues of the alpha 2-adrenoceptor antagonist idazoxan (RX 781094) in peripheral systems.

    abstract::The profiles of four analogues of idazoxan have been examined at alpha-adrenoceptors and the results compared to those obtained with idazoxan and yohimbine. The compounds possessed either a methyl (RX 801079), ethyl (RX 811033), n-propyl (RX 811054) or isopropenyl (RX 811005) group at the two position of idazoxan. The...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1984.tb16225.x

    authors: Doxey JC,Roach AG,Strachan DA,Virdee NK

    更新日期:1984-11-01 00:00:00

  • Trigeminal antidromic vasodilatation and plasma extravasation in the rat: effects of acetylcholine antagonists and cholinesterase inhibitors.

    abstract::Antidromic stimulation of sensory peripheral branches of the trigeminal system (mental nerve) leads to cutaneous vasodilatation and increases vascular permeability in the rat. Antidromic vasodilatation is observed only at high intensity stimulation (10 V, 15 Hz, 0.2 or 5 ms) supporting the participation of afferent C-...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1985.tb16144.x

    authors: Couture R,Cuello AC,Henry JL

    更新日期:1985-03-01 00:00:00

  • Inhibition by ethanol of NMDA-induced responses and acute tolerance to the inhibition in rat sympathetic preganglionic neurons in vitro and in vivo.

    abstract::N-methyl-d-aspartate (NMDA) receptors have been demonstrated to be a pivotal target for ethanol action. The present study examined the actions of acute ethanol exposure on NMDA-induced responses and the acute tolerance to ethanol actions in rat sympathetic preganglionic neurons (SPNs) in vitro and in vivo. NMDA (50 mi...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705512

    authors: Lin HH,Hsieh WK,Shiu JY,Chiu TH,Lai CC

    更新日期:2003-11-01 00:00:00

  • Resistance to myocardial infarction induced by heat stress and the effect of ATP-sensitive potassium channel blockade in the rat isolated heart.

    abstract::1. Heat stress (HS) is known to protect against myocardial ischaemia-reperfusion injury by improving mechanical dysfunction and decreasing necrosis. However, the mechanisms responsible for this form of cardioprotection remain to be elucidated. ATP-sensitive potassium (K(ATP)) channels have been shown to be involved in...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701710

    authors: Joyeux M,Godin-Ribuot D,Ribuot C

    更新日期:1998-03-01 00:00:00

  • LF 16.0335, a novel potent and selective nonpeptide antagonist of the human bradykinin B2 receptor.

    abstract::1. In the present paper, we describe the in vitro pharmacological properties of LF 16.0335 (1-[[3-[(2,4-dimethylquinolin-8-yl)oxymethyl]-2,4-dichloro-p henyl]sulphonyl] -2(S) - [[4 -[4-(aminoiminomethyl)phenylcarbonyl]piperazin-1-yl]ca rbonyl]pyrrolidine), a novel and potent nonpeptide antagonist of the human bradykin...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702083

    authors: Pruneau D,Luccarini JM,Fouchet C,Defrêne E,Franck RM,Loillier B,Duclos H,Robert C,Cremers B,Bélichard P,Paquet JL

    更新日期:1998-09-01 00:00:00

  • Insights into the function of opioid receptors from molecular dynamics simulations of available crystal structures.

    abstract::The opioid receptors are key targets in the treatment of acute and chronic pain, and the development of novel analgesics with reduced side effects is crucial in the search for more effective medications. The crystal structures of opioid receptors have provided a wealth of knowledge on many aspects of opioid receptor p...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.13774

    authors: Marino KA,Shang Y,Filizola M

    更新日期:2018-07-01 00:00:00

  • Recent progress in the understanding of relaxin family peptides and their receptors.

    abstract:LINKED ARTICLES:This article is part of a themed section on Recent Progress in the Understanding of Relaxin Family Peptides and their Receptors. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v174.10/issuetoc. ...

    journal_title:British journal of pharmacology

    pub_type: 社论

    doi:10.1111/bph.13778

    authors: Summers RJ

    更新日期:2017-05-01 00:00:00

  • RhoA kinase and protein kinase C participate in regulation of rabbit stomach fundus smooth muscle contraction.

    abstract::1. The degree to which the RhoA kinase (ROK) blockers, Y-27632 (1 micro M) and HA-1077 (10 micro M), and the PKC blocker, GF-109203X (1 micro M), reduced force produced by carbachol, a muscarinic receptor agonist, and phenylephrine, an alpha-adrenoceptor agonist, was examined in rabbit stomach fundus smooth muscle. 2....

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704952

    authors: Ratz PH,Meehl JT,Eddinger TJ

    更新日期:2002-12-01 00:00:00

  • Altered pharmacology of native rodent spinal cord TRPV1 after phosphorylation.

    abstract:BACKGROUND AND PURPOSE:Evidence suggests that phosphorylation of TRPV1 is an important component underlying its aberrant activation in pathological pain states. To date, the detailed pharmacology of diverse TRPV1 receptor agonists and antagonists has yet to be reported for native TRPV1 under phosphorylating conditions....

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12005

    authors: Mogg AJ,Mill CE,Folly EA,Beattie RE,Blanco MJ,Beck JP,Broad LM

    更新日期:2013-02-01 00:00:00

  • The role of cyclic AMP in non-adrenergic non-cholinergic contraction in guinea-pig bronchi.

    abstract::1. We investigated the role of adenosine 3':5'-cyclic monophosphate (cyclic AMP) in non-adrenergic non-cholinergic (NANC) contraction in guinea-pig bronchial strips. 2. Forskolin (3 nM to 1 microM) reduced NANC contraction induced by electrical field stimulation (EFS) in a concentration-dependent fashion (-log EC50 wa...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1992.tb09027.x

    authors: Aikawa T,Sekizawa K,Morikawa M,Itabashi S,Sasaki H,Takishima T

    更新日期:1992-03-01 00:00:00

  • Blockade of the development of morphine tolerance by U-50,488, an AVP antagonist or MK-801 in the rat hippocampal slice.

    abstract::1. In this study, we investigated the effects of different drugs (a kappa-opioid receptor agonist U-50,488, a vasopressin receptor antagonist dPTyr(Me)AVP or an N-methyl-D-aspartate (NMDA) receptor antagonist MK-801) on the development of morphine tolerance in rat hippocampal slices. 2. Hippocampal slices (450 microm)...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0701646

    authors: Su MT,Lin WB,Lue WM,Cheng CY,Tao PL

    更新日期:1998-02-01 00:00:00