Thermodynamic analysis of agonist and antagonist binding to the chicken brain melatonin receptor.

Abstract:

:1. The binding of 2-[125I]-iodomelatonin to chicken brain membranes, and the inhibition of binding by melatonin, N-acetyltryptamine and luzindole, were examined at temperatures between 4 degrees C and 37 degrees C. 2. At all temperatures studied, the binding affinity (Kd or Ki) for 2-[125I]-iodomelatonin, melatonin (both agonists) and, to a lesser extent, N-acetyltryptamine (a partial agonist) was reduced by inclusion of guanosine triphosphate (GTP, 1 mM) in the assay. GTP did not affect the Ki for luzindole, a melatonin receptor antagonist. 3. The maximal density of binding sites (Bmax) was not affected by temperature but the Kd showed a peak at 21 degrees C with lower values at both higher and lower temperatures giving curvilinear van't Hoff plots (lnKA vs l/temperature). 4. Derived changes in entropy (delta S degree) and enthalpy (delta H degree) of binding for all of the melatonin ligands decreased as temperature increased. 5. The affinity, and thus the free energy of binding, delta G degree, of these ligands at the melatonin receptor have identical values at several temperatures yet at these temperatures delta S degree and delta H degree were very different, implying that more than one intermolecular force must be involved in the binding of ligand and receptor. 6. Conceivably, the large positive delta S degree observed at low temperatures, perhaps as a result of hydrophobic interactions, is compensated by a corresponding, but opposite, change in enthalpy at higher temperatures. However, it is not clear what type of binding force(s) would show such a temperature-dependence. 7. These studies suggest that caution must be exercised in the molecular interpretation of derived measures of delta S degree and delta H degree obtained from direct measurements of delta G degree.

journal_name

Br J Pharmacol

authors

Chong NW,Sugden D

doi

10.1111/j.1476-5381.1994.tb14059.x

subject

Has Abstract

pub_date

1994-01-01 00:00:00

pages

295-301

issue

1

eissn

0007-1188

issn

1476-5381

journal_volume

111

pub_type

杂志文章
  • Microbial biotransformations in the human distal gut.

    abstract::The human distal gut is home to a rich and dense microbial community with representatives of all three domains of life which are intricately connected with our physiology and health. The combined genomes of these microbes, collectively called the human microbiome, vastly expand the metabolic capacities of our own geno...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.14085

    authors: Bik EM,Ugalde JA,Cousins J,Goddard AD,Richman J,Apte ZS

    更新日期:2018-12-01 00:00:00

  • Activation of I(2)-imidazoline receptors enhances supraspinal morphine analgesia in mice: a model to detect agonist and antagonist activities at these receptors.

    abstract::This work investigates the receptor acted upon by imidazoline compounds in the modulation of morphine analgesia. The effects of highly selective imidazoline ligands on the supraspinal antinociception induced by morphine in mice were determined. 2. Intracerebroventricular (i.c.v.) or subcutaneous (s.c.) administration ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703294

    authors: Sánchez-Blázquez P,Boronat MA,Olmos G,García-Sevilla JA,Garzón J

    更新日期:2000-05-01 00:00:00

  • Determination of halothane-induced sleeping time in the rat: effect of prior administration of centrally active drugs.

    abstract::A method is described for the determination of halothane-induced sleeping time in the rat. 2 The sleeping time exhibited a diurnal variation which was due, at least in part, to a change in the sensitivity of the central nervous system (CNS) to the anaesthetic. 3 Tolerance to halothane did not develop in rats repeatedl...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1976.tb07689.x

    authors: Turnbull MJ,Watkins JW

    更新日期:1976-09-01 00:00:00

  • Phosphodiesterase 4D: an enzyme to remember.

    abstract::Cyclic adenosine monophosphate (cAMP) is one of the second messengers critically involved in the molecular mechanisms underlying memory formation. In the CNS, the availability of cAMP is tightly controlled by phosphodiesterase 4 (PDE4), a family of enzymes that degrades the cyclic nucleotide to inactive AMP. Among the...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/bph.13257

    authors: Ricciarelli R,Fedele E

    更新日期:2015-10-01 00:00:00

  • Comparative effects of glyceryl trinitrate on venous and arterial smooth muscle in vitro; relevance to antianginal activity.

    abstract::1. A quantitative in vitro study has been made of the actions of glyceryl trinitrate and sodium nitrite on vascular smooth muscle (dog femoral artery and saphenous vein; rat portal vein); these have been compared with the actions of papaverine, isoprenaline, salbutamol, pentaerythritol tetranitrate and trimetazidine. ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1977.tb16760.x

    authors: Mackenzie JE,Parratt JR

    更新日期:1977-05-01 00:00:00

  • The effect of Kö 1173, a new anticonvulsant agent on experimental cardiac arrhythmias.

    abstract::1. The effects of the intravenous injection of Kö 1173, a new anticonvulsant drug, phenytoin and procainamide were studied on three types of cardiac arrhythmia in dogs.2. Ventricular ectopic beats produced by intravenous injection of adrenaline in anaesthetized dogs respired with halothane were abolished by Kö 1173, 0...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1972.tb08114.x

    authors: Allen JD,Ekue JM,Shanks RG,Zaidi SA

    更新日期:1972-08-01 00:00:00

  • Action of agonists and antagonists at muscarinic receptors present on ileum and atria in vitro.

    abstract::The action of 'selective' agonists and antagonists at muscarinic receptors mediating ileal contractions, and the rate and force of atrial contractions has been assessed. The effect of nicotinic receptor stimulation, catecholamine release and acetylcholinesterase (AChE) action on muscarinic activity has also been asses...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1985.tb09446.x

    authors: Clague RU,Eglen RM,Strachan AC,Whiting RL

    更新日期:1985-09-01 00:00:00

  • Androgen receptor antagonism accelerates disease onset in the SOD1G93A mouse model of amyotrophic lateral sclerosis.

    abstract:BACKGROUND AND PURPOSE:Amyotrophic lateral sclerosis (ALS) is a fatal neurodegenerative disease typically more common in males, implicating androgens in progression of both patients and mouse models. Androgen effects are mediated by androgen receptor which is highly expressed in spinal motor neurons and skeletal muscle...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.14657

    authors: McLeod VM,Lau CL,Chiam MDF,Rupasinghe TW,Roessner U,Djouma E,Boon WC,Turner BJ

    更新日期:2019-07-01 00:00:00

  • Inhibition of polycomb repressor complex 2 ameliorates neointimal hyperplasia by suppressing trimethylation of H3K27 in vascular smooth muscle cells.

    abstract:BACKGROUND AND PURPOSE:The increased proliferation and migration of vascular smooth muscle cells (VSMCs) after arterial injury contributes greatly to the pathogenesis of neointimal hyperplasia. As a major component of epigenetics, histone methylation plays an important role in several cardiovascular diseases. However, ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.14754

    authors: Liang J,Li Q,Cai W,Zhang X,Yang B,Li X,Jiang S,Tian S,Zhang K,Song H,Ai D,Zhang X,Wang C,Zhu Y

    更新日期:2019-09-01 00:00:00

  • YM-53601, a novel squalene synthase inhibitor, reduces plasma cholesterol and triglyceride levels in several animal species.

    abstract::The aim of this study was to evaluate the potency of YM-53601 ((E)-2-[2-fluoro-2-(quinuclidin-3-ylidene) ethoxy]-9H-carbazole monohydrochloride), a new inhibitor of squalene synthase, in reducing both plasma cholesterol and triglyceride levels, compared with 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase in...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0703545

    authors: Ugawa T,Kakuta H,Moritani H,Matsuda K,Ishihara T,Yamaguchi M,Naganuma S,Iizumi Y,Shikama H

    更新日期:2000-09-01 00:00:00

  • Plasmid encoded antibiotic resistance: acquisition and transfer of antibiotic resistance genes in bacteria.

    abstract::Bacteria have existed on Earth for three billion years or so and have become adept at protecting themselves against toxic chemicals. Antibiotics have been in clinical use for a little more than 6 decades. That antibiotic resistance is now a major clinical problem all over the world attests to the success and speed of ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1038/sj.bjp.0707607

    authors: Bennett PM

    更新日期:2008-03-01 00:00:00

  • Toll-like receptor 4 contributes to vascular remodelling and endothelial dysfunction in angiotensin II-induced hypertension.

    abstract:BACKGROUND AND PURPOSE:Toll-like receptor 4 (TLR4) signalling contributes to inflammatory cardiovascular diseases, but its role in hypertension and the associated vascular damage is not known. We investigated whether TLR4 activation contributed to angiotensin II (AngII)-induced hypertension and the associated vascular ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13117

    authors: Hernanz R,Martínez-Revelles S,Palacios R,Martín A,Cachofeiro V,Aguado A,García-Redondo L,Barrús MT,de Batista PR,Briones AM,Salaices M,Alonso MJ

    更新日期:2015-06-01 00:00:00

  • The effect of arginine and nitric oxide on resistance blood vessels of the perfused rat kidney.

    abstract::1. The vasodilator effects of arginine, nitric oxide (NO), acetylcholine (ACh) and sodium nitroprusside (NP) in the noradrenaline-preconstricted ('high tone') perfused rat kidney have been examined. 2. L-Arginine (0.6-23 mumol) caused a biphasic change in renal perfusion pressure. D-Arginine (0.6-23 mumol) was without...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1989.tb12011.x

    authors: Bhardwaj R,Moore PK

    更新日期:1989-07-01 00:00:00

  • Different pharmacological profiles of big-endothelin-3 and big-endothelin-1 in vivo and in vitro.

    abstract::1. Human big-endothelin-1 (big-ET-1) and endothelin-1 (ET-1) are equipotent as pressor agents and produce a significant change in mean arterial blood pressure (MAP) in anaesthetized guinea-pigs (2 nmol kg-1: peak delta MAP: 23 +/- 6 mmHg and 26 +/- 5 mmHg, respectively). 2. Unlike big-ET-1, big-endothelin-3 (big-ET-3)...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1991.tb12448.x

    authors: D'Orléans-Juste P,Télémaque S,Claing A

    更新日期:1991-10-01 00:00:00

  • GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation.

    abstract::Peroxisome proliferator-activated receptor gamma (PPARgamma), a member of the nuclear receptor superfamily, is activated by several compounds, including the thiazolidinediones. In addition to being a therapeutic target for obesity, hypolipidaemia and diabetes, perturbation of PPARgamma signalling is now believed to be...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705973

    authors: Seargent JM,Yates EA,Gill JH

    更新日期:2004-12-01 00:00:00

  • Platelet P2Y₁₂ receptors are involved in the haemostatic effect of notoginsenoside Ft1, a saponin isolated from Panax notoginseng.

    abstract:BACKGROUND AND PURPOSE:Saponins isolated from Panax notoginseng (Burk.) F.H. Chen have been shown to relieve thrombogenesis and facilitate haemostasis. However, it is not known which saponin accounts for this haemostatic effect. Hence, in the present study we aimed to identify which saponins contribute to its haemostat...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.12435

    authors: Gao B,Huang L,Liu H,Wu H,Zhang E,Yang L,Wu X,Wang Z

    更新日期:2014-01-01 00:00:00

  • Enhancement of vascular permeability by specific activation of protease-activated receptor-1 in rat hindpaw: a protective role of endogenous and exogenous nitric oxide.

    abstract::1. To clarify the role of the first thrombin receptor/protease-activated receptor (PAR)-1 in an inflammatory process, we tested and characterized the effect of intraplantar (i.pl.) administration of the highly specific PAR-1 agonist TFLLR-NH2 in rat hindpaw. 2. TFLLR-NH2 administered i.pl. at 0.01-0.03 micromol per pa...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702513

    authors: Kawabata A,Kuroda R,Nishikawa H,Asai T,Kataoka K,Taneda M

    更新日期:1999-04-01 00:00:00

  • Antithrombotic activity of a monoclonal antibody inducing the substrate form of plasminogen activator inhibitor type 1 in rat models of venous and arterial thrombosis.

    abstract::1. Elevated plasminogen activator inhibitor 1 (PAI-1) is a risk factor for thrombosis, and inhibitors of the interaction between PAI-1 and tissue plasminogen activator (t-PA) have antithrombotic and prothrombolytic activity in animals. We describe the antithrombotic effects in the rat of a monoclonal antibody (MA33H1)...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0702030

    authors: Berry CN,Lunven C,Lechaire I,Girardot C,O'Connor SE

    更新日期:1998-09-01 00:00:00

  • Increase in neuropeptide Y activity impairs social behaviour in association with glutamatergic dysregulation in diabetic mice.

    abstract:BACKGROUND AND PURPOSE:Patients with diabetes mellitus are reported to show a raised prevalence of mental disorders, which may be reflected in impaired social interaction. However, the mechanisms underlying such impairment in diabetes are unknown. EXPERIMENTAL APPROACH:The present study investigated whether social int...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.15326

    authors: Ueda D,Yonemochi N,Kamata T,Shibasaki M,Kamei J,Waddington JL,Ikeda H

    更新日期:2021-02-01 00:00:00

  • Positive correlation between initial pupil diameter and amplitude of miotic response to pilocarpine in rabbits and to carbachol in man.

    abstract::A linear correlation between amplitude of miotic response and initial pupil diameter has been demonstrated in rabbits using various concentrations of pilocarpine HC1. The same correlation was found when published results in humans using carbachol were examined and it is likely that the correlation also applies to pilo...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1970.tb10635.x

    authors: Burns J,Horlington M,Robson D

    更新日期:1970-11-01 00:00:00

  • Effects of the AT1-receptor antagonist eprosartan on the progression of left ventricular dysfunction in dogs with heart failure.

    abstract::1. We examined the effects of eprosartan, an AT(1) receptor antagonist, on the progression of left ventricular (LV) dysfunction and remodelling in dogs with heart failure (HF) produced by intracoronary microembolizations (LV ejection fraction, EF 30 to 40%). 2. Dogs were randomized to 3 months of oral therapy with low...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0705032

    authors: Suzuki G,Mishima T,Tanhehco EJ,Sharov VG,Todor A,Rostogi S,Gupta RC,Chaudhry PA,Anagnostopoulos PV,Nass O,Goldstein S,Sabbah HN

    更新日期:2003-01-01 00:00:00

  • In vitro effects of non-steroidal anti-inflammatory drugs on human polymorphonuclear cells and lymphocyte migration.

    abstract::1. The action of the non-steroidal anti-inflammatory drugs (NSAID), sodium salicylate, aspirin, phenylbutazone and indomethacin was investigated on the migration of human polymorphonuclear cells (PMNs) and lymphocytes, using the system of migration of leucocytes from glass capillary tubes. 2. All NSAID produced a dose...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:

    authors: Brown KA,Collins AJ

    更新日期:1978-11-01 00:00:00

  • The effect of cold storage on the inhibitory action of isoprenaline, phenylephrine and nicotine on the mechanical and membranal activities of guinea-pig taenia caecum.

    abstract::1. The effects of prolonged cold storage on the mechanical and membranal responses to stimulation of alpha- and beta-adrenoceptors by phenylephrine and isoprenaline, respectively, were studied on the guinea-pig taenia caecum.2. Cold storage invariably caused a decrease in the resting membrane potential, and this effec...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1972.tb08141.x

    authors: Fukuda H,Shibata S

    更新日期:1972-11-01 00:00:00

  • An effect of haloperidol on the increased food and water intake induced in rabbits by 2-deoxy-D-glucose.

    abstract::Rabbits treated with 2-deoxy-D-glucose (2DG) (300 mg/kg) show an increased intake of food and water. Pretreatment with haloperidol (1 mg/kg) abolishes the increase in water intake but does not prevent the increase in food intake. ...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:

    authors: Anderson J,Sharman DF,Stephens DB

    更新日期:1979-05-01 00:00:00

  • Locomotor effects of imidazoline I2-site-specific ligands and monoamine oxidase inhibitors in rats with a unilateral 6-hydroxydopamine lesion of the nigrostriatal pathway.

    abstract::The present study examined the ability of the selective imidazoline I(2)-site ligands 2-(-2-benzofuranyl)-2-imidazoline (2-BFI) and 2-[4,5-dihydroimidaz-2-yl]-quinoline (BU224) and selected monoamine oxidase (MAO) inhibitors to evoke locomotor activity in rats bearing a lesion of the nigrostriatal pathway. Male Spragu...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0706019

    authors: Macinnes N,Duty S

    更新日期:2004-12-01 00:00:00

  • Capsinolol: the first beta-adrenoceptor blocker with an associated calcitonin gene-related peptide releasing activity in the heart.

    abstract::1. The beta-adrenoceptor blocking and calcitonin gene-related peptide (CGRP)-releasing properties of capsinolol (N-[4-(2-hydroxy-3 (isopropylamino) propoxy)-3-methoxybenzyl]-nonanamide), derived from nonivamide, were investigated under in vivo and in vitro conditions. 2. Capsinolol (0.1, 0.5, 1.0 mg kg-1, i.v.), as we...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/j.1476-5381.1996.tb15670.x

    authors: Chen IJ,Yeh JL,Lo YC,Sheu SH,Lin YT

    更新日期:1996-09-01 00:00:00

  • Metformin attenuates angiotensin II-induced TGFβ1 expression by targeting hepatocyte nuclear factor-4-α.

    abstract:BACKGROUND AND PURPOSE:Metformin, a small molecule, antihyperglycaemic agent, is a well-known activator of AMP-activated protein kinase (AMPK) and protects against cardiac fibrosis. However, the underlying mechanisms remain elusive. TGFβ1 is a key cytokine mediating cardiac fibrosis. Here, we investigated the effects o...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1111/bph.13753

    authors: Chen R,Feng Y,Wu J,Song Y,Li H,Shen Q,Li D,Zhang J,Lu Z,Xiao H,Zhang Y

    更新日期:2018-04-01 00:00:00

  • Effects of chronic in vivo administration of nitroglycerine on ACh-induced endothelium-dependent relaxation in rabbit cerebral arteries.

    abstract:BACKGROUND AND PURPOSE:In the setting of nitrate tolerance, endothelium-dependent relaxation is reduced in several types of peripheral vessels. However, it is unknown whether chronic in vivo administration of nitroglycerine modulates such relaxation in cerebral arteries. EXPERIMENTAL APPROACH:Isometric force and smoot...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0707562

    authors: Watanabe Y,Kusama N,Itoh T

    更新日期:2008-01-01 00:00:00

  • Disruption of inflammatory signals by cytokine-targeted therapies for inflammatory bowel diseases.

    abstract::Gut inflammation occurring in patients with inflammatory bowel diseases (IBD) is associated with an excessive immune response that is directed against constituents of the normal bacterial flora and results in the production of large amounts of inflammatory cytokines. Anti-cytokine compounds, such as the neutralizing T...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章,评审

    doi:10.1111/j.1476-5381.2011.01614.x

    authors: Caprioli F,Caruso R,Sarra M,Pallone F,Monteleone G

    更新日期:2012-02-01 00:00:00

  • 5-HT(2B) receptors play a key role in mediating the excitatory effects of 5-HT in human colon in vitro.

    abstract::1. 5-Hydroxytryptamine (5-HT) is known to produce a number of different effects in the gastrointestinal tract of various species, and has been proposed to play a key role in a number of intestinal disorders in man, including irritable bowel syndrome (IBS), although the receptors involved have yet to be established. Th...

    journal_title:British journal of pharmacology

    pub_type: 杂志文章

    doi:10.1038/sj.bjp.0704571

    authors: Borman RA,Tilford NS,Harmer DW,Day N,Ellis ES,Sheldrick RL,Carey J,Coleman RA,Baxter GS

    更新日期:2002-03-01 00:00:00