Abstract:
:Large species differences have been previously observed in the pharmacology of bradykinin (BK) B2 receptor antagonists. We investigated the effect of two novel non-peptide antagonists, compound 9 (a benzodiazepine peptidomimetic related to icatibant) and the thiosemicarbazide bradyzide on the rabbit B2 receptor (contractility of the jugular vein, competition of [3H]BK binding to a B2 receptor-green fluorescent protein (B2R-GFP) conjugate, subcellular distribution of B2R-GFP). While compound 9 is about 9000-fold less potent than icatibant, it shares with the latter peptide drug a selective, insurmountable and largely irreversible antagonist behavior against BK and the capacity to translocate B2R-GFP from the membrane into the cells. Bradyzide, reportedly very potent at rodent B2 receptors, was a competitive and reversible antagonist of moderate potency at the rabbit B2 receptor (contractility pA2 6.84, binding competition IC50 5 nM). The C-terminal region of icatibant, reproduced by compound 9, is likely to be important in the non-equilibrium behavior of icatibant. Bradyzide, a non-peptide antagonist developed on different structural grounds, is competitive at the rabbit B2 receptor.
journal_name
Peptidesjournal_title
Peptidesauthors
Marceau F,Houle S,Bouthillier J,Said NB,Garratt PJ,Dziadulewicz EKdoi
10.1016/s0196-9781(01)00481-8subject
Has Abstractpub_date
2001-09-01 00:00:00pages
1397-402issue
9eissn
0196-9781issn
1873-5169pii
S0196-9781(01)00481-8journal_volume
22pub_type
杂志文章相关文献
PEPTIDES文献大全abstract::Biological and immunological relationships between molt-inhibiting hormone (MIH) activity in eyestalk ganglia extracts of the crab, Cancer antennarius Stimpson, and peptides of the vasopressin-oxytocin family were assessed. Lysine vasopressin (LVP), arginine vasopressin (AVP), vasotocin (VT), and oxytocin (OT) mimicke...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(85)90166-4
更新日期:1985-07-01 00:00:00
abstract::A pancreatic ductal carcinoma was established as a transplantable tumor line in an inbred strain of Syrian golden hamsters. Intracellular recordings of membrane potentials and input resistance were made from cultured cells obtained from the transplanted tumors using indwelling glass microelectrode. The mean value of t...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(84)90247-x
更新日期:1984-03-01 00:00:00
abstract::Antibodies to the extreme C-terminal pentapeptide of procholecystokinin, YEYPS (in the single letter notation), have been used in radioimmunoassay and immunohistochemistry to characterize the material in rat intestine. There is a single major immunoreactive peptide in intestinal extracts that has the properties of the...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(87)90170-7
更新日期:1987-01-01 00:00:00
abstract::Glucocorticoids have been shown to decrease CRF receptor binding in the anterior pituitary. To determine whether glucocorticoids or CRF peptide modulate CRF-R1 gene expression, CRF-R1 mRNA levels in rat pituitary and brain were measured after administration of a synthetic glucocorticoid, dexamethasone (DEX) or rat/hum...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(96)00014-9
更新日期:1996-01-01 00:00:00
abstract::Orexin (ORX) plays a critical role in reward-seeking behavior for natural rewards and drugs of abuse. The mesolimbic dopamine (DA) pathway that projects into the nucleus accumbens (NAc) from the ventral tegmental area is deeply involved in the neural mechanisms underlying reward, drug abuse and motivation. A recent st...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2010.10.023
更新日期:2011-02-01 00:00:00
abstract::VIP and secretin control the secretory function of the normal pancreas. We analysed their regulatory functions in a human pancreatic cancer cell line: Capan-1. Saturation binding experiments with 125I-VIP showed the existence of one class of binding sites of very high affinity: KD 6.4 +/- 3.0 X 10(-11) M and a low Bma...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(86)90200-7
更新日期:1986-01-01 00:00:00
abstract::CGRP has potent cardiovascular effects but its role in heart failure is unclear. Effects of CGRP on calcium concentrations in fresh adult rat cardiomyocytes, cultured adult cardiomyocytes and neonatal cardiomyocytes were determined by real time fluorescence spectrophotometry. Treatment of cultured adult cardiomyocytes...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2004.10.020
更新日期:2005-03-01 00:00:00
abstract::The secretin receptor is a member of a large family of G-protein-coupled receptors that recognize polypeptide hormone and/or neuropeptides. Charged, conserved residues might play a key role in their function, either by interacting with the ligand or by stabilizing the receptor structure. Of the four charged amino acid...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(99)00122-9
更新日期:1999-01-01 00:00:00
abstract::alpha-MSH stimulates steroid secretion by rat adrenal zona glomerulosa cells and tissues but not fasciculata/reticularis cells when added to in vitro incubations. With glomerulosa cells from control animals on a normal sodium intake, production of corticosterone was significantly stimulated at an alpha-MSH concentrati...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(81)80026-5
更新日期:1981-07-01 00:00:00
abstract::Antisauvagine-30 (aSVG) is the only high-affinity antagonist for the corticotropin-releasing factor (CRF) type 2 (CRF(2)) receptor. A structure-activity relationship study was performed to pinpoint residues conferring aSVG's selectivity. The aSVG-analogues being N-terminally extended by one or two residues or containi...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(02)00139-0
更新日期:2002-10-01 00:00:00
abstract::Liver-expressed antimicrobial peptide 2 (LEAP-2) is a 40-residue cationic peptide originally purified from human blood ultrafiltrate. The native peptide contains two disulfide bonds and is unique regarding its primary structure. Its biological role is not known but a previous study showed that chemically synthesized L...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2009.10.006
更新日期:2010-01-01 00:00:00
abstract::TRH and PS-24 (a TRH peptidase resistant analogue) induce different effects on body temperature and motor activity in rats kept at 4 degrees C. PS-24 induced hypothermia, but TRH did not. PS-24 induced hypermotility, while TRH induced slight hypomotility. The thermal effect of TRH in hypophysectomized rats was similar...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(81)80024-1
更新日期:1981-07-01 00:00:00
abstract::The renin-angiotensin system (RAS) is now recognized as an important modulator of body metabolic processes. The discovery of angiotensin-converting enzyme 2 (ACE2) has renewed interest in the potential therapeutic role of RAS modulation. Recent studies have pointed out the importance of the local balance between ACE/A...
journal_title:Peptides
pub_type: 杂志文章,评审
doi:10.1016/j.peptides.2014.10.005
更新日期:2014-12-01 00:00:00
abstract::This mass spectrometric study confines itself to peptide masses in the range of 500-1500Da. Adipokinetic hormones (AKHs) that are predicted from the genome of the red flour beetle, Tribolium castaneum, and the silk moth, Bombyx mori, are shown to exist as expressed peptides in the corpora cardiaca (CC) of the respecti...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2008.03.002
更新日期:2008-07-01 00:00:00
abstract::C-type natriuretic peptide (CNP) was recently found in the myocardium, but possible insights into differences between atrium and ventricle production are so far lacking. Our aim was to evaluate, in an experimental model of pacing-induced heart failure (HF), plasma and tissue levels of CNP and mRNA expression of the pe...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2008.09.005
更新日期:2008-12-01 00:00:00
abstract::The study was undertaken to investigate the oxidation and reduction of cholecystokinin (CCK) both as pure standards and as endogenous porcine peptides. Furthermore an attempt was made to prevent oxidation of the endogenous porcine peptides in the extraction procedure. CCK-8 and CCK-33 standards were always oxidized in...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(85)90069-5
更新日期:1985-01-01 00:00:00
abstract::Orexin is one of the orexigenic neuropeptides in the hypothalamus. Orexin neurons in the lateral hypothalamus (LH) project into the cerebral cortex and hippocampus in which the receptors are distributed in high concentrations. Therefore, to elucidate the actions of orexin in the cerebral cortex, we examined its effect...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2008.05.002
更新日期:2008-09-01 00:00:00
abstract::Gastric inhibitory polypeptide (GIP) is a 42-amino acid peptide, belonging to the VIP-secretin-glucagon superfamily, some members of this group are able to regulate adrenocortical function. GIP-receptor mRNA has been detected in the rat adrenal cortex, but investigations on the effect of GIP on steroid-hormone secreti...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(99)00011-x
更新日期:1999-01-01 00:00:00
abstract::Glucagon is a peptide hormone secreted from the pancreatic alpha cells in response to hypoglycemia but in some patients with type 2 diabetes a paradoxical hypersecretion results from the intake of glucose. In rodent, antagonizing the actions of glucagon have been shown to be effective for lowering blood glucose levels...
journal_title:Peptides
pub_type: 杂志文章,评审
doi:10.1016/j.peptides.2017.11.016
更新日期:2018-02-01 00:00:00
abstract::Incorporation of N-succinimidyl-3(4-hydroxyphenyl) propionate (Bolton-Hunter reagent) or its 125I-labeled derivative into peptides can be selectively directed towards either alpha- or epsilon-amine functions by modifying the pH of the reaction. Acylation of alpha-amino groups is favored at pH 6.5 whereas epsilon-amino...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(92)90027-z
更新日期:1992-11-01 00:00:00
abstract::We examined the mechanism through which leptin increases Na(+), K(+)-ATPase activity in the rat kidney. Leptin was infused under anaesthesia into the abdominal aorta proximally to the renal arteries and then Na(+), K(+)-ATPase activity was measured in the renal cortex and medulla. Leptin (1mug/kgmin) increased Na(+), ...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2006.08.010
更新日期:2006-12-01 00:00:00
abstract::Many neuroendocrine peptides that are distributed in amphibian gastrointestinal tract and central nervous system are also found in amphibian skins, and these peptides are classified into skin-gut-brain triangle peptides, such as bombesins, gastrin-releasing peptides. Cholecystokinins (CCKs) are neuroendocrine peptides...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2007.07.006
更新日期:2007-08-01 00:00:00
abstract::Dissociated muscle cells prepared from hearts of the pulmonate snail Helix aspersa were used to study signal transduction induced by molluscan cardioactive peptides. The effects of SCPb on the cAMP levels of whole hearts and the cell preparation were compared. The cells responded to SCPb with a dose-dependent increase...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(97)00196-4
更新日期:1997-01-01 00:00:00
abstract::The experiments reported here investigate the conditionability, using taste aversion conditioning, of the antagonistic effects of alpha-MSH on the thermoregulatory changes associated with injection of bacterial endotoxin lipopolysaccharide (LPS) in rats. Animals were administered LPS and then given alpha-MSH, as an un...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(94)90182-1
更新日期:1994-01-01 00:00:00
abstract::In lieu of H-Dmt-Tic-OH, H-Dmt-analogues included 2-amino-3(1H-benzoimidazol-2-yl)-propionic acid, N(Bzl)Gly, L-octahydroindole-2-carboxylic acid, [3S-(3alpha,4abeta, 8abeta)]-decahydro-3-isoquinoline carboxylic acid, benzimidazole-, pyridoindole- or spiroinden-derivatives, or C-terminally modified. L- or D-Ala, Sar, ...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/s0196-9781(00)00315-6
更新日期:2000-11-01 00:00:00
abstract::Naltrexone, an opiate antagonist, was administered to young obese (ob/ob) and lean mice for five weeks. Animals had continuous access to food and received 10 mg/kg SC twice daily with equivalent volumes of saline given to controls. The effects on body weight, and pituitary and plasma levels of beta-endorphin-like mate...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(80)90008-x
更新日期:1980-01-01 00:00:00
abstract::Opioid-like immunoreactive material was extracted from the pituitary and brain of the Spiny Dogfish Shark Squalus acanthias. The immunoreactive material in the pituitary extracts was purified to apparent homogeneity by reverse phase high performance liquid chromatography and subsequently characterized by amino acid an...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(86)90071-9
更新日期:1986-01-01 00:00:00
abstract::We employed a proteomic approach to search for peptides that have a physiological role in labor. Cervicovaginal secretions were collected at term from women in labor and women at term not in labor. Samples were spotted onto weak cation exchange chips (WCX-2) and analyzed using Surface-Enhanced Laser Desorption Ionizat...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2006.03.015
更新日期:2006-07-01 00:00:00
abstract::The binding of monoiodo 125I-Trp11-neurotensin to purified rat gastric fundus smooth muscle plasma membranes was characterized. Specific binding of ligand in subcellular fractions from rat fundus smooth muscle showed a distribution that paralleled that of several plasma membrane marker enzymes. 125I-Trp11-neurotensin ...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/0196-9781(84)90117-7
更新日期:1984-09-01 00:00:00
abstract::Trefoil factor family (TFF) 1, 2, and 3 is a mucin-associated protein involved in the maintenance of mucosal barrier and restitution of lining epithelial cells. In this study, the expression of TFF1, 2, and 3 and MUC mucins were examined immunohistochemically in hepatolithiasis and control livers. The expression of TF...
journal_title:Peptides
pub_type: 杂志文章
doi:10.1016/j.peptides.2003.12.023
更新日期:2004-05-01 00:00:00