Abstract：
:Five different muscarinic receptor subtypes can be distinguished by the differences in their amino acid sequence, the coupled signal transduction system, pharmacological binding properties and activation of ionic fluxes. The present study served to characterize the binding profile of muscarinic receptors in human colon carcinoma cells (HT-29) using selective muscarinic antagonists. The affinities of the compounds were compared with their potency to inhibit cholinergically-activated phosphoinositide metabolism. Pirenzepine displaced [3H]N-methyl-scopolamine binding and inhibited inositolphosphate (IP) release with potencies typical of those of non-M1 receptors. The M3 subtype-selective antagonists sila-hexocyclium and hexahydro-sila-difenidol had high affinity to the muscarinic receptors in HT-29 cells (KD = 3.1 nM and 27 nM, respectively) and inhibited IP release at nanomolar concentrations. The M2 receptor antagonists, AF-DX 116 and methoctramine, had low antimuscarinic potencies. Our results demonstrate that HT-29 human colon carcinoma cells contain an apparently pure population of M3 receptors. These cells could serve as a model system for further investigations concerning regulatory and signal transduction mechanisms associated with glandular muscarinic M3 receptors.
journal_name
Eur J Pharmacoljournal_title
European journal of pharmacologyauthors
Kopp R,Lambrecht G,Mutschler E,Moser U,Tacke R,Pfeiffer Adoi
10.1016/0922-4106(89)90021-7subject
Has Abstractpub_date
1989-10-17 00:00:00pages
397-405issue
4-5eissn
0014-2999issn
1879-0712journal_volume
172pub_type
杂志文章abstract：:The cellular mechanisms underlying the inhibitory effects of phenylephrine on dihydropyridine-sensitive, voltage-dependent Ca2+ currents recorded from single smooth muscle cells dissociated from the rat anococcygeus muscle were examined. Phenylephrine (0.1-30 microM) produced a concentration-dependent inhibition of th...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(95)90049-7
更新日期：1995-02-15 00:00:00
abstract：:Induction of mRNA or protein for immediate-early genes, such as c-fos, is used to identify brain areas, specific cell types, and neuronal circuits that become activated in response to various stimuli including psychoactive drugs. The objective of the present study was to identify the cell types in the prefrontal corte...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.12.031
更新日期：2008-03-31 00:00:00
abstract：:Calcitonin gene-related peptide (CGRP) released from vasodilator nerves is implicated in the gastroprotective action of capsaicin. This experimental paradigm was used to prove the effectiveness of a monoclonal anti-CGRP antibody. The experiments were performed in anaesthetized rats in which intragastric capsaicin (0.5...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90645-x
更新日期：1993-11-30 00:00:00
abstract：:In rat neocortical slices activation of glutamate metabotropic receptors with glutamate, quisqualate and 1S,3R-ACPD caused a spike-evoked afterdepolarization which replaced the normal afterhyperpolarization. In some neocortical neurons the afterdepolarization reached action potential threshold causing prolonged self-s...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0922-4106(92)90073-5
更新日期：1992-07-01 00:00:00
abstract：:Earlier studies demonstrated that cytokine production is under the tonic control of noradrenaline. As the level and/or the duration of noradrenaline action is regulated by the noradrenaline transporter (NET), which is also a target of antidepressant treatment, we studied its role in the regulation of the cytokine resp...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(03)01721-7
更新日期：2003-05-23 00:00:00
abstract：:Opiates impair neutrophil-mediated host defense, but the involvement of kappa-opioid receptors in this action has not been defined. The selective kappa-opioid receptor agonist [trans-(+)3,4-dichloro-N-methyl-N[2-(1-pyrrolidinyl)-cyclohexyl]benzeneacetamide methanesulfonate inhibited macrophage inflammatory protein-2-i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(01)00727-0
更新日期：2001-03-02 00:00:00
abstract：:We have investigated the possible mechanisms underlying the antihyperglycaemic effect of the imidazoline derivative S-22068. In vitro, in the presence of 5 mmol/l glucose, S-22068 (100 micromol/l) induced a significant and sustained increase in insulin secretion from isolated, perifused, rat islets and a marked sensit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(99)00395-7
更新日期：1999-07-14 00:00:00
abstract：:Migraine is a common painful neurovascular disorder usually associated with several symptoms, such as photophobia, phonophobia, nausea, vomiting and inflammation, and involves immune cells. Mast cells (MCs) are immune cells derived from hematopoietic pluripotent stem cells which migrate and mature close to epithelial,...
journal_title：European journal of pharmacology
pub_type： 杂志文章,评审
doi：10.1016/j.ejphar.2018.12.004
更新日期：2019-02-05 00:00:00
abstract：:The effect of colchicine on jejunal adenylate cyclase activity, prostaglandin E2 (PGE2) and cAMP contents, the enzyme and mediators involved in intestinal fluid secretion was tested in rats. Four h after the intraperitoneal injection of colchicine (0.5 mg/100 g body wt.) mucosal PGE2 content, adenylate cyclase activit...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(80)90503-8
更新日期：1980-10-17 00:00:00
abstract：:The decrease in mesenteric blood flow produced by dopamine administered intra-arterially in the anaesthetised dog was investigated by means of drugs selective for alpha 1- and alpha 2-adrenoceptors. The selective alpha 1-adrenoceptor agonist phenylephrine (0.3-100 microgram) given by intra-arterial injection (i.a.) in...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90352-1
更新日期：1982-07-30 00:00:00
abstract：:A significant stimulatory action of PGE1 on adenylate cyclase of the particulate membrane preparation of rat heart was observed at 1 X 10(-4) M. PGE1 caused a positive inotropic effect on isolated spontaneously beating rat atria 1 X (10(-5) M, and an increase in atrial cyclic AMP level at 1 X 10(-6) M. PGE2 stimulate...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(78)90025-0
更新日期：1978-11-01 00:00:00
abstract：:The breakdown of inositol phospholipid (PI) stimulated by hippocampal noradrenaline in rat miniprisms in vitro was used as an index of alpha 1-adrenoceptor function after selective noradrenergic denervation. Selective denervation was produced by microinjections of 6-hydroxydopamine (6-OHDA) into either the dorsal nora...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(86)90715-6
更新日期：1986-04-29 00:00:00
abstract：:A comparison was made of the effects of 5-MeoDMT or LSD on serotonergic unit activity in the dorsal raphe nucleus (DRN) and nucleus raphe pallidus (NRP) of freely moving cats. NRP neurons were substantially less responsive than DRN neurons to both drugs. NRP neurons were unresponsive to behaviorally effective low dose...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(82)90360-0
更新日期：1982-07-30 00:00:00
abstract：:In addition to its well-known interaction with ionotropic and metabotropic receptors, glutamate may, at high concentrations, interfere with a cystine-glutamate antiport designated as Xc- and lead to a significant decrease in cystine uptake and intracellular glutathione level. These effects, in turn, may induce death i...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/s0014-2999(97)00155-6
更新日期：1997-05-12 00:00:00
abstract：:Single myocytes isolated from the guinea-pig ventricle were used under voltage-clamp conditions to study the activity of a newly developed drug, R56865, a benzothiazolamine derivative, against digitalis toxicity. Multicellular Purkinje preparations were used in some experiments. The drug blocked the transient inward c...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(91)90407-h
更新日期：1991-04-10 00:00:00
abstract：:Acute administration of delta 9-tetrahydrocannabinol (THC) (50 mg/kg) at puberty (35-40 days) significantly (P less than 0.05) reduced Ca2+ ATPase activity in hypothalamic plasma membranes but increased, although not significantly, enzyme activity in hypothalamic tissue obtained from adult mice. In contrast, testicula...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(87)90186-5
更新日期：1987-05-07 00:00:00
abstract：:We have investigated the effects of antagonists at functional prejunctional alpha 2-adrenoceptors of rat was deferens and rat submandibular gland and compared potencies with affinities for the alpha 2A-, alpha 2B- and putative alpha 2D-ligand binding sites of human platelet, rat kidney, and rat submandibular gland, re...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90297-h
更新日期：1992-08-25 00:00:00
abstract：:Statins are some of the most widely used drugs worldwide, but one of their major side effects is myotoxicity. Using mouse myoblast (C2C12) and human alveolar rhabdomyosarcoma cell lines (RH30) in both 2-dimensional (2D) and 3-dimensional (3D) cell culture, we investigated the mechanisms of simvastatin's myotoxicity. W...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2019.172616
更新日期：2019-11-05 00:00:00
abstract：:The highly toxic monomer 12-deoxyphorbol 13-palmitate (G) was extracted from the roots of Euphorbia fischeriana. Our experimental data confirmed studies showing that 12-deoxyphorbol 13-palmitate had certain antitumor activities. The MTT method, soft agar experiments, and nude mouse tumor experiments proved that 12-deo...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.11.015
更新日期：2013-01-30 00:00:00
abstract：:In cardiac muscle cells both T-and L-type Ca(2+) channels (TTCCs and LTCCs, respectively) are expressed, and the latter are relevant to a process known as excitation-contraction coupling (ECC). Evidence obtained from docking studies suggests that isoindolines derived from α-amino acids bind to the LTCC CaV1.2. In the ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2016.04.027
更新日期：2016-06-15 00:00:00
abstract：:The effect of local administration of big endothelin-1 (1-38, big ET-1) has been investigated on blood flow in the skin of anaesthetised rats, measured by 133Xe clearance. The local effects of big ET-1 and big endothelin-3 (1-41, big ET-3) have also been determined on microvessel diameter by intravital microscopy of t...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(93)90056-n
更新日期：1993-03-23 00:00:00
abstract：:The effect of selective D1 receptor agonists on acetylcholine (ACh) release in the striatum was investigated using in vivo microdialysis. Administration of the reactive enantiomer, (+)-SKF 38393 (2, 10 mg/kg s.c.), doses which elevate grooming and sniffing behaviour, increased ACh release by 40 and 75%, respectively. ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(90)90456-g
更新日期：1990-09-21 00:00:00
abstract：:Although the gastrointestinal tract is a rich source of melatonin and possesses numerous melatonin-binding sites, the role of melatonin in this tissue has not yet been fully elucidated. In this work we focused on the role of melatonin in the modulation of ion transport in rat distal colon. Whereas melatonin had no eff...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2007.11.031
更新日期：2008-02-26 00:00:00
abstract：:Horizontal motor activity, rearing and head dipping were recorded automatically in rats placed on a holeboard and taken as indices of locomotion and exploration. Other behaviours were assessed visually using a video camera. SKF 38393, 15-30 mg/kg (D-1 agonist), suppressed all three behavioural measures more effectivel...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(85)90014-7
更新日期：1985-11-19 00:00:00
abstract：:Previous functional studies with the rat jugular vein have shown alpha-adrenergically mediated contraction was minimal to nonexistent, yet this tissue relaxed in response to norepinephrine via beta 1 and to isoproterenol via beta 2-receptor activation. Unlike the rat jugular vein, the rat aorta markedly contracted to ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90182-4
更新日期：1992-08-06 00:00:00
abstract：:The origin of the thrombocytopenia and leucopenia induced by protamine-heparin complexes is unknown. We studied the biochemical and cellular effects of protamine (6 mg x kg-1, i.v.) injected after heparin (5 mg x kg-1, i.v.) in New Zealand rabbits. After protamine injection (0.5 min) increases in blood platelet-activa...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(96)00069-6
更新日期：1996-04-29 00:00:00
abstract：:In our previous study, it was found that linoleoyl ethanolamide (LE) is present in sake lees, which are produced as a byproduct during the making of Japanese sake. LE is a fatty acid ethanolamide, which have been demonstrated to exert a variety of biological functions, and in this study, the anti-inflammatory effects ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/j.ejphar.2012.11.030
更新日期：2013-01-15 00:00:00
abstract：:Oral pretreatment with E3330, a novel quinone derivative, attenuated liver injury induced with tumor necrosis factor-alpha in galactosamine-sensitized mice. Tumor necrosis factor-alpha is known to induce inflammatory mediators such as leukotrienes and prostanoids. An in vitro study showed that E3330 inhibited the gene...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(92)90286-d
更新日期：1992-12-08 00:00:00
abstract：:In conscious rats, intracerebroventricular (i.c.v.) treatment with the GABA agonist muscimol (1-100 ng) suppressed the pressor responses to ANG II (100 ng i.c.v.) in a dose-dependent and reversible fashion. Treatment i.c.v. with GABA (1-500 micrograms) produced a similar but shorter inhibition. Inhibition of endogenou...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(83)90207-8
更新日期：1983-05-20 00:00:00
abstract：:Neuromedin K, a decapeptide isolated from porcine spinal cord and suggested to have tachykinin-like activity in vitro, produced reciprocal hind-limb scratching when injected intrathecally to mice. Neuromedin K was 20-60 times less potent in producing scratching (on a molar basis) than substance P, kassinin, eledoisin ...
journal_title：European journal of pharmacology
pub_type： 杂志文章
doi：10.1016/0014-2999(84)90499-0
更新日期：1984-08-17 00:00:00
