当前位置： SCI文献检索 > BRITISH JOURNAL OF PHARMACOLOGY期刊下所有文献 > Further studies on the mode of action of psychotomimetic drugs: antagonism of the excitatory actions of 5-hydroxytryptamine by methylated derivatives of tryptamine.

Further studies on the mode of action of psychotomimetic drugs: antagonism of the excitatory actions of 5-hydroxytryptamine by methylated derivatives of tryptamine.

Abstract：

:1 The actions of 5-methoxytryptamine (5-MeOT), N,N-dimethyltryptamine (DMT), 5-hydroxy-N,N-dimethyltryptamine (bufotenine, 5-HODMT) and 5-methoxy-N,N-dimethyltryptamine (5-MeODMT), and their interactions with 5-hydroxytryptamine (5-HT), acetylcholine, (-)-noradrenaline, and glutamate were studied by microiontophoresis on single neurones in the brain stem of rats anaesthetized with urethane or decerebrate cats.2 Like D-lysergic acid diethylamide (LSD 25) the three psychotomimetic derivatives (DMT, 5-HODMT, 5-MeODMT) specifically antagonized 5-HT excitations of single neurones, but the non-psychotomimetic 5-MeOT had no antagonistic effects.3 In contrast to LSD 25, the psychotomimetic tryptamines only rarely antagonized glutamate effects, indicating that the excitatory 5-HT receptors and the glutamate receptors on the same neurones may be closely related spatially, but are separate.4 The methylated tryptamine derivatives were able to mimic the actions of 5-HT on neurones. The non-psychotomimetic 5-MeOT was most potent in this respect, while the other three derivatives which are psychotomimetic, were less active.5 The 5-HT mimicking actions of 5-MeOT were the same in rats pretreated with p-chlorophenylalanine or reserpine as in untreated rats. It therefore seems that the 5-HT mimicking actions are unlikely to be due to release of 5-HT, but are due to direct actions on 5-HT receptors.6 The evidence presented supports the hypothesis that LSD-like psychotomimetics act by an antagonism of 5-HT in the lower brain stem, and is not compatible with the suggestion that the psychotomimetic action of these drugs is related to 5-HT receptor stimulation.

journal_name

Br J Pharmacol

journal_title

British journal of pharmacology

authors

Bradley PB,Briggs I

doi

10.1111/j.1476-5381.1974.tb09609.x

subject

Has Abstract

pub_date

1974-03-01 00:00:00

pages

345-54

issue

3

eissn

0007-1188

issn

1476-5381

journal_volume

50

pub_type

杂志文章

相关文献

BRITISH JOURNAL OF PHARMACOLOGY文献大全
  • Comparative neuropharmacology of three psychostimulant cathinone derivatives: butylone, mephedrone and methylone.

    abstract：BACKGROUND AND PURPOSE:Here, we have compared the neurochemical profile of three new cathinones, butylone, mephedrone and methylone, in terms of their potential to inhibit plasmalemmal and vesicular monoamine transporters. Their interaction with 5-HT and dopamine receptors and their psychostimulant effect was also stud...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2012.01998.x

    authors： López-Arnau R,Martínez-Clemente J,Pubill D,Escubedo E,Camarasa J

    更新日期：2012-09-01 00:00:00

  • Modulation of histamine H(2) receptor signalling by G-protein-coupled receptor kinase 2 and 3.

    abstract：:To evaluate the role of G-protein-coupled receptor kinases (GRK) in the desensitization of the histamine H(2) receptor, the H(2) receptor was transiently cotransfected with GRK2, 3, 5 or 6 in COS-7 cells and the cyclic AMP levels in response to histamine were studied. Coexpression of the H(2) receptor with GRK2 and 3 ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0703676

    authors： Rodriguez-Pena MS,Timmerman H,Leurs R

    更新日期：2000-12-01 00:00:00

  • Characterization of the 5-HT4 receptor mediating tachycardia in piglet isolated right atrium.

    abstract：:1. In order to explore whether 5-HT4 receptor subtypes exist, we have characterized further the 5-HT4 receptor that mediates tachycardia in the piglet isolated right atrium. All experiments were carried out in the presence of propranolol (400 nM) and cocaine (6 microM). We used tryptamine derivatives, substituted benz...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1993.tb13916.x

    authors： Medhurst AD,Kaumann AJ

    更新日期：1993-11-01 00:00:00

  • Synergistic protective effect of caspase inhibitors and bFGF against brain injury induced by transient focal ischaemia.

    abstract：:We tested the hypothesis that combined use of trophic factors and caspase inhibitors increases brain resistance to ischaemia in mice. Intracerebroventricular administration of bFGF (>10 ng) 30 min after MCA occlusion decreased infarct size and neurological deficit in a dose-dependent manner following 2 h ischemia and ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0704075

    authors： Ma J,Qiu J,Hirt L,Dalkara T,Moskowitz MA

    更新日期：2001-06-01 00:00:00

  • The enhanced immunopharmacology of VIB4920, a novel Tn3 fusion protein and CD40L antagonist, and assessment of its safety profile in cynomolgus monkeys.

    abstract：BACKGROUND AND PURPOSE:Inhibition of the T- and B-cell interaction through the CD40/CD40 ligand (L) axis is a favourable approach for inflammatory disease treatment. Clinical studies of anti-CD40L molecules in autoimmune diseases have met challenges because of thromboembolic events and adverse haemostasis. VIB4920 (for...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.14897

    authors： Nicholson SM,Casey KA,Gunsior M,Drabic S,Iverson W,Cook H,Scott S,O'Day T,Karanth S,Dixit R,Ryan PC

    更新日期：2020-03-01 00:00:00

  • Effects of an intrathecally administered benzodiazepine receptor agonist, antagonist and inverse agonist on morphine-induced inhibition of a spinal nociceptive reflex.

    abstract：:1. The effects of an intrathecally administered benzodiazepine receptor (BZR) agonist (midazolam, up to 50 micrograms), antagonist (flumazenil, Ro 15-1788, 5 micrograms) and inverse agonist (Ro 19-4603, 15 micrograms) on nociception and on morphine-induced antinociception were studied in rats. 2. By themselves, none o...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1988.tb11486.x

    authors： Moreau JL,Pieri L

    更新日期：1988-04-01 00:00:00

  • The association of statins plus LDL receptor-targeted liposome-encapsulated doxorubicin increases in vitro drug delivery across blood-brain barrier cells.

    abstract：BACKGROUND AND PURPOSE:The passage of drugs across the blood-brain barrier (BBB) limits the efficacy of chemotherapy in brain tumours. For instance, the anticancer drug doxorubicin, which is effective against glioblastoma in vitro, has poor efficacy in vivo, because it is extruded by P-glycoprotein (Pgp/ABCB1), multidr...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2012.02103.x

    authors： Pinzón-Daza M,Garzón R,Couraud P,Romero Ia,Weksler B,Ghigo D,Bosia A,Riganti C

    更新日期：2012-12-01 00:00:00

  • Glucagon-like peptide 1 receptor stimulation as a means of neuroprotection.

    abstract：:Glucagon-like peptide 1 (GLP-1) is a relatively recently discovered molecule originating in the so-called L-cells of the intestine. The peptide has insulinotrophic properties and it is this characteristic that has predominantly been investigated. This has led to the use of the GLP-1-like peptide exendin-4 (EX-4), whic...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章,评审

    doi：10.1111/j.1476-5381.2009.00486.x

    authors： Harkavyi A,Whitton PS

    更新日期：2010-02-01 00:00:00

  • Effect of nitrovasodilators and inhibitors of nitric oxide synthase on ischaemic and reperfusion function of rat isolated hearts.

    abstract：:1. The functional role of the nitric oxide (NO)/guanosine 3':5'-cyclic monophosphate (cyclic GMP) pathway in experimental myocardial ischaemia and reperfusion was studied in rat isolated hearts. 2. Rat isolated hearts were perfused at constant pressure with Krebs-Henseleit buffer for 25 min (baseline), then made ischa...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0701694

    authors： du Toit EF,McCarthy J,Miyashiro J,Opie LH,Brunner F

    更新日期：1998-03-01 00:00:00

  • Chronic heart rate reduction by ivabradine prevents endothelial dysfunction in dyslipidaemic mice.

    abstract：BACKGROUND AND PURPOSE:High resting heart rate is a predictor for total and cardiovascular mortality independent of other risk factors in patients with coronary artery disease. We tested the hypothesis that a reduction of resting heart rate with the cardiac pacemaker I(f) current inhibitor ivabradine prevents the endot...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/bjp.2008.116

    authors： Drouin A,Gendron ME,Thorin E,Gillis MA,Mahlberg-Gaudin F,Tardif JC

    更新日期：2008-06-01 00:00:00

  • Differential classification of vascular smooth muscle and endothelial cell 5-HT receptors by use of tryptamine analogues.

    abstract：:In ring preparations of the rabbit external jugular vein contracted with the thromboxane-mimetic U-46619, submicromolar concentrations of 5-hydroxytryptamine (5-HT) and chemically related analogues produced relaxations that were dependent on the integrity of the vascular endothelium. The receptor mediating endothelium...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1987.tb10287.x

    authors： Leff P,Martin GR,Morse JM

    更新日期：1987-06-01 00:00:00

  • Contractile properties of the pig bladder mucosa in response to neurokinin A: a role for myofibroblasts?

    abstract：BACKGROUND AND PURPOSE:The bladder urothelium is now known to have active properties. Our aim was to investigate the contractile properties of the urinary mucosa in response to the tachykinin neurokinin A (NKA) and carbachol. EXPERIMENTAL APPROACH:Discrete concentration-response curves for carbachol and NKA were obtai...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/bjp.2008.29

    authors： Sadananda P,Chess-Williams R,Burcher E

    更新日期：2008-04-01 00:00:00

  • Enhancement of inflammatory mediator release by beta(2)-adrenoceptor agonists in airway epithelial cells is reversed by glucocorticoid action.

    abstract：BACKGROUND AND PURPOSE:Due to their potent bronchodilator properties, beta(2)-adrenoceptor agonists are a mainstay of therapy in asthma. However, the effects of beta(2)-adrenoceptor agonists on inflammation are less clear. Accordingly, we have investigated the effects of beta(2)-adrenoceptor agonists on inflammatory me...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2010.00708.x

    authors： Holden NS,Rider CF,Bell MJ,Velayudhan J,King EM,Kaur M,Salmon M,Giembycz MA,Newton R

    更新日期：2010-05-01 00:00:00

  • Prevention by dexrazoxane of down-regulation of ryanodine receptor gene expression in anthracycline cardiomyopathy in the rat.

    abstract：:Anthracyclines can cause cumulative dose-related cardiotoxicity characterized by changes in Ca(2+) metabolism, including dysfunction of the sacroplasmic reticulum (SR) and decreased expression of Ca(2+)-handling proteins, such as the ryanodine receptor (RyR2). In this study, we examined the effect of dexrazoxane (ICRF...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0703538

    authors： Burke BE,Gambliel H,Olson RD,Bauer FK,Cusack BJ

    更新日期：2000-09-01 00:00:00

  • Cardiac alpha 1-adrenoceptor densities in different mammalian species.

    abstract：:1. alpha 1-Adrenoceptor densities were studied in cardiac membrane preparations from several mammalian species including human failing hearts under identical experiment conditions; the alpha 1-adrenoceptor antagonist, [3H]-prazosin, was used as radioligand. End-stage heart failure (NYHA IV) in human hearts was due to ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1992.tb14484.x

    authors： Steinfath M,Chen YY,Lavický J,Magnussen O,Nose M,Rosswag S,Schmitz W,Scholz H

    更新日期：1992-09-01 00:00:00

  • A comparison of the facilitatory actions of 4-aminopyridine methiodide and 4-aminopyridine on neuromuscular transmission.

    abstract：:1 4-Aminopyridine methiodide (4-APMI), a quaternary analogue of aminopyridine (4-AP), was tested for neuromuscular facilitatory actions on the chick biventer cervicis and frog sartorius nerve-muscle preparations. 2 In the chick, 4-APMI (10(-4) to 10(-2) M) augmented indirectly elicited twitches and reversed tubocurari...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1979.tb17333.x

    authors： Horn AS,Lambert JJ,Marshall IG

    更新日期：1979-01-01 00:00:00

  • Show the data, don't conceal them.

    abstract：:Data presentation and statistical analysis in scientific writing are agreed to be in need of improvement, despite the profusion of advice and instruction. Recent evidence supports the need for better planning and analysis of animal experiments. This series of short articles aims to provide advice in small easily diges...

    journal_title：British journal of pharmacology

    pub_type： 社论

    doi：10.1111/j.1476-5381.2011.01251.x

    authors： Drummond GB,Vowler SL

    更新日期：2011-05-01 00:00:00

  • M2 TAM-associated STAT3/NF-κB signalling suppression as major target of immunomodulatory therapy with PLGA-based nanocarriers and anti-PD-L1 in breast cancer.

    abstract：BACKGROUND AND PURPOSE:Inflammation associated with the tumour microenvironment (TME) plays a critical role in the cancer development, and immunotherapeutic strategies that aim to modulate the immune response in cancer have been crucial. In this study, a Methotrexate-loaded (MTX) poly (lactic-co-glycolic acid)-based (P...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/bph.15373

    authors： Cavalcante RS,Ishikawa U,Silva ES,Silva Júnior AA,Araújo AA,Cruz LJ,Chan AB,Araújo Júnior RF

    更新日期：2021-01-12 00:00:00

  • Selective inhibition of arachidonate 5-lipoxygenase by novel acetohydroxamic acids: biochemical assessment in vitro and ex vivo.

    abstract：:1. The chemically novel acetohydroxamic acids, BW A4C, BW A137C and BW A797C, are potent inhibitors of the synthesis of leukotriene B4 (LTB4) from arachidonic acid by human leucocyte homogenates: the concentrations required for 50% inhibition (IC50) were 0.1 microM, 0.8 microM and 0.5 microM respectively. Inhibition w...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1988.tb11557.x

    authors： Tateson JE,Randall RW,Reynolds CH,Jackson WP,Bhattacherjee P,Salmon JA,Garland LG

    更新日期：1988-06-01 00:00:00

  • Cannabidiol improves brain and liver function in a fulminant hepatic failure-induced model of hepatic encephalopathy in mice.

    abstract：BACKGROUND AND PURPOSE:Hepatic encephalopathy is a neuropsychiatric disorder of complex pathogenesis caused by acute or chronic liver failure. We investigated the effects of cannabidiol, a non-psychoactive constituent of Cannabis sativa with anti-inflammatory properties that activates the 5-hydroxytryptamine receptor 5...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.2010.01179.x

    authors： Avraham Y,Grigoriadis N,Poutahidis T,Vorobiev L,Magen I,Ilan Y,Mechoulam R,Berry E

    更新日期：2011-04-01 00:00:00

  • Identification of a prostanoid FP receptor population producing endothelium-dependent vasorelaxation in the rabbit jugular vein.

    abstract：:1. Prostaglandin F2 alpha (PGF2 alpha) and its synthetic analogue, fluprostenol, potently relaxed the precontracted isolated jugular vein of the rabbit (RJuV). The vasorelaxant activity of PGF2 alpha and fluprostenol was dependent upon an intact vascular endothelium. Although removal of the vascular endothelium abolis...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1995.tb15960.x

    authors： Chen J,Champa-Rodriguez ML,Woodward DF

    更新日期：1995-12-01 00:00:00

  • Cardiotoxic effects of fenfluramine hydrochloride on isolated cardiac preparations and ventricular myocytes of guinea-pigs.

    abstract：:The cardiotoxic effects of fenfluramine hydrochloride on mechanical and electrical activity were studied in papillary muscles, Purkinje fibres, left atria and ventricular myocytes of guinea-pigs. Force of contraction (f(c)) was measured isometrically, action potentials and maximum rate of rise of the action potential ...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0703118

    authors： Rajamani S,Studenik C,Lemmens-Gruber R,Heistracher P

    更新日期：2000-03-01 00:00:00

  • Pharmacology of 5-hydroxytryptamine receptors in frog skin epithelium.

    abstract：:1. 5-Hydroxytryptamine (5-HT) stimulates active sodium transport and decreases the passive mucosal to serosal chloride permeability across frog skin. The relative importance of the different regions of the 5-HT molecule in the mediation of these responses has been studied using a range of structurally related compound...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1979.tb07867.x

    authors： Dalton T

    更新日期：1979-04-01 00:00:00

  • Pharmacological profile of PD 117302, a selective kappa-opioid agonist.

    abstract：:1 PD 117302, a new nonpeptide opioid compound shown in in vitro studies to be a selective kappa-opioid agonist, has been evaluated in vivo for antinociceptive activity and other effects characteristic of kappa-receptor activation. 2 Dose-related long lasting antinociception was produced by PD 117302 against a mechanic...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1987.tb11398.x

    authors： Leighton GE,Johnson MA,Meecham KG,Hill RG,Hughes J

    更新日期：1987-12-01 00:00:00

  • Baclofen and phaclofen modulate GABA release from slices of rat cerebral cortex and spinal cord but not from retina.

    abstract：:1. The effects of (-)-baclofen, muscimol and phaclofen on endogenous gamma-aminobutyric acid (GABA) release from rat cortical slices, spinal cord slices and entire retinas were studied. 2. The spontaneous resting release of GABA from the three tissues was 3 to 6 pmol mg-1 wet wt 10 min-1. Depolarization of cortical sl...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1989.tb16869.x

    authors： Neal MJ,Shah MA

    更新日期：1989-09-01 00:00:00

  • Effect of milacemide on extracellular and tissue concentrations of dopamine and 5-hydroxytryptamine in rat frontal cortex.

    abstract：:1. Milacemide is a glycine prodrug which is both an inhibitor and a substrate for monoamine oxidase-type B (MAO-B) and also an inhibitor of MAO-type A (MAO-A). Its effects on dopamine and 5-hydroxytryptamine (5-HT) metabolism in rat frontal cortex tissue and dialysate were evaluated. 2. Dialysate dopamine concentratio...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1992.tb14210.x

    authors： Semba J,Doheny M,Patsalos PN,Sarna G,Curzon G

    更新日期：1992-01-01 00:00:00

  • Antagonism by fenamates and like-acting drugs of bronchoconstriction induced by bradykinin or antigen in the guinea-pig.

    abstract：:1. Nine non-steroidal anti-inflammatory drugs were tested for antagonism of bradykinin-induced bronchoconstriction in guinea-pig lungs in vivo. Only one, benzydamine, was inactive.2. The descending order of potency of the active anti-inflammatory drugs was meclofenamate = Scha 306>Scha 87/2>indoxole>Mi85>indomethacin>...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1968.tb07952.x

    authors： Collier HO,James GW,Piper PJ

    更新日期：1968-09-01 00:00:00

  • The effects of (+)-amphetamine, alpha-methyltyrosine, and alpha-methylphenylalanine on the concentrations of m-tyramine and alpha-methyl-m-tyramine in rat striatum.

    abstract：:The concentration in rat striatum of the meta and para isomers of tyramine and alpha-methyltyramine, after the administration of (+)-amphetamine, alpha-methyl-p-tyrosine (AMPT) and alpha-methylphenylalanine (AMPA) has been determined using chemical ionization gas chromatography mass spectrometry (c.i.g.c.m.s.). Twenty...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1983.tb10035.x

    authors： Dougan DF,Duffield AM,Duffield PH,Wade DN

    更新日期：1983-10-01 00:00:00

  • Effects of endorphins on different parts of the gastrointestinal tract of rat and guinea-pig in vitro.

    abstract：:1 The spasmogenic and spasmolytic effects of beta-lipotropin (LPH) fragments and one analogue were investigated on different parts of the gastro-intestinal tract of guinea-pig and rat in vitro.2 Changes in muscle tone were observed in colon and rectum and to a lesser extent in jejunum and ileum of both species. Rat co...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1111/j.1476-5381.1980.tb10849.x

    authors： Nijkamp FP,Van Ree JM

    更新日期：1980-04-01 00:00:00

  • The expression of functionally-coupled B2-bradykinin receptors in human corneal epithelial cells and their pharmacological characterization with agonists and antagonists.

    abstract：:1. Bradykinin (BK) and Lys-BK are peptides which are released at high nanomolar concentrations into the tear-film of ocular allergic patients. We hypothesized that these peptides may activate specific receptors on the ocular surface, especially the corneal epithelium (CE) and thus the CE cells may represent a potentia...

    journal_title：British journal of pharmacology

    pub_type： 杂志文章

    doi：10.1038/sj.bjp.0701168

    authors： Wiernas TK,Griffin BW,Sharif NA

    更新日期：1997-06-01 00:00:00