(1) The hypothesis that opiate agonism requires an N substituent in the axial position does not appear to be consistent with the increased potency of beta isomers in which axial N substituents are thermodynamically more unstable.
(2) Under conditions of 5-HT1-like, 5-HT2 and 5-HT3 receptor blockade, the following rank order of agonism was observed: 5-HT > 5-methoxytryptamine = renzapride > (S)-zacopride > (R,S-zacopride > 5-carboxamidotryptamine > BRL 24682 > (R-zacopride > metoclopramide > 2-methyl-5-HT > sulpiride.
(3) At the agonal stage, the isoproterenol dose-response curve was shifted significantly to the right in myocardial membranes from endotoxic rats, but there was no significant decrease in maximum stimulated activity.
(4) Agonal state effects the stability of brain compounds and causes brain hypoxia.
(5) However, further studies showed compounds which exhibited either partial agonism in the RFA and competitive antagonism of 5-HT in the RA, or antagonism of 5-HT in both arteries with different affinities.
(6) Catecholamines were detectable in the major neurons, in small intensely fluorescent cells, and in adrenergic fibers with varicosities at levels that varied with the patient's age, cause of death, duration of the agonal period, the treatment administered, and the time when the material had been taken after death.
(7) Certain derivatives of the antagonists naloxone and naltrexone showed partial agonism.
(8) Except for desGly(NH2)AVP, which is a weak V2 agonist, the remaining desGly and desGly(NH2) analogues of 1-3 exhibit substantial V2 agonism and are thus highly selective V2 agonists.
(9) But bureaucratic dysfunction means less than half have been given out – as shown by two state department charts – and only at the end of agonizingly long waiting periods .
(10) The results failed to support the female agonism hypothesis and indicate a need for more detailed studies of intermale social dynamics.
(11) In the inferior parietal cortex, agonal status confounded this comparison.
(12) Dilevalol is a novel antihypertensive agent combining vasodilation due to selective beta 2-adrenergic receptor agonism with nonspecific beta antagonism.
(13) The results indicate that alpha 2-adrenergic agonism with clonidine inhibits the bronchoconstriction induced by histamine.
(14) We have found no evidence of a physiologically relevant effect of serotonin agonism on osmoregulated vasopressin release, or on the ability of normal man to excrete a water load.
(15) The partial agonism of N alpha-guanylhistamine is related to the ability of the drug to bind with the receptor in two different modes with similar affinity.
(16) In contrast U50,488H produced biphasic curves characterized by a higher potency phase of agonism that was susceptible to antagonism by 16-methylcyprenorphine (RX8008M) and a lower potency phase that was apparently non-opioid in nature.
(17) As this profile of activity is not shared by the shorter-acting compound, salbutamol, it would seem that anti-inflammatory activity is associated with beta-adrenoceptor agonism of long duration.
(18) To clarify the regulation of duodenal motility, the aim of the present study was to investigate the effects of alpha-adrenoceptor agonism and blockade and of galanin on duodenal motility.
(19) Agonist-independent pA2 estimates for ICS 205-930 (6.3-6.6) suggest a single site of agonism.
(20) In addition, analyses of beta-adrenoceptor agonism and antagonism, using selective (beta 1: T-1583, beta 2: procaterol) and non-selective (isoproterenol) agonists as well as selective (beta 1: atenolol, beta 2: ICI 118,551) and non-selective (propranolol) antagonists, confirmed that beta-adrenoceptors in the canine facial vein are not homogeneous, with the beta 1-subtype predominating over the beta 2-subtype, and that the canine saphenous vein has a homogeneous population of the beta 2-subtype, as reported in the other species.
Agonist
Definition:
(n.) One who contends for the prize in public games.
Example Sentences:
(1) alpha 1-Adrenergic agonists, phenylephrine and norfenefrine, did not affect the synthesis.
(2) Data obtained with fenoldopam were corroborated with use of SK&F 38393, another dopamine D1-receptor agonist.
(3) The GABA receptor agonist progabide reduced VCMs and locomotor activity.
(4) This novel mechanism of receptor regulation, named transmodulation, should be distinguished from the reduction in total receptor number caused by the homologous ligand (downregulation) and from the change in affinity produced by the binding of agonists or antagonists to the same receptor site.
(5) Exposure to nanomolar concentrations of saralasin, an Ang II agonist, attenuated the passage of the fluorophores across the monolayers by 50-75%.
(6) The effects of low doses of dihydropyridine (DHP) calcium channel antagonists nimodipine, nifedipine, (-)-R-202-791, and amlodipine, the DHP calcium channel agonist BAY K 8644 were investigated on clonic convulsions to pentylenetetrazole (PTZ) in mice.
(7) The binding to DNA-cellulose of heat-activated [3H]RU486-receptor complexes was slightly decreased (37%) when compared with that of the agonist [3H]R5020-receptor complexes (47%).
(8) These later results suggest that dopamine agonists increase sensorimotor reactivity measured with acoustic startle by acting on sensory rather than motor parts of the reflex arc.
(9) Only methoxyindole acetic acid was detectable after incubation of unstimulated and alpha-adrenergic-agonist-treated pineal glands.
(10) It inhibits platelet and vascular smooth muscle activation by cGMP-dependent attenuation of the agonist-induced rise of intracellular free Ca2+.
(11) The elimination half-life of most beta-agonists is relatively short, and pharmacokinetics are independent of dose and duration of treatment.
(12) Substance P (SP), a relatively non-selective tachykinin receptor agonist, and Septide and Senktide, highly selective NK-1 and NK-3 tachykinin receptor agonists, respectively, were injected intradermally in rats.
(13) Responses of control tissues to an alpha agonist (norepinephrine) were increased at lower temperatures and responses to a beta agonist (isoprenaline) were increased at higher temperatures.
(14) The inhibition of all three agonist responses by 1.1 mM calcium was competitive.
(15) The alpha 2 agonist, clonidine, produced a larger dose-related increase in food intake in lean rats than in the fatty rats.
(16) This stimulation is mediated by one receptor with an apparent affinity of 3.3 X 10(-6) M. The hydroxyl group in the para position on phenylethanolamine was absolutely necessary to obtain an agonist whereas the meta hydroxyl group or the presence of a catechol almost suppressed the activity.
(17) The alpha 2-adrenoceptor agonist clonidine is most potent for stimulating Isc.
(18) Moreover, the ribosylation inhibitors converted the glucocorticoid antagonist RU-486 into a potent agonist for cytolysis of L1210 cells.
(19) We have characterized the effects of adenosine, the A1-receptor agonist N6-(L-2-phenylisopropyl)-adenosine (PIA) and the A2-receptor agonist 5'-(N-ethyl)-carboxamido-adenosine (NECA), in isolated human pulmonary vessels.
(20) Long-term treatment with agents that stimulate the beta-receptor (prenalterol and pirbuterol) has not proved to be useful in the treatment of chronic heart failure; moreover, prolonged treatment with beta-agonists (dobutamine and pirbuterol) may adversely affect survival.