(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.
Azonic
Definition:
(a.) Confined to no zone or region; not local.
Example Sentences:
(1) A marked analgesic effect was found after application of morphine hydrochloride patch containing Azone and N-methyl-2-pyrrolidone.
(2) During the early part of the experiments, when the sink condition was maintained, FAH was the most effective for hairless mouse skin, whereas Azone showed the highest effect in the rat skin.
(3) Azone doubled the amount of PFA in the skin, more than tripled the amount permeated across the skin, and increased the flux fourfold.
(4) The addition of Azone (3%) or lauric acid (BH: lauric acid molar ratio, 1:1) considerably increased BH penetration to a relatively large penetration rate.
(5) In order to develop the transdermal formulations of morphine hydrochloride with high skin permeation rate and prolonged action, several gels and patches containing potent penetration enhancer, laurocapram (Azone), were prepared.
(6) The results indicate that Azone may be capable of forming ion pairs with anionic drugs.
(7) The efficacy of 5 and 10% Azone applied topically was evaluated during the treatment of HSV-1 cutaneous infections in guinea pigs.
(8) The performance of Tween 80, Tween 60, oleic acid, oleyl alcohol and Azone as enhancers of clonazepam permeation from a Carbopol hydrogel through a cellulose nitrate membrane was investigated.
(9) At the same time, plasma concentrations were maintained at a high level for more than 7 h. The increase in bioavailability is presumed to be caused by an enhancement in absorption and prolongation of the time DA is retained in the nasal cavity due to Azone and HPC, respectively.
(10) Azone and NMP showed maximum efficacy at 0.1% and 12.0% concentration, respectively.
(11) 0.5 ml solutions of different pH (3, 4, 5, 6, 7.5) or of pH 7.5 in combination with sorption promoters (sodium taurocholate, dextran sulfate, linoleic acid, TranscutolR, LabrafilR M 1944 CS, urea and AzoneR) were administered for 0.5 h to anesthetized dogs.
(12) The tests were conducted with 2',3'-di-O-acetyl-ara-A (4) and 5'-O-valeryl-ara-A (3) topically applied with and without 15% 1-dodecylazacycloheptan-2-one (2) (Azone), a percutaneous penetration enhancer.
(13) From these results, it was predicted that the topical formulations of morphine hydrochloride containing Azone and N-methyl-2-pyrrolidone might be useful for the relief of severe chronic pain in patients.
(14) First, the effect of Azone on the skin components was compared with that of other penetration enhancers.
(15) Two cleavage stage embryos, two blastocyts surrounded by zona pellucida, and two azonal ('hatched') blastocysts were recovered from uteri of rhesus monkeys and examined with the electron microscope.
(16) Both the in vitro permeation and the in vivo absorption of propranolol across the cheek pouch were enhanced by the incorporation of Azone to the film-dosage form.
(17) In addition, ethanol increased the amount of free sulfhydryl (SH) group of keratin in the stratum corneum, whereas Azone did not directly affect the stratum corneum protein.
(18) Azone increased percutaneous penetration of HpD in human skin in vitro.
(19) In order to clarify the mechanism of action of laurocapram (Azone) on the skin permeation of drugs, the following experiments were done.
(20) In contrast, the enhancing effect of Azone on the pretreated skin was similar to that of Azone on the in vitro non-treated skin.