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At least 865 records · Page 48Linked to original sources
PubMed1978

Effect of thyroxine on permeability of the neonatal rat lung to drugs.

The effect of thyroxine (1-2 microgram/g i.p. on days 1-4 after birth) on development of adult-type permeability characteristics in the lung was investigated in rats 6-18 days of age. In both treated and control rats, the lipid-soluble drug procaine amide was absorbed at similar rates in all age groups. In contrast, in thyroxine-treated animals, pulmonary absorption rates for the lipid-insoluble compounds mannitol and p-aminohippuric acid declined to adult levels at age 6-12 days, 6 days earlier than in controls. Thyroxine treatment thus accelerates development of adult permeability characteristics in the pulmonary epithelium.

Aminohippuric Acids↗
PubMed1987

Contribution of neurogenic and myogenic factors in the response of rat proximal colon to distension.

The response of the rat proximal colon to distension and drugs that interfere with intrinsic and extrinsic nerves was investigated in vivo (urethan anesthesia) and in vitro. Saline distension induced the appearance of a cyclic contractile activity that was slightly inhibited by atropine (ATRO) and enhanced by physostigmine. Hexamethonium increased the distension-induced motor activity. Topical tetrodotoxin (TTX), lidocaine, or procaine produced an increase in motility of the proximal colon. Isolated segments of the proximal colon exhibit a high-amplitude phasic contractile activity that was increased by stretching, transiently inhibited by ATRO, unaffected by hexamethonium, and increased by TTX. The effects of both ATRO and TTX were more evident at high- than low-resting tone. In the presence of ATRO plus guanethidine, field stimulation of the isolated rat proximal colon suppressed the spontaneous contractile activity of the preparations. These findings indicate that, in the proximal colon of urethan-anesthetized rats, a tonic discharge of intramural nonadrenergic noncholinergic neurons suppresses the inherent myogenic contractile activity of the smooth muscle cells. Extrinsic nervous supply plays a subsidiary role in maintaining colonic motility.

Animals↗
PubMed1982

[Differences in the blocking action of benzocaine and amino compounds on batrachotoxin-modified node of Ranvier sodium channels].

Voltage-clamp experiments on the frog Ranvier node have shown that batrachotoxin (BTX) decreases drastically the sensitivity of sodium channels to the blocking action of various tertiary (procaine, trimecaine, ajmalin, strychnine) and quaternary (QX-572, N-propylajmaline) amine drugs but does not affect noticeably sodium channels blockade produced by neutral benzocaine. The inhibition of BTX-modified sodium current by large concentrations of trimecaine (3.5 mM) is time- and voltage-dependent. Neither of the amines used proved to be able to cause frequency-dependent (cummulative) block of modified channels. Unblocking of these channels during washing of the node with Ringer solution proceeds much faster than that of normal channels. On the contrary, restoration of normal and modified currents blocked previously by benzocaine has the same time course. The relationships between "receptors" for BTX and various sodium channel blockers are discussed.

Amines↗
PubMed1989

Effect of cocaine and cocaine congeners on veratridine-induced depolarization in mouse cerebrocortical synaptoneurosomes.

Structure-activity relationships were determined for cocaine congeners in counteracting the depolarization induced by the action of veratridine on voltage-dependent sodium channels of synaptoneurosomes from mouse brain cortex, and their potency was compared to those determined previously on Na+ uptake and batrachotoxinin binding. Cocaine, norcocaine, (+)-pseudococaine, (-)-pseudococaine, (+)-neopseudococaine, benzoyltropine, benzoylpseudotropine, ecgonine methylester, atropine, WIN-35,428, WIN-35,140, WIN-35,065-3, WIN-35,004, and procaine were tested for their potency in inhibiting depolarization as measured by the distribution of the lypophilic cation [3H]triphenylmethylphosphonium across the membrane. All of the tested compounds inhibited the veratridine-induced depolarization in a competitive manner. The structure-activity relationships were similar to those for inhibition of 22Na+ uptake in mouse brain homogenates, and the potency of these local anesthetics in inhibiting veratridine-induced uptake of [3H]triphenylmethylphosphonium correlated well with their potency in inhibiting [3H]batrachotoxinin A 20-alpha-benzoate binding in mouse brain synaptosomes.

Anesthetics, Local↗
PubMed1984

Lipidosis-like alterations in cultured macrophages exposed to local anaesthetics.

In this ultrastructural study, the simple model of cultured rat peritoneal macrophages was used to examine whether local anaesthetics can induce lipidosis-like alterations. Exposure (24h) of macrophages to 1 X 10(-5) M dibucaine, or to 5 X 10(-5) M tetracaine, quinidine, and quinine, respectively, led to the occurrence of lamellated cytoplasmic inclusions in most cells. This is interpreted as indicating lipidosis. Type and degree of alterations were similar to those induced by the reference compound chlorphentermine (5 X 10(-5) M) for which lipidosis has previously been shown by biochemical methods. Tocainide (5 X 10(-5) M) caused weak alterations only; procaine (5 X 10(-5) M) was without effect. The differential potencies presently observed are paralleled by differential affinities of the local anaesthetics towards polar lipids as determined by other authors. The present results support the hypothesis that the lipidosis-inducing potency inherent to an amphiphilic cationic drug can be tentatively predicted on the basis of its affinity to polar lipids, although it may be obscured by secondary factors when the drug is administered to intact organisms. The present communication emphasizes the advantage of cell cultures over animal experiments for studying the structure-response relationships underlying drug-induced lipidosis, and to reliably ascertain that a given drug has only low lipidosis-inducing potency or none at all as found for tocainide and procaine, respectively.

Anesthetics, Local↗
PubMed1976

Bimodal action of glycine on frog spinal motoneurones.

In the presence of procaine the changes in electrical potential caused by glycine in the ventral root of the isolated hemisected spinal cord of the frog have been shown to be compounded of both hyperpolarizing and depolarizing responses to the amino acid. From a comparison of the effects of changes in the perfusion medium on the potentials produced by glycine, beta-alanine and L-glutamate in the presence and absence of strychnine, it was concluded that glycine acts on a similar receptor to beta-alanine and causes a hyperpolarizing response which is blocked by strychnine. However, glycine has an additional, depolarizing, action which is usually the major effect and masks the hyperpolarizing response. The depolarizations produced by L-glutamate and glycine could be differentiated by their different ionic dependencies. The glycine depolarization was selectively decreased by a lowered sodium ion concentration in the medium while L-glutamate depolarizations were selectively enhanced by lowered potassium ion concentration.

Alanine↗
PubMed1976

Pharmacological studies on a new 1-benzoyloxy-alkylaminocycloalkane derivative (YAU-17) with special reference to its mucosa anesthetic activity.

A new compound, dl-cis-1-benzoyloxy-2-dimethylamino-1,2,3,4-tetrahydronaphthalane (YAU-17) was found to produce sciatic nerve block, corneal and intradermal anesthesia in guinea-pigs, which markedly exceeded the effect of procaine and lidocaine. YAU-17, when given orally to mice, was much less toxic than any other drugs tested, though YAU-17 showed a considerably high acute toxicity by i.v. route. Oral administration of YAU-17 was effective in antagonizing the emetic response of dogs to intragastric phenylalanine isopropyl ester, but produced no distinct inhibition against vomiting elicited by oral copper sulfate. Furthermore, it possessed a spasmolytic activity which was comparable to that of papaverine, and showed an effect of suppressing the mucosal intrinsic reflex in the dog intestine. These pharmacological properties of YAU-17 were qualitatively similar to those of oxetacaine which was used as one of the reference compounds.

2-Naphthylamine↗
PubMed1995

Polymorphic metabolism of flestolol and other ester containing compounds by a carboxylesterase in New Zealand white rabbit blood and cornea.

Flestolol, N(1,1-dimethyl-2-ureidocthyl)-2-hydroxy-3-(o-fluorobenzoyloxy++ +) propylamine, (F), is an ester containing an ultra short-acting beta blocker intended for the treatment of myocardial dysfunctions. In vitro incubation of F, procaine, chloroprocaine, and atropine with blood from different New Zealand White (NZW) rabbits resulted in a bimodal distribution (70% fast, 30% slow) of ester hydrolysis rates. Using F as a model substrate, bimodal hydrolysis rates were also observed in NZW rabbit cornea but not aqueous humor, iris-ciliary body complex and ocular tissues of pigmented rabbits. In addition, the bimodal distribution of esterase activity was not observed in blood from rats, dogs, and humans. Incubation of esters at various positions of the phenoxypropanolamine nucleus of beta blockers with NZW rabbit blood indicated structural specificity of the carboxylesterase in terms of unimodal or biomodal distribution of activity. These results strongly suggest that the carboxylesterase in NZW rabbit blood that hydrolyzes F and similar compounds is atropine esterase as described in the literature.

Adrenergic beta-Antagonists↗