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At least 937 records · Page 52Linked to original sources
PubMed1966

The inhibitory innervation of the taenia of the guinea-pig caecum.

1. The inhibitory innervation of the taenia of the guinea-pig caecum has been studied, after blocking the responses to stimulation of excitatory cholinergic nerves with atropine.2. Stimulation of the perivascular nerves supplying the taenia caused relaxations. These nerves had properties which were typical of sympathetic post-ganglionic adrenergic nerves. The relaxations caused by stimulation were maximal at frequencies of stimulation above 30 pulses/sec and they were abolished by bretylium, guanethidine and 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP).3. The taenia is also innervated by intramural inhibitory nerves with their cell bodies in Auerbach's plexus. These nerves can be excited by electrical stimulation of the taenia or by the application of ganglion-stimulating drugs.4. The intramural inhibitory nerves have different properties from sympathetic adrenergic nerves. Relaxations in response to stimulation were maximal with frequencies of stimulation of about 5 pulses/sec and they were not blocked by bretylium, guanethidine or DMPP.5. Preganglionic cholinergic fibres in the caecal wall make synaptic connexions with the intramural inhibitory neurones.6. The role of the intramural inhibitory neurones in intestinal activity and their possible connexions with the central nervous system have been discussed.

Anesthetics, Local↗
PubMed1975

Analgesic activity of the epimeric tropane analogs of meperidine. A physical and pharmacological study.

Condensation of cis-N-benzyl-2,5-bis(chloromethyl)pyrrolidine (6) and phenylacetonitrile afforded a mixture of epimers 7 and 8. Compound 8 was readily converted to the meperidine analog 1 prepared earlier by Bell and Archer. Compound 7 was converted to a new tropane analog of meperidine, compound 3. The ED50 of 1 and 3 in the D'Amour-Smith "tail flick" test for narcotic type analgesia, which differs by a factor of only 3 or 4 potency, supports the accumulated data that suggest that the analgesic activity of the meperidine type is not very sensitive to the conformation of the phenyl group in 4-phenylpiperidines. A proton and 13C magnetic resonance spectral comparison of 1 and 3, as well as a reevaluation of the conformational requirements of 17-19, leads to the conclusion that the differences in conformation of 1,3,17, and 18 are due to the varying degrees of flattening of piperidine ring. The 1H NMR and 13C NMR data are not consistent with the boat conformation suggested earlier for compound 17.

Analgesics↗
PubMed1973

A study of compounds which initiate and block nerve impulses in the perfused rabbit liver.

1. A technique for the perfusion of the rabbit liver with Krebs solution is described: the hepatic nerves were monitored for centripetal action potentials. Spontaneous afferent activity, and a good response to stimulating agents persisted for 7 h or longer.2. Action potentials were elicited by injections or infusions of acetylcholine, 5-hydroxytryptamine, bradykinin, phenyldiguanide, adrenaline and various other compounds. From comparison with experiments carried out in vivo by other authors, it would appear that most of the nerves stimulated were afferent.3. Inhibition of action potentials, either those occurring spontaneously or those elicited by injections, was produced by aspirin, paracetamol, mepyramine, chlorpheniramine, procaine and lignocaine but not by morphine or atropine. Pentolinium produced some inhibition, as did hexamethonium in concentrations of about 7.5 mug/ml.4. Three methods for using the preparation for the assessment of local anaesthetic action are described.5. Lobeline, potassium cyanide and 2,4-dinitrophenol stimulated nerve bundles which were not stimulated by anoxia or hypoxia.

Acetylcholine↗
PubMed1976

Investigations to characterize a new anti-arrhythmic drug, ORG 6001 including a simple test for calcium antagonism.

1 The compound Org 6001 (3alpha-amino-2beta-hydroxy-5alpha-androstan-17-one hydrochloride) was found in recent experiments to exhibit anti-arrhythmic activity. Evidence is presented in this paper concerning its mode of action. 2 Org 6001 was 1.8 times more potent than procaine as a local anaesthetic on desheathed frog nerve. 3 Org 6001 had no effect on the resting potential of isolated cardiac muscle of rabbit, but greatly reduced the maximum rate of depolarization tion (MRD). The action potential duration TAPD) WAS MARGINALLY PROLONGED IN ATRIAL AND VENTRICULAR MUSCLE. 4 Org 6001 preferentially shortened APD in that part of the Purkinje system in which APD is normally longer than elsewhere, so that APD

17-Ketosteroids↗
PubMed1995

Potentiometric, enantioselective sensors for alkyl and aryl ammonium ions of pharmaceutical significance, based on lipophilic cyclodextrins.

Lipophilic alpha, beta and gamma cyclodextrins (CDs) have been systematically analysed in order to establish their selective binding to onium ions. They have been identified as excellent ionophores for a range of ions of vital importance in clinical, pharmaceutical and forensic analysis. From the results obtained we found the following. A peroctylated cyclodextrin provides a size-selective cavity for the binding and detection of onium ions. Potentiometric alpha, beta and gamma cyclodextrin-based electrodes selectively sense NH4+, NMe4+ and NEt4+ ions respectively. These experiments were performed in order to enable us to understand the nature of analyte recognition by the lipophilic cyclodextrins. Peroctylated alpha CD is a suitable ionophore for dopamine hydrochloride, -log[C] = 5.4, -log K = 2.0 (in serum level of Na+, K+, Ca2+) whereas peroctylated and 2,6 didodecyl beta CD sense acetylcholine chloride, -log[C] = 5.0, -log K = 4.2 (in serum level of Na+, K+, Ca2+) and creatinine hydrochloride, -log K = 2.7 (in serum level of Na+, K+, Ca2+), respectively. The 2,6 didodecyl beta CD responds to more bulky aryl ammonium ions such as the anaesthetics procaine, prilocaine and lignocaine hydrochlorides, -log K = 4.2 (in serum level of Na+, K+, Ca2+). Partially octylated alpha CD has been identified as an enantioselective sensor for ephedrine hydrochloride, -log K = 4.5 (in serum level of Na+, K+, Ca2+), -log Kpot+/- = 2.6, and related compounds such as amphetamine hydrochloride. The 2,6 didodecyl beta CD is enantioselective for propranalol hydrochloride, -log K = 4.2 (in serum level of Na+, K+, Ca2+), -log Kpot+/- = 2.7. Complexation has also been studied by electrospray mass spectrometry (ESMS).

Acetylcholine↗
PubMed1989

A comparison of the actions of 4-aminopyridine, caffeine and quinine on the toad isolated rectus abdominis muscle.

1. 4-Aminopyridine (4-AP)-induced contractures have been compared with those evoked by caffeine and quinine on the toad rectus abdominis muscle. 2. All three compounds produced slowly-developing sustained contractures. The time to half maximal contracture and relaxation was significantly longer for 4-AP than for caffeine or quinine. 3. Verapamil and manganese inhibited 4-AP, caffeine and quinine-induced contractures. 4. Ca2+-free-EGTA Ringer and procaine severely inhibited caffeine and quinine responses, but 4-AP contractures were relatively unaffected. 5. In depolarizing (100 mM K+) Ringer solution, caffeine and quinine responses were reduced to 6-9% of their controls. 4-AP responses were reduced by about 25%. 6. It is concluded that in the toad rectus muscle, 4-AP-induced contractures differ from those produced by caffeine and quinine, and appear to rely mainly on the release of intracellular located Ca2+, while caffeine and quinine are considered to act predominantly on plasma membrane sites.

4-Aminopyridine↗
PubMedDate not supplied

Effects of local anesthetics on phorbol ester-induced ornithine decarboxylase activity in mouse and human skin.

In preparation for experiments to determine the effects of various orally administered compounds on human skin ornithine decarboxylase (ODC) activity, it was observed that intradermal lidocaine hydrochloride inhibited 12-0-tetradecanoylphorbol-13-acetate (TPA)-induced ODC. Topically applied ethyl chloride had variable and unpredictable effects on ODC induction. Adequate local anesthesia can be obtained by using intradermal 1.0% procaine hydrochloride or normal saline; neither of these agents inhibited TPA induction of epidermal ODC activity in incubated human skin punch biopsies.

Anesthetics, Local↗
PubMed1986

Liquid chromatographic determination of guanethidine salts and hydrochlorothiazide using electrochemical detection and ion-pair techniques.

A high-performance liquid chromatographic method with amperometric detection utilizing oxidation at the glassy carbon electrode is reported for the quantitative determination of a guanethidine (1)-hydrochlorothiazide (2) mixture. The drug mix is difficult to analyze by a single assay procedure due to large differences in the chemistry and chemical structure of the compounds. The drugs are best separated on an octadecylsilane column using 30:70 acetonitrile:0.05 M aqueous sodium dihydrogen phosphate containing 0.02 M sodium pentanesulfonate (pH 2.5) as the mobile phase at a 1.0 mL/min flow rate. Using a cell potential of +1300 mV versus Ag/AgCl and procaine hydrochloride as the internal standard, calibration curves were established for 1 monosulfate or sulfate and 2 in the 0.5-10 and 1.25-25 micrograms/mL range, respectively. Accuracy and precision of the assay are in the 1.7-6% range. The procedure is shown applicable to the analysis of a combination dosage form and is also useful for either drug in a single component dosage form.

Chromatography, High Pressure Liquid↗
PubMed1993

Inhibition by anaesthetics of 14C-guanidinium flux through the voltage-gated sodium channel and the cation channel of the 5-HT3 receptor of N1E-115 neuroblastoma cells.

The influence of local and general anaesthetics on cation influx through the fast, voltage-dependent sodium channel and the 5-HT3 receptor cation channel was studied in N1E-115 mouse neuroblastoma cells by measuring 2-min influx of the organic cation 14C-guanidinium induced by either veratridine (1 mmol/l) or 5-HT (100 mumol/l). The veratridine-induced influx of 14C-guanidinium was potentiated by scorpion toxin and inhibited by tetrodotoxin. The 5-HT-induced 14C-guanidinium influx was not affected by tetrodotoxin but it was inhibited by nanomolar concentrations of the selective 5-HT3 receptor antagonists ondansetron and ICS 205-930; at high micromolar concentrations these compounds also inhibited the veratridine-induced influx of 14C-guanidinium. The 14C-guanidinium influx through both channels was inhibited by local and general anaesthetics. The rank order of potency for inhibition of veratridine-induced influx by local anaesthetics was tetracaine > bupivacaine > cocaine > lidocaine > procaine and that for inhibition of the 5-HT3 receptor channel was tetracaine > bupivacaine > cocaine > procaine > lidocaine. With the exception of procaine and cocaine, which were equipotent at both channels, the local anaesthetics were 4.4-fold (lidocaine) to 25-fold (tetracaine) more potent at the fast sodium channel than at the 5-HT3 receptor channel. The rank order of potency for general anaesthetics was propofol > etomidate = alfaxalone = ketamine > thiopental = methohexital at the fast sodium channel, and propofol > or = etomidate > alfaxalone = methohexital > thiopental > ketamine at the 5-HT3 receptor channel.(ABSTRACT TRUNCATED AT 250 WORDS)

Anesthesia, General↗