PubMed Health⌕ Search

SEARCH · PubMed Health

Results for “PROPIOPHENONES”

Explore indexed PubMed citations for clinical trials, systematic reviews and public health research. Read source abstracts and follow each citation to its original PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 541 records · Page 30Linked to original sources
PubMed1985

Age-related changes in guinea pig respiratory tissues: considerations for assessment of bronchodilators.

Tracheal tissues from immature guinea pigs were significantly more sensitive to histamine and carbachol than their counterparts from mature animals. Bronchial but not tracheal tissues from immature animals were more sensitive to isoproterenol and salbutamol than tissues from mature animals. Functional antagonism between carbachol-induced tension and salbutamol-induced relaxation was greatest in bronchial tissues from immature animals. Functional antagonism was not evident when a concentration of histamine required to induce maximal but not supramaximal tension was used to induce tone. Inhibition of catechol-o-methyl transferase (COMT) with U 0521 (10 microM) or inhibition of extraneuronal uptake with hydrocortisone (200 microM), in tissues from animals in either age group, affected neither the potency of, nor the extent of relaxation induced by, isoproternol or salbutamol in histamine-contracted tissues. We conclude that extraneuronal uptake and metabolism by COMT do not modify tissue sensitivity to the relaxants studied. Therefore age-related changes in the relaxant properties of isoproterenol and salbutamol are not due to differences in their uptake or metabolism but probably reflect changes at the receptor level.

Age Factors↗
PubMed1986

Antiulcer and gastroprotective effects of solon, a synthetic flavonoid derivative of sophoradin. Role of endogenous prostaglandins.

Solon is a synthetic isoprenyl flavonoid derived from sophoradin which is isolated from the root of an ancient Chinese plant. Solon was administered orally or intraperitoneally to rats. It inhibited dose dependently gastric ulcers produced by acidified aspirin, water immersion and restraint stress. Solon was also gastroprotective for the stomach as it reduced dose dependently the gastric necrotic lesions induced by absolute ethanol given orally. The degree of gastroprotection decreased with time, the optimal effects occurring 60-90 min after oral administration. Pretreatment with indomethacin partly prevented the gastroprotective effects of Solon. When given alone to fasted rats, Solon increased dose dependently the mucosal content of prostaglandins (PG), suggesting that the protective effects of this drug may be mediated at least in part by endogenous PG.

Animals↗
PubMed1987

Intraventricular administration of l-kynurenine and kynuramine facilitates lordosis in the female rat.

Intraventricular administration of the tryptophan metabolites l-kynurenine (2-32 micrograms) and kynuramine (0.064-8 micrograms) facilitated lordosis behavior in estrogen-primed ovariectomized rats. The facilitatory effects of these drugs were not attenuated by pretreatment with the progesterone antagonist RU 38486, indicating that the effects were not mediated by release of adrenal progesterone. It is suggested that l-kynurenine and kynuramine may serve a physiological role in the modulation of female sexual behavior.

Animals↗
PubMed1987

Increase by 5-hydroxykynuramine of spontaneous acetylcholine release from myenteric neurons: mediated by serotonin M receptors.

The effects of 5-hydroxykynuramine (5-OH-K) and of 3-(2-amino-5-hydroxyphenyl)-propaneamine (AHPP) on spontaneous and electrically evoked release of [3H]acetylcholine were studied in the guinea-pig myenteric plexus longitudinal muscle preparation preincubated with [3H]choline. 5-OH-K caused a concentration-dependent increase in spontaneous [3H]acetylcholine release (EC50 5.3 microM). This effect was diminished in the presence of a desensitizing concentration of 5-hydroxytryptamine (5-HT). AHPP (1-100 microM) did not affect the spontaneous outflow of [3H]acetylcholine. The electrically evoked release of [3H]acetylcholine was significantly reduced in the presence of 100 microM of either 5-OH-K or AHPP. Metitepine did not antagonize the inhibition, which suggests that 100 microM of either compound non-specifically depressed the evoked release. It is concluded that 5-OH-K is inactive at the release-inhibitory 5-HT1 receptor, but is a potent agonist at the M receptor of myenteric neurons.

Acetylcholine↗
PubMed1988

Alifedrine, a positive inotropic agent that moderately reduces the severity of ischaemia and reperfusion-induced ventricular arrhythmias.

The effects of alifedrine, a positive inotropic agent, were examined in greyhounds anaesthetised with chloralose. An intravenous dose of 0.3 mg kg-1 resulted in a substantial increase in myocardial contractility (increased dP/dtmax, cardiac output and stroke volume) without significantly affecting heart rate. The effects of alifedrine on the severity of arrhythmias resulting from both coronary artery occlusion and reperfusion were also determined. A mild antiarrhythmic effect was observed during early ischaemia when the incidence of ventricular tachycardia was reduced from 90% in controls to 50% in treated dogs. There was also a significant reduction in the number of extrasystoles appearing as ventricular tachycardia (from 511 +/- 138 to 151 +/- 84). The total number of extrasystoles during the first 30 min of ischaemia was also reduced, although not significantly, from 846 +/- 193 to 527 +/- 86. Following release of a 40 min coronary artery occlusion there was a marked reduction in reperfusion-induced ventricular fibrillation from 75% in controls, to 37% in the alifedrine-treated dogs. The overall survival from the combined occlusion-reperfusion insult was increased from 20% in controls to 50%. These results suggest that alifedrine has an unusual and useful spectrum of pharmacological activity in that it combines antiarrhythmic activity with an ability to improve cardiac function.

Animals↗
PubMed1989

Suppression of calcium current in a snail neurone by eperisone and its analogues.

The effects of eperisone, tolperisone and isoperisone on the calcium current (ICa) were studied in an identified neurone of Achatina fulica under voltage clamping. At a holding voltage of -50 mV, these drugs inhibited ICa dose dependently without affecting activation time. Eperisone (IC50 = 0.348 mM) and isoperisone (0.226 mM) were significantly more effective than tolperisone (1.089 mM). Eperisone binds competitively with Ca2+ to the Ca2+ channels, based on its effects seen with various extracellular Ca2+ concentrations. The three drugs shifted the steady state inactivation curves in the hyperpolarizing direction. The mean dissociation constants for inactivated Ca2+ channels were calculated to be 0.070 mM (eperisone), 0.162 mM (tolperisone) and 0.014 mM (isoperisone). These values were much lower than their IC50 at Vh of -50 mV, which are reflected as the dissociation constants for resting Ca2+ channels. High frequency stimulation did not potentiate ICa suppression, suggesting that the drugs hardly bind to activated Ca2+ channels. These findings indicate that the selectivities of the Ca2+ channels to the drugs are in the order of their inactivated, resting and open states.

Animals↗
PubMed1992

Inhibitory effect of inaperisone hydrochloride (inaperisone), a new centrally acting muscle relaxant, on the micturition reflex.

We examined the effects of inaperisone hydrochloride (inaperisone), a new centrally acting muscle relaxant, on bladder function in anesthetized rats and isolated rat tissues. We also investigated its mechanism of action. When a balloon inserted into the bladder was expanded, rhythmic bladder contractions were observed; inaperisone (4 mg/kg i.v.) abolished these contractions, in both normal and decerebrated rats. The bladder tonus or bladder contraction induced by peripheral stimulation of the pelvic nerve was barely inhibited by inaperisone (4 mg/kg i.v.), but this dose of inaperisone abolished the efferent discharge from the pelvic nerve that accompanied the rhythmic bladder contractions. The doses of intracerebroventricularly (i.c.v.) and intrathecally injected inaperisone which abolished the rhythmic bladder contractions were 10 and 100 micrograms, respectively. The inhibitory effects of inaperisone (4 mg/kg i.v.) were not diminished by naloxone (1 mg/kg i.v.) or by bicuculline (0.5 mg/kg i.v.), but were diminished by phaclofen (30 mg/kg i.v. or 300 micrograms i.c.v.). The specific binding of [3H]baclofen to rat brain synaptosomal membranes was barely inhibited by inaperisone (up to 1 mM). From these results, it is speculated that, among other possible mechanisms, inaperisone inhibits the micturition reflex by acting indirectly on GABAB receptors in the brainstem.

Anesthesia↗
PubMed1995

Pharmacological properties of NK433, a new centrally acting muscle relaxant.

The pharmacological properties of NK433 ((-)-(R)-2-methyl-3-(1-pyrrolidinyl)-4'-trifluoromethylpropiophenone+ ++ monohydrochloride), a novel muscle relaxant, were investigated. NK433 inhibited intercollicular decerebrate rigidity (gamma-rigidity) and anemic decerebrate rigidity (alpha-rigidity) dose dependently. NK433 was stronger in inhibiting gamma-rigidity than alpha-rigidity. NK433 inhibited the increase in muscle spindle discharges induced by pinna pinching (gamma-activity) without affecting muscle spindle discharges or neuromuscular transmission. At muscle relaxant doses in decerebrate rigidities, NK433 did not affect the muscle tone induced by morphine-HCl nor that of normal animals. These results suggest that NK433 selectively depresses the excessive muscle tone of decerebrate rigidities through its effects on the central nervous system, and inhibition of gamma-activity causes a preferential depression of gamma-rigidity in comparison to alpha-rigidity. In i.v. experiments, the effects of NK433 on decerebrate rigidities were similar to those of eperisone-HCl and tolperisone-HCl, but in p.o. experiments, NK433 was at least 3 times as potent as eperisone-HCl and tolperisone-HCl.

Analgesics↗
PubMed1996

Effects of NK433, a new centrally acting muscle relaxant, on masticatory muscle reflexes in rats.

The effects of (-)-(R)-2-methyl-3-(1-pyrrolidinyl)-4'- trifluoromethylpropiophenone monohydrochloride (NK433), a novel centrally acting muscle relaxant, on masticatory muscle reflexes were investigated in rats. NK433 inhibited the monosynaptic tonic vibration reflex of the masseter muscle and the polysynaptic tonic periodontal masseteric reflex. These reflexes are increased by gamma-motor activity. NK433 had a weak inhibitory effect on the polysynaptic jaw opening reflex evoked by electrical stimulation of the tooth pulp, which is little related with gamma-motor activity. Eperisone-HCl depressed the three types of masticatory muscle reflexes. When intravenously administered, eperisone-HCl was equipotent to NK433, but the effect of eperisone-HCl was shorter-lasting than that of NK433. The effect of intragastrically administered NK433 on the periodontal masseteric reflex was about three times stronger than that of eperisone-HCl. These results suggest that NK433 inhibits masticatory muscle reflexes controlled by the gamma-motor system and thus may ameliorate the temporomandibular joint syndrome in man.

Animals↗
PubMed1987

Suppression of c-mos expression in teratocarcinoma cells with a new type of inducer of differentiation, 3,5-di-tert-butylchalcone 4'-carboxylic acid.

The treatment of 311 cells, a pluripotent mouse teratocarcinoma cell line, with a new type of inducer, 3,5-di-tert-butylchalcone 4'-carboxylic acid (Ch55), results in the suppression of the c-mos gene, accompanied by early marker changes associated with cell differentiation, i.e., the enhanced secretion of plasminogen activator and the decrease in peanut agglutinin receptors and glucose transport. This indicates that Ch55 is a potent inducer of teratocarcinoma cells and suppresses c-mos expression.

3-O-Methylglucose↗
PubMed1990

Catecholamines inhibit steroidogenesis by cultured porcine thecal cells.

The ovaries of many species contain catecholamines and beta-adrenergic receptors. The present studies were done to determine if catecholamines play a role in the regulation of androgen production by porcine theca cells. Basal and luteinizing hormone (LH)-stimulated androstenedione production was significantly inhibited by noradrenaline and isoproterenol. The inhibitory effects were dose-dependent and were enhanced when the cultures contained the carboxy-O-methyl transferase inhibitor, U-0521. The inhibitory effect of isoproterenol was reversed by the beta-adrenergic antagonist, metoprolol. Isoproterenol caused a generalized inhibition of LH-stimulated steroidogenesis, decreasing the accumulation of pregnenolone, progesterone, androstenedione and estradiol in the culture medium. These studies suggest that catecholamines may be important regulators of thecal androgen production.

Androstenedione↗