• YAKHAK HOEJI
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• v.43 no.2
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• pp.150-159
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• 1999

Hollow type suppositories inserted polyvinyl alcohol (PVA) hydrogel capsule containing propranolol·HCI (PPH) were prepared using different bases, polyethylene glycol (PEG), Witepsol H-15 (WH-15) and Witepsol W-35 (WW-35) to improve the controlled release of PPH. The release of PPH from the hollow type suppository inserted PVA hydrogel capsule was retarded than that from PEG, WH-15, or WW-35 hollow type suppositories in rat rectal cavity. When the suppositories were administered to rats, the controlled release of PPH was proved by the plasma concentration-time-profiles of PPH. No significant difference (p〈0.05) among the three different hollow type suppositories was observed in terms of AUC and MRT of PPH. WH-15 hollow type suppository inserted 12% of PVA hydrogel capsule caused irritation to rat rectal mucosa. However, the WH-15 hollow type suppository inserted PVA hydrogel capsule caused no severe irritation on rectal mucosa. The application of the hollow type suppositories using PVA in sustained rectal delivery of drugs might be feasible.

• The Korean Journal of Pharmacology
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• v.12 no.2 s.20
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• pp.7-11
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• 1976

A portion of duodenum laid pancreatic duct opening were perfused continuously with physiological saline under urethane anesthesia in rats. The pancreatic amylase secretory response to caerulein was studied with autonomic blockers, such as phenoxybenzamine, dibenamine, phentolamine, hexamethonium, propranolol, atropine, and cyproheptadine. The pancreatic amylase output to caerulein, 7.5ng/kg i.v., was markedly increased and the value was approximately three times greater than control. The caerulein-stimulated pancreatic amylase secretion was significantly decreased by i.v. phenoxybenzamine and propranolol treatment, but not by phentolamine or dibenamine. Secretory response of pancreatic amylase to caerulein was not affected by i.v. atropine, hexamethonium or cyproheptadine. These result lead to the conclusion that phenoxybenzamine may inherently inhibit the secretory response of pancreatic amylase to caerulein, and this effect was not related with ${\alpha}-adrenergic$ receptor blocking action.

• Biomolecules & Therapeutics
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• v.8 no.4
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• pp.305-310
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• 2000

The present study examined the effect of a methanol extract of Evodiae Fructus on the blood pressure in spontaneously hypertensive rats (SHR). The systolic blood pressure was measured after rats were pretreated with phentolamine, propranolol, or $N_{\omega}$-nitro-$_{L}$-arginine methyl ester(NAME) and subsequently received methanol extract of Evodiae Fructus. In SHR, intraperitoneal administration of methanol extract of Evodiae Fructus (0.5 mg/kg) produced antihypertensive effect that lasted for at least 4 hours. Antihypertensive effect of Evodiae Fructus was more stronger than that with $\alpha$-adrenergic receptor antagonist phentolamine and was not affected by $\beta$-adrenergic receptor antagonist propranolol. The antihypertensive effect of Evodiae Fructus was abolished by pretreatment of NAME. Our findings suggest Evodiae Fructus has an hypertensive effect, which may be mediated through nitric oxide synthesis.s.

• Korean Journal of Veterinary Research
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• v.14 no.2
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• pp.207-210
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• 1974

Pharmacological investigation was performed in chickens which were pretreated with reserpine. Transmural stimulations were given to the isolated jejunum of chickens and studied the responses and the effects of dibenamine, propranolol, atropine and tetrodotoxin on them. The results obtained were summerized as follows: 1. Three different patterns of response were obtained from the isolated jejunum of non-treated chickens after giving them transmural stimulation. The first pattern was contraction followed by relaxation, the second pattern was contraction only and the third pattern was relaxation only. 2. The transmural stimulation of the jejunum preparations evoked relaxation while the periarterial stimulation evoked contraction in the reserpinized chick. 3. The relaxation response to the transmural stimulation was not affected by the pretreatment with dibenamine, propranolol and atropine. 4. The relaxation response to the transmural stimulation was abolished by tetrodotoxin. The results obtained in these studies indicate that the relaxation response to the transmural stimulation is due to non-adrenergic inhibitory fibers.

• Journal of Pharmaceutical Investigation
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• v.25 no.4
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• pp.365-369
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• 1995

The acute cytotoxicities of chloroquine sulfate, propranolol, ascorbic acid, acetylsalicylic acid and acrylamide on cultured adult rat hepatocytes were evaluated by the use of LDH leakage and NR uptake test. On the basis of $IC_{50}$ values, the rank order of cytotoxicities of these drugs in both tests was chloroquine sulfate > propranolol > acetylsalicylic acid > ascorbic acid. The $IC_{50}$ of LDH test was very similar to that of NR uptake test. Thus, we concluded that both tests are reliable and sensitive methods in detecting toxicity in adult cultured rat hepatocytes.

• Archives of Pharmacal Research
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• v.18 no.2
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• pp.129-132
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• 1995

Intravenous administration of O-acetyliervine (an alkaloid from Vertrum album) produced a dose-dependent (10-100 .mu.g/kg) fall in blood pressure and tachycardia in anaesthetized normotensive rats. Pretreatment of animals with propranolol (1mg/kg) abolished these cardiovascular responses of O-acetyljervine similar to that of isoprenaline $(1\mu/ml)$. In isolated tissue experiments, O-acetyljervine $(10-100\mu/ml)$ produced a dose-dependent relaxation of phenylephrine-induced contraction of the rabbit aorta. In guinea-pig spontaneously beating atria, it caused positive inotropic and chronotorpic responses in a dose-dependent fashion $(10-100\mu/ml)$. These responses were abolished in the presence of propranolol $(1\mu/ml)$ similar to that of isoprenaline. These results indicate that O-accetyljervine is adrenoceptor stimulant $(\beta_1\; and\;beta_2)$ like isoprenaline.

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.308.1-308.1
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• 2003

We underwent this study to know correlation between the amount of portosysternic shunt/hepatic fibrosis and bioavailability parameters such as AUC, Cmax, Tmax and t1 /2 of high extraction ratio drug, propranolol, in CCl4-induced liver cirrhosis model of rats. This study describes the bioavaility study of propranolol(5 mg/kg), Shunt Index using thallium-201 per rectum scintigraphy to to measure the amount of portosystemic shunt indirectly and intrahepatic hydroxyproline content performed in the CCl4-induced liver cirrhosis model of rats. (omitted)

• 대한핵의학회:학술대회논문집
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• 1978.06a
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• pp.67-67
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• 1978

• Korean Journal of Veterinary Research
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• v.41 no.4
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• pp.497-503
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• 2001

Evidence from the last 10 years have been suggested that melatonin mainly produce a depressant effect on the cardiac system, but we found an activating effect of melatonin on heart rate in this research. To determine the hypothesis that melatonin has dual effects on physiological behaviour of cardiac system, we investigated the effects of melatonin on heart rate in isolated rat atria and anesthetized rats. Regardless of concentration, melatonin produced bradycardia in the 84 cases of 148 experiments (57 %) and tachycardia in the 64 cases of 148 experiments (43 %). And in atrium, melatonin produced a decrease automaticity in 52 cases of 86 experiments (60 %) and increase automaticity in 40 % (34/86 cases). Also, these effects are not significnat relationship with concetration of melatonin. The melatonin-induced bradycardia in vivo was inhibited by pretreatment of atropine or bilateral cervical vagotomy. Also, in isolated atrium the melatonin-induced decrease in automaticity was inhibited by pretreatment of atropine. These melatonin-induced responses were potenitated by pretreatment of propranolol. The melatonin-induced tachycardia in vivo was inhibited by pretreatment of propranolol, nifedipine or bilateral cervical vagotomy, but not by pretreatment of atropine. The melatonin-induced incease in automaticity in isolated atrium was converted to decrease in automaticity by pretreatment of propranolol. In addition, the change in heart rate caused by adrenoceptor agonists was inhibited by pretreatment of melatonin. These results indicate that melatonin-induced bradycardia may be related to a muscarinic receptor activation and melatonin-induced tachycardia may be related to a $\beta$-adrenoceptor stimulation.

• BMB Reports
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• v.47 no.9
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• pp.506-511
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• 2014

We investigated the effects of high calorie and low calorie diets on skeletal integrity, and whether ${\beta}$-adrenergic blockade (BB) attenuates bone loss induced by dietary calorie alteration. Male 6-week-old C57BL/6 mice were assigned to either an ad-lib fed control diet (CON), a high calorie diet (HIGH), or a low calorie diet (LOW) group. In each diet group, mice were treated with either vehicle (VEH) or propranolol, a ${\beta}$-adrenergic antagonist. Over 12-weeks, ${\beta}$-blockade mitigated body weight and fat mass increases induced by the high calorie diet. Femoral trabecular bone mineral density and the expression levels of osteogenic marker genes in bone marrow cells were reduced in HIGHVEH and LOWVEH mice, and BB significantly attenuated this decline only in HIGH mice. In summary, the magnitude of bone loss induced by low calorie diet was greater than that caused by high calorie diet in growing mice, and ${\beta}$-blockade mitigated high calorie diet-induced bone loss.