• The Korean Journal of Pharmacology
• /
• v.15 no.1_2 s.25
• /
• pp.7-12
• /
• 1979

Employing clonidine, phenoxybenzamine, and phentolamine, the author attempted to clarify the mechanism of the pressor response in raised intracranial pressure (ICP) in urethaneanesthetized rabbits. Intravenous clonidine inhibited the pressor response in raised ICP as intraventricular (I.V.T ) clcnidine did. Intravenous phenoxybenzamine and phentolamine weakened markedly the pressor response in raised ICP I.V.T. phenoxybenzamine did not affect the pressor response as I.V.T. phentolamine. I.V.T. phenoxybenzamine antagonized the inhibitory effect of I.V.T. clonidine on the pressor response as I.V.T. phentolamine. It is concluded that the central and peripheral sympathetic activity plays an important role in producing the pressor response in raised ICP.

• The Korean Journal of Pharmacology
• /
• v.24 no.1
• /
• pp.83-92
• /
• 1988

Although the release of lysosomal enzymes from activated PMN leukocyte can be regulated by intracellular cyclic nucleotide levels, other responses of PMN leukocyte according to the binding of neurotransmitters to either ${\beta}$-adrenergic or muscarinic receptors are still not clarified. In addition, the function of PMN leukocyte mediated by ${\alpha}$-adrenergic receptors is uncertain. Atropine, phentolamine and propranolol inhibited calcium uptake, superoxide generation, NADPH oxidase activity and phagocytic activity in activated PMN leukocyte, whereas carbachol and isoproterenol slightly further stimulated the responses of activated cells. Either carbachol or isoproterenol stimulated superoxide generation was inhibited by their antagonists, atropine and propranolol, respectively. The response of activated PMN leukocyte was inhibited by chlorpromazine, verapamil and dantrolene but slightly stimulated by lithium. On the other hand, chlorpromazine and dibucaine did not affect NADPH oxidase activity. Atropine, phentolamine and propranolol suppressed the calcium dependent phagocytic activity. Thus, the results suggest that atropine, phentolamine and propranolol may inhibit superoxide generation in activated PMN leukocyte by the inhibition of calcium influx and by their direct action on the NADPH oxidase system which is associated with autonomic receptors.

• YAKHAK HOEJI
• /
• v.23 no.1
• /
• pp.31-39
• /
• 1979

Bethanidine was administered into the lateral ventricle of the rabbit brain for the investigation of the effect on the renal function in doses ranging from 0.1 to 1.0mg/kg. In a dose of 0.1 mg/kg, bethanidine did not exhibit significant changes on the renal function of the rabbit, on the other hand, in the doses of 0.3 and 1.0mg/kg bethanidine elicited the reduction of renal plasma flow and glomerular filtration rate with a marked antidiuresis, at the same time bethanidine produced the decrement of urinary sodium and potassium excretion. After intravenous pretreatment of phentolamine, intraventricular bethanidine in a dose of 0.3mg/kg did not produced the antidiuresis and the decrement of urinary sodium and potassium excretion, wherease renal plasma flow and glomerular filtration rate reduced as before of phentolamine pretreatment although the durations of their reduction were shortened. These observations suggest that bethanidine induces the antidiuresis through the centrally mediated mechanism which interposed other factors in addition to sympathetic stimulation affected by phentolamine, alpha adrenergic blocking agent.

• Journal of Dental Anesthesia and Pain Medicine
• /
• v.21 no.1
• /
• pp.49-59
• /
• 2021

Background: To evaluate changes in the effectiveness of phentolamine mesylate in combination with different local anesthetics (LAs) and vasoconstrictors. A prospective randomized double-blind study was conducted with 90 patients divided into three groups, with each group being administered one of three different LAs: lidocaine 2% 1/80,000, articaine 4% 1/200,000, and bupivacaine 0.5% 1/200,000. Methods: We compared treatments administered to the mandible involving a LA blockade of the inferior alveolar nerve. Results were assessed by evaluating reduction in total duration of anesthesia, self-reported patient comfort using the visual analog pain scale, incidence rates of the most common adverse effects, overall patient satisfaction, and patient feedback. Results: The differences among the three groups were highly significant (P < 0.001); time under anesthesia was especially reduced for both the lip and tongue with bupivacaine. The following adverse effects were reported: pain at the site of the anesthetic injection (11.1%), headaches (6.7%), tachycardia (1.1%), and heavy bleeding after treatment (3.3%). The patients' feedback and satisfaction ratings were 100% and 98.9%, respectively. Conclusions: Efficient reversal of LAs is useful in dentistry as it allows patients to return to normal life more readily and avoid common self-injuries sometimes caused by anesthesia. Phentolamine mesylate reduced the duration of anesthesia in the three studied groups, with the highest reduction reported in the bupivacaine group (from 460 min to 230 min for the lip and 270 min for the tongue [P < 0.001]).

• The Korean Journal of Pharmacology
• /
• v.12 no.2 s.20
• /
• pp.7-11
• /
• 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
• /
• v.8 no.4
• /
• pp.305-310
• /
• 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.

• The Journal of Korean Medicine
• /
• v.18 no.1
• /
• pp.267-277
• /
• 1997

Experiments were performed to determine the effects of the Oyacksunkisan(烏藥順氣散) and Kamioyacksunkisan(加味烏藥順氣散) liquid extract on the hypertension and the pulse rate in Sprague-Dawley rat(SDR) and Spontaneous Hypertensive rats(SHR). The results were obtained as follows ; 1. Blood pressure was significantly decreased firstday and 11th day after administration of Oyacksunkisan extract and pretreatment of phentolamine. 2. Blood pressure and pulse rate were regulated first day after administration of Kamioyacksunkisan and blood pressure was significantly decreased after pretreatment of clonidine and phentolamine. 3. Oyacksunkisan and Kamioyacksunkisan didn't show any significant changes of blood pressure and pulse rate after pretreatment of prdpranolol, hydralazine and verapamil From the above result, it was concluded that Oyacksunkisan(烏藥順氣散) and Kamioyacksunkisan(加味烏藥順氣散) could be applied effectively to the hypertension.

• Restorative Dentistry and Endodontics
• /
• v.21 no.1
• /
• pp.375-384
• /
• 1996

The purpose of this study was to investigate the functional involvement of sympathetic nerve in the control of the microcirculation in the dental pulp with the aim of elucidation of the involvement of neuropeptides and sympathetic nerve in neurogenic inflammation. Experiments were done on the 7 cats anesthetised with sodium pentobarbital, and sympathetic nerve to the' dental pulp was stimulated electrically (10 Hz, 4 V, 1.5 ms, 3.5 mins). Ana-adrenoceptor antagonist phentolamine and a neuropeptide Y antagonist D-myo-inositol-1,2,6-trisphosphate (PP56) were injected close intra-arterially into the dental pulp without changing the systemic blood pressure. The probe of laser Doppler flowmeter was placed on the buccal surface of ipsilateral canine teeth to the stimulation, and pulpal blood flow was measured. Stimulation of the sympathetic nerve decreased pulpal blood flow by $55.24{\pm}7.74\;%$ (mean${\pm}$SEM, n = 13). Stimulation of the sympathetic nerve following the injection of the ${\alpha}$-adrenoceptor antagonist phentolamine ($0.1{\mu}g$/kg) caused decrease of pulpal blood flow by $14.35{\pm}3.43%$ (mean${\pm}$SEM, n=5). Phentolamine attenuated the sympathetic nerve-induced pulpal blood flow decrease by $74.02{\pm}9.32%$ (mean${\pm}$SEM) Stimulation of the sympathetic nerve following the injection of the neuropeptide Y antagonist PP56 (2.3 mg/kg) caused decrease of pulpal blood flow by $30.64{\pm}7.92%$ (mean${\pm}$SEM, n=6). PP56 attenuated the sympathetic nerve-induced pulpal blood flow decrease by $44.37{\pm}11.01%$ (mean${\pm}$SEM). These data provide evidences of the co-contribution of nerepinephrine and neuropeptide Y on the sympathetic nerve-induced vasoconstriction in the feline dental pulp. In addition, they show functional evidences that sympathetic nerve plays an active role in controlling the microcirculation of the dental pulp.

• The Korean Journal of Pharmacology
• /
• v.28 no.1
• /
• pp.75-79
• /
• 1992

Higenamine, which is one of active component of Aconiti tuber, has been known to have positive inotropic effect through adrenergic beta-receptor. The effect of higenamine on norepinepharine or potassium induced contraction of pulmonary aorta in rabbit were studies. 1. The contraction of aortic strips induced by norepinephrine was suppressec by pre-or post-treatment of higenamine dose dependently and those effects of higenamine were prevented by propranolol. The $pA_2$ value of higenamine against propranolol calculated as 8.25. 2. The effect of higenamine was not affected by phentolamine. 3. Isoprotrenol has shown 10 times stronger vasodiatory effect on norepinephrine induced cntracture than that of higenamine but high concentration $(3.3{\times}10^{-6}\;M)$ of isoproterenol produce intrinsic activity. 4. Vasodilatory effect of higenamine or isoproterenol was not observed in potassium induced contacture of pulmonary aortic strips. These results strongly suggest that higenamine dilated the pulmonary vascular smooth muscle through stimulation of adrenergic beta-receptor.

• The Korean Journal of Pharmacology
• /
• v.29 no.1
• /
• pp.65-72
• /
• 1993

Ultraviolet light radiation (UVR) did not affect resting tension of isolated thoracic aortae of rats. In aortic rings contracted with phenylephrine, however, UVR produced contractile and relaxant responses in preparations with and without endothelium, respectively. The contractile response was dependent upon the duration $(10{\sim}320\;sec)$ of irradiation, while the relaxation was not. UVR-induced contractions in endothelium-intact rings were significantly potentiated by increasing the concentrations of phenylephrine from $10^{-7}M$ to $10^{-5}M$, and also by addition of $10^{-6}M$ acetylcholine, $10^{-7}M$ isoproterenol and $3.5{\times}10^{-8}M$ nitroglycerine. However, addition of $10^{-6}M$ phentolamine, or $10^{-7}M$ to $10^{-6}M$ LY83583 inhibited the contraction or reversed the contraction to a relaxation. In endothelium-removed preparations the UVR-induced relaxation was attenuated by increasing concentractions of phenylephrine, and by addition of isoproterenol, nitroglycerin, phentolamine or LY83583. These results suggest that UVR produces contractile and relaxant responses in rat thoracic aortae with and without endothelium, respectively, and that the contractile effect results from the inhibition of endothelium-derived relaxing factor (EDRF) release by UVR the inhibition of and/or is in part re-lated to some endothelium-derived contractile factors (EDCFs).