Characterization of propranolol-induced relaxation of coronary artery.

Sakanashi, Matao; Takeo, Satoshi

doi:10.1254/jjp.33.603

Cited by 14 publications

(10 citation statements)

References 12 publications

(10 reference statements)

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“…22 Earlier studies have shown that propranolol relaxes dog coronary arteries, possibly through inhibition of calcium influx in the cell membrane. 23,24 Nevertheless, no further studies have been undertaken to gain an understanding of the receptor-independent mechanisms by which propranolol exerts its vasodilatory effect and the contribution of the endothelium to this phenomenon. Therefore, the aim of the present study was to investigate the underlying mechanisms by which propranolol induces relaxation in rat isolated aorta and mesenteric artery, focusing on the contribution of the NO-c GMP pathway and Ca 2+ entry blockade to arterial resistance.…”

Section: Introductionmentioning

confidence: 99%

Vasorelaxing Effects of Propranolol in Rat Aorta and Mesenteric Artery: A Role for Nitric Oxide and Calcium Entry Blockade

Priviero

Teixeira

Toque

et al. 2006

Clin Exp Pharma Physio

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1. Propranolol has been prescribed successfully to patients with cardiovascular diseases, but the exact mechanisms by which it reduces peripheral vascular resistance have been poorly investigated. 2. The present study was designed to investigate the relaxing effects of propranolol in the rat isolated aorta and mesenteric artery, focusing on the contribution of the nitric oxide (NO)-cGMP pathway and calcium entry blockade. Relaxation responses to propranolol were obtained in precontracted rat aortic and mesenteric artery rings. 3. DL-Propranolol (10-100 micromol/L) produced concentration-dependent relaxations in the aorta and mesenteric artery rings with intact endothelium. The isomers D- and L-propranolol produced relaxation responses that were equipotent to the racemic mixture. 4. Metoprolol (10-100 micromol/L) produced slight relaxations, whereas atenolol (10-100 micromol/L) had no relaxant activity. 5. The NO inhibitor N(G)-nitro-L-arginine methyl ester (100 micromol/L) and the soluble guanylate cyclase inhibitor 1H-[1,2,4]oxadiazolo[4,3-a]quinoxalin-1-one (1 micromol/L), as well as removal of the endothelium, significantly reduced the relaxation responses induced by the lower concentrations of propranolol without affecting maximal responses. In addition, DL-propranolol markedly increased cGMP levels in endothelium-intact preparations. 6. In Ca(2+)-free Krebs' solution, DL-propranolol (10-100 micromol/L) caused marked rightward shift in the concentration-response curves to CaCl(2), with a decrease of maximal responses in tissues with either intact or denuded endothelium. Nifedipine (1 micromol/L) in combination with DL-propranolol virtually abolished the CaCl(2)-induced contractile responses. 7. The relaxation responses induced by DL-propranolol were significantly reduced in aortic and mesenteric rings precontracted with phorbol-12,13-dibutyrate (1 micromol/L). 8. In conclusion, DL-propranolol relaxes arterial smooth muscle by mechanisms involving activation of the NO-cGMP pathway and calcium influx blockade, independent of beta-adrenoceptor blockade.

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Section: Introductionmentioning

confidence: 99%

Vasorelaxing Effects of Propranolol in Rat Aorta and Mesenteric Artery: A Role for Nitric Oxide and Calcium Entry Blockade

Priviero

Teixeira

Toque

et al. 2006

Clin Exp Pharma Physio

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show abstract

“…It has been reported that there is no difference between the d and I-isomer of propranolol regarding the potency to inhibit high K or Ca-induced contractions in the coronary artery of the dog and taenia coli of the guinea pig (3,21). On the other hand, significant stereoselectivity has been shown to exist for the inhibitory effects of organic Ca-antagonists on the Ca-channels (22).…”

Section: Methodsmentioning

confidence: 99%

“…These results may suggest that pro pranolol inhibits Ca channels due to non specific actions on the membrane rather than the direct blocking actions of Ca channels as organic Ca-antagonists do. However, inhibition of Ca channels by propranolol may be caused by a mechanism other than one which involves local anes thetic action since inhibition of contractions by local anesthetics was much weaker in the vas deferens and coronary artery (4,21).…”

Section: Methodsmentioning

confidence: 99%

Inhibitory Action of Propranolol on the Contractions Induced by Nerve Stimulations or Calcium in the Smooth Muscle of Rat Vas Deferens

Suzuki

Inagaki

Kasuya

1986

Japanese Journal of Pharmacology

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“…In contrast, R‐ but not S‐propranolol inhibits the conversion of thyroxine to triiodothyronine 12 . However, both enantiomers of propranolol are equipotent with regard to the membrane stabilizing effect 13,14 …”

Section: Introductionmentioning

confidence: 99%

“…12 However, both enantiomers of propranolol are equipotent with regard to the membrane stabilizing effect. 13,14 Because nipradilol possesses two asymmetric carbon atoms in its chemical structure, it has four optical isomers. Nipradilol is an equal mixture of four optical isomers, as shown in Fig.…”

Section: Introductionmentioning

confidence: 99%

β‐Adrenoceptor Blocking Activities Of Nipradilol And Its Optical Isomers In Pig Coronary Artery

Itomine

Matsuzaki

Sakanashi

et al. 2001

Clin Exp Pharma Physio

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1. beta-Adrenoceptor blocking activities of nipradilol, its four optical isomers (RR, RS, SR, SS) and denitro nipradilol were evaluated using pig isolated coronary arteries. 2. (-)-Isoprenaline produced concentration-dependent relaxations of the arteries, which were antagonized by nipradilol, its four optical isomers or denitro nipradilol under KCl-induced contracture. 3. The order of pA2 values for beta-adrenoceptor blocking activities was SR > nipradilol > SS > or = denitro nipradilol > RR > RS. 4. The nitroxy group in nipradilol appears to enhance its beta-adrenoceptor blocking activity, because the beta-adrenoceptor blocking activity of nipradilol was more potent than that of denitro nipradilol. 5. Isomers that have the S configuration (SR, SS) at the 2' position (having a hydroxyl group) in the aryloxypropanolamine showed more potent beta-adrenoceptor blocking activity than isomers that have the R configuration (RR, RS). 6. Isomers that have the R configuration (SR, RR) at the 3 position (having a nitroxy group) in the benzopyran ring showed more potent beta-adrenoceptor blocking activity than those with the S configuration (SS, RS). 7. It is suggested that the difference in configuration of the chemical structure of nipradilol may result in variations of binding affinity for the beta-adrenoceptor.

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Characterization of propranolol-induced relaxation of coronary artery.

Cited by 14 publications

References 12 publications

Vasorelaxing Effects of Propranolol in Rat Aorta and Mesenteric Artery: A Role for Nitric Oxide and Calcium Entry Blockade

Vasorelaxing Effects of Propranolol in Rat Aorta and Mesenteric Artery: A Role for Nitric Oxide and Calcium Entry Blockade

Inhibitory Action of Propranolol on the Contractions Induced by Nerve Stimulations or Calcium in the Smooth Muscle of Rat Vas Deferens

β‐Adrenoceptor Blocking Activities Of Nipradilol And Its Optical Isomers In Pig Coronary Artery

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