PMID: 9530991Apr 8, 1998Paper

Affinity constants and beta-adrenoceptor reserves for isoprenaline on cardiac tissue from normotensive and hypertensive rats

The Journal of Pharmacy and Pharmacology
Sheila A DoggrellC W Barnett

Abstract

To determine whether there are differences in cardiac beta-adrenoceptor responsiveness, isoprenaline affinity constants and fractional beta-adrenoceptor occupancy-response relationships for isoprenaline in the early stages of established hypertension, we studied the effects of bromoacetylalprenololmenthane (BAAM) and ([3,5-diamino-6-chloro-N-(1[N-beta-(2-hydroxyl-3-alpha-naphthoxypropy lamino)ethylcarbamoyl]-1-methylethyl)-pyrazine-2-carboxamide (ICI 147 798), slowly reversible beta-adrenoceptor antagonists, on the isoprenaline responses of the left ventricular papillary muscle and the left and right atria of 6-month-old Wistar Kyoto rats (WKY) and spontaneously hypertensive rats (SHR). The papillary muscles, but not the right and left atria, of the SHR were less responsive to isoprenaline than those of the WKY. The isoprenaline pD2 values (the negative logarithms of the molar concentrations of agonist producing 50% of the maximum response) were 7.72 and 8.00 on the SHR and WKY papillary muscles, respectively. On the WKY papillary muscle the isoprenaline KA values were 2-3 x 10(-6) M, which is as expected for isoprenaline at beta1 or beta2-adrenoceptors. Isoprenaline had 100-fold greater affinity on the WKY and SHR left atria t...Continue Reading

References

Oct 1, 1988·Naunyn-Schmiedeberg's Archives of Pharmacology·M BöhmE Erdmann
Jul 1, 1985·Hypertension·P G McGuire, T A Twietmeyer
Dec 1, 1982·Journal of Autonomic Pharmacology·R R Ruffolo
Oct 1, 1994·Cardiovascular Research·S E HardingP A Poole-Wilson
Jun 1, 1995·Clinical and Experimental Pharmacology & Physiology·A HoeyL Brown

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Citations

Feb 15, 2011·Naunyn-Schmiedeberg's Archives of Pharmacology·Aida Salameh, Stefan Dhein
Jan 27, 1999·Journal of Pharmacological and Toxicological Methods·V Calderone, E Martinotti
Dec 15, 2005·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·A SalamehS Dhein
Apr 24, 2017·Kidney International·Yoshiki HigashijimaOsamu Nureki

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