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beta-adrenoreceptor blocking and antihypertensive activity of PP-24, a newly synthesized aryloxypropanolamine derivative.

Abstract
PP-24 is a newly synthesized putative beta-adrenoceptor antagonist. The objective of the study was to the evaluate beta-adrenoceptor blocking activity of PP-24 on isolated rat preparations: right atria, uterus and colon. Effects on the rat ECG and renal hypertension (induced by left renal artery ligation) were also investigated. Treatment with PP-24 (3 and 10 mg kg(-1)) for 7 days in rats with renal hypertension significantly reduced the mean atrial blood pressure. Single i.v. injections of isoprenaline (0.3, 1 and 3 microg kg(-1)) alone in normal anaesthetized rat caused hypotension and tachycardia, while PP-24 alone produced dose-dependent falls in mean aterial pressure and bradycardia. Pretreatment of anaesthetized rats with test compounds significantly blocked the hypotension response but not the tachycardia induced by isoprenaline (0.3, 1 and 3 microg kg(-1)). The pA(2) of PP-24 to beta(1)-, beta(2)- and beta(3)-adrenoceptors was 7.72 +/- 0.082, 7.40 +/- 0.082 and 6.39 +/- 0.16, respectively. The beta(1)/beta(2) selectivity ratio was 2.08, compared with 1.27 for propranolol and 39.17 for atenolol. It is concluded that PP-24 possesses beta-adrenoceptor blockade activity but with non-specific affinity for beta(1)- and beta(2)-adrenoceptor subtypes. The rank order of potency of the antagonists for beta(1)-adrenoceptors was atenolol > PP-24 > propranolol. The antihypertensive activity of PP-24 in rats with renal hypertension appears to be due to blockade of beta-adrenoceptors.
AuthorsAniket P Nikam, Subhash L Bodhankar, Poonam Piplani, Jyotika Bansal, Prasad A Thakurdesai
JournalThe Journal of pharmacy and pharmacology (J Pharm Pharmacol) Vol. 60 Issue 11 Pg. 1501-6 (Nov 2008) ISSN: 0022-3573 [Print] England
PMID18957171 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • 1-(isopropylamino)-3-(5-((isopropylamino)methyl)-2-methoxyphenoxy)propan-2-ol
  • Adrenergic beta-1 Receptor Antagonists
  • Adrenergic beta-2 Receptor Antagonists
  • Adrenergic beta-3 Receptor Antagonists
  • Adrenergic beta-Antagonists
  • Benzylamines
  • Propanolamines
  • Atenolol
  • Propranolol
  • Isoproterenol
Topics
  • Adrenergic beta-1 Receptor Antagonists
  • Adrenergic beta-2 Receptor Antagonists
  • Adrenergic beta-3 Receptor Antagonists
  • Adrenergic beta-Antagonists (administration & dosage, pharmacology)
  • Animals
  • Atenolol (pharmacology)
  • Benzylamines (administration & dosage, pharmacology)
  • Blood Pressure (drug effects)
  • Colon (drug effects, metabolism)
  • Dose-Response Relationship, Drug
  • Electrocardiography
  • Female
  • Heart Atria (drug effects, metabolism)
  • Hypertension, Renal (drug therapy)
  • Isoproterenol (administration & dosage, pharmacology)
  • Male
  • Propanolamines (administration & dosage, pharmacology)
  • Propranolol (pharmacology)
  • Rats
  • Rats, Wistar
  • Uterus (drug effects, metabolism)

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