Cardiovascular actions of a new selective postjunctional alpha-adrenoceptor antagonist, SK&F 104856, in normotensive and hypertensive dogs

Br J Pharmacol. 1992 Apr;105(4):992-6. doi: 10.1111/j.1476-5381.1992.tb09090.x.

Abstract

1. SK&F 104856 (2-vinyl-7-chloro-3,4,5,6-tetrahydro-4- methylthieno[4,3,2ef][3]benzazepine) is a novel postjunctional alpha 1- and alpha 2-adrenoceptor antagonist. 2. SK&F 104856 as well as prazosin and SK&F 86466 reduced blood pressure in the anaesthetized normotensive dog. 3. SK&F 86466 and rauwolscine but not SK&F 104856 or prazosin, produced a marked increase in myocardial contractility which corresponds with their ability to block prejunctional alpha 2-adrenoceptors. 4. Intravenous or oral administration of SK&F 104856 resulted in dose-dependent antihypertensive responses in 1-kidney, 1-clip (1-K, 1-C) Goldblatt hypertensive dogs with baseline blood pressure of approximately 140 mmHg. At 0.1 and 1 mg kg-1, i.v., mean arterial blood pressure fell by 11 +/- 5 and 23 +/- 5 mmHg, respectively. At 3 and 10 mg kg-1, p.o., blood pressure fell by 9 +/- 3 and 22 +/- 5 mmHg, respectively. At 10 mg kg-1, p.o., the antihypertensive effect of SK&F 104856 was still evident at 4 h. 5. The data indicate that SK&F 104856 shows selectivity in vivo for postjunctional versus prejunctional alpha-adrenoceptors and is a potent and long-acting antihypertensive agent in 1-K, 1-C Goldblatt hypertensive dogs.

MeSH terms

  • Adrenergic alpha-Antagonists / pharmacology
  • Animals
  • Benzazepines / administration & dosage
  • Benzazepines / pharmacology*
  • Blood Pressure / drug effects
  • Cardiovascular Physiological Phenomena
  • Cardiovascular System / drug effects*
  • Dogs
  • Female
  • Heart Rate / drug effects
  • Hypertension, Renovascular / drug therapy*
  • Hypertension, Renovascular / physiopathology
  • Male
  • Myocardial Contraction / drug effects
  • Prazosin / pharmacology
  • Yohimbine / pharmacology

Substances

  • Adrenergic alpha-Antagonists
  • Benzazepines
  • SK&F 104856
  • Yohimbine
  • Prazosin
  • benalfocin