Contractile responses of the human urinary bladder, renal pelvis and renal artery to endothelins and sarafotoxin S6b

Gen Pharmacol. 1990;21(2):247-9. doi: 10.1016/0306-3623(90)90909-6.

Abstract

1. Endothelin-1 (ET-1), endothelin-3 (ET-3) and sarafotoxin S6b (SRFTX) produced a concentration-dependent tonic contraction of the human isolated urinary bladder, renal pelvis and renal artery with threshold at nM concentration. 2. In the bladder, the following order of potency was found: ET-1 greater than SRFTX greater than ET-3. In the renal pelvis, all peptides displayed similar affinity but, at high concentrations the maximal response was highest for SRFTX followed by ET-1 and ET-3. In the renal artery ET-1 and SRFTX were about equipotent and equieffective while ET-3 produced only a slight and inconsistent (2 out of 5 cases) vasoconstrictor response. 3. As shown previously for the human bladder muscle, the response to ET-1 in the renal pelvis was nifedipine (1 microM)-resistant while a consistent fraction of the response was blocked by nifedipine in the human renal artery. 4. These findings indicate that peptides of the endothelin family exert a potent contractile effect on various human smooth muscles. Participation of dihydropyridine- and voltage-sensitive calcium channels in the contractile response produced by these peptides may vary from one organ to another.

MeSH terms

  • Endothelins
  • Humans
  • In Vitro Techniques
  • Muscle, Smooth / drug effects*
  • Muscle, Smooth, Vascular / drug effects*
  • Nifedipine / pharmacology
  • Peptides / pharmacology*
  • Renal Artery / drug effects
  • Renal Circulation / drug effects
  • Urinary Bladder / drug effects
  • Viper Venoms / pharmacology*

Substances

  • Endothelins
  • Peptides
  • Viper Venoms
  • sarafotoxins s6
  • Nifedipine