Selective ETA receptor antagonism with BQ-123 is insufficient to inhibit angioplasty induced neointima formation in the rat.

Abstract

OBJECTIVE:

The aim was to assess whether or not the endothelin ETA receptor selective antagonist BQ-123 could inhibit neointima formation in vivo following balloon angioplasty.

METHODS:

The effect of either acute administration of BQ-123 (0.1 mg.kg-1.min-1 intra-arterial infusion for 1 h before and 1 h after angioplasty) or chronic administration (bolus intraperitoneal injection, 2.5 mg.kg-1 twice daily; continuous intraperitoneal infusion, 0.8 and 8 mg.kg-1.d-1) on neointima formation was examined in rats which had undergone left common carotid artery balloon angioplasty.

RESULTS:

Neither acute intra-arterial infusion nor either mode of chronic intraperitoneal administration of BQ-123 had a significant effect on the degree of neointima formation observed following balloon angioplasty.

CONCLUSIONS:

Neither acute nor chronic ETA receptor blockade is sufficient to inhibit angioplasty induced neointima formation in the rat. Since it was previously shown that the ETA/B antagonist SB 209670 was effective in this model, while the ETA selective antagonist BQ-123 is now found to be ineffective, the data implicate the ETB receptor subtype in the pathogenesis of neointima formation.

• Authors: S A Douglas, L M Vickery-Clark, C Louden, E H Ohlstein
• Journal: Cardiovascular research (Cardiovasc Res) Vol. 29 Issue 5 Pg. 641-6 (May 1995) ISSN: 0008-6363 [Print] England
• PMID: 7606751 (Publication Type: Journal Article)

Chemical References

• Endothelin Receptor Antagonists
• Peptides, Cyclic
• cyclo(Trp-Asp-Pro-Val-Leu)

Topics

• Angioplasty, Balloon
• Animals
• Carotid Stenosis (therapy)
• Endothelin Receptor Antagonists
• Infusions, Intra-Arterial
• Injections, Intraperitoneal
• Male
• Peptides, Cyclic (pharmacology)
• Rats
• Rats, Sprague-Dawley
• Recurrence
• Tunica Intima (drug effects)