Melanin affinity: a possible explanation of isoxsuprine retention in the horse

Abstract

Isoxsuprine is used in veterinary medicine as a vasodilating agent. The drug has been detected in the urine of horses up to 6 weeks after the cessation of administration, In the present study, the distribution pattern of H-3-isoxsuprine was investigated using whole body autoradiography in mice to find a possible site of retention, Melanin was the only place of retention identified. Additional in vitro studies showed an affinity of isoxsuprine to both melanin and keratin. The K-d values were 0.02 mmol/l and 1 mmol/l, and the B-max values were 0.2 mu mol/mg and 2 mu mol/mg, respectively. A low affinity site with approximately the same K-d and B-max as keratin was also detected for melanin, H-3-isoxsuprine was found to have affinity to pigmented horse skin after incubation in vitro and microautoradiography. We believe that affinity to melanin and possibly also to keratin can cause retention of the drug in the body and therefore explain the prolonged excretion of low levels of isoxsuprine in the horse.

Keywords

horse; isoxsuprine; melanin; distribution; mouse; autoradiography

Published in

Equine Veterinary Journal
2000, Volume: 32, number: 2, pages: 114-118 Publisher: EQUINE VETERINARY JOURNAL LTD

SLU Authors

• Törneke, Karolina

  • Department of Pharmacology and Toxicology, Swedish University of Agricultural Sciences
    

• Ingvast Larsson, Carina

  • Department of Pharmacology and Toxicology, Swedish University of Agricultural Sciences
    

• Appelgren, Lars-Erik

  • Department of Pharmacology and Toxicology, Swedish University of Agricultural Sciences
    

UKÄ Subject classification

Pathobiology


Publication identifier

DOI: https://doi.org/10.2746/042516400777591606

Permanent link to this page (URI)

https://res.slu.se/id/publ/97422