PMID: 9650050Jul 3, 1998Paper

Binding of [3H]m-aminolevamisole to receptors in levamisole-susceptible and -resistant Haemonchus contortus

International Journal for Parasitology
N C SangsterL J Wiley

Abstract

M-aminolevamisole, a potent analogue of the commercial anthelmintic levamisole, was used to investigate ligand-binding properties of homogenates of larval and parasitic stages of the nematode parasite of sheep, Haemonchus contortus. Kinetics of the binding of [3H]m-aminolevamisole to homogenates was measured in a drug-susceptible isolate and compared with a levamisole-resistant isolate. Equilibrium binding studies and kinetic studies revealed a high affinity binding component with a KD of 3 nM. A low affinity component (KD = 2.4 microM) was also apparent in equilibrium studies. High affinity [3H]m-aminolevamisole binding was displaced in a concentration-dependent manner by levamisole analogues and cholinergic agonists. Compared with the susceptible isolate, binding in a levamisole-resistant isolate of the parasite, was quantitatively similar over a range of developmental stages and binding conditions. However, under the conditions of binding there was a reduced affinity (larger KD) and more binding sites (larger Bmax) at the low affinity site in the resistant compared with the susceptible isolate. It was concluded that the ligand was binding to acetylcholine receptor populations of the nematode and that resistance may be associ...Continue Reading

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Citations

Jun 13, 2001·International Journal for Parasitology·P Köhler
Feb 27, 1999·International Journal for Parasitology·N C Sangster
May 14, 1999·Parasitology Today·N C Sangster, J Gill
Aug 23, 2001·Veterinary Parasitology·R Prichard, A Tait
Dec 26, 2001·Veterinary Parasitology·M A TaylorK L Goodyear
Aug 24, 1999·Veterinary Parasitology·T G GearyD P Thompson
Nov 19, 2003·Current Opinion in Infectious Diseases·Ronald Kaminsky
Feb 5, 2021·Animals : an Open Access Journal From MDPI·Konstantinos V ArsenopoulosElias Papadopoulos
Apr 3, 2021·International Journal for Parasitology. Drugs and Drug Resistance·Paulius BaltrušisJohan Höglund
Sep 15, 2004·Trends in Parasitology·Adrian J WolstenholmeNicholas C Sangster

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