Muscarinic Cholinergic Binding in Rat Brain
AUTOR(ES)
Yamamura, Henry I.
RESUMO
Binding sites with high affinity and specificity for [3H]quinuclidinyl benzilate (QNB) are present in homogenates of rat brain. The characteristics of the binding sites resemble those of muscarinic cholinergic receptors. Specific binding is saturable with respect to [3H]QNB and tissue concentration and is time-, temperature-, and pH-dependent. The bimolecular rate of association (2.0 × 108 M-1 min-1) and dissociation (1.2 × 10-2 min-1) at 35° indicate a dissociation constant of 60 pM and a density of 65 pmol/g of brain. Muscarinic antagonists and agonists displace specific [3H]QNB binding, while nicotinic and non-cholinergic drugs possess little affinity for [3H]QNB-binding sites.
ACESSO AO ARTIGO
http://www.pubmedcentral.nih.gov/articlerender.fcgi?artid=388311Documentos Relacionados
- Muscarinic cholinergic receptors in murine lymphocytes: demonstration by direct binding.
- Quantitative in vivo receptor binding III: Tracer kinetic modeling of muscarinic cholinergic receptor binding.
- Reduction in muscarinic receptor binding in limbic areas of Alzheimer brain.
- Reciprocal modulation of agonist and antagonist binding to muscarinic cholinergic receptor by guanine nucleotide.
- M2 muscarinic receptor-mediated inhibition of the Ca2+ current in rat magnocellular cholinergic basal forebrain neurones.