These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: [3H]methylcarbamylcholine, a new radioligand for studying brain nicotinic receptors.
    Author: Abood LG, Grassi S.
    Journal: Biochem Pharmacol; 1986 Dec 01; 35(23):4199-202. PubMed ID: 3790148.
    Abstract:
    A new radioligand, [3H]methylcarbamylcholine, has been developed for the study of the nicotinic cholinergic and nicotine-like binding sites in rat brain membranes. A Scatchard analysis with the radioligand yielded a Kd of 1.1 X 10(-9) M and a Bmax of 4.0 X 10(-14) moles/mg protein which compares with a lower affinity site for (-)-[3H]nicotine having a Kd of 3 X 10(-9) M and a Bmax of 2 X 10(-14) moles/mg. Comparable values for the Kd were obtained from a Hill plot and from calculations based on rate constants for association and dissociation. A comparison of the binding affinities of various nicotine analogues, nicotinic cholinergic agents, and other neurotropic agents revealed a close similarity between the two radioligands, with the exception that quaternization of nicotine or carbamate esters increased affinity by at least an order of magnitude with [3H]methylcarbamylcholine and resulted in a comparable decrease in affinity with [3H]nicotine as the ligand. The binding of [3H]methylcarbamylcholine, like [3H]nicotine, was not displaceable by muscarinic cholinergic antagonists. It was concluded that, although [3H]methylcarbamylcholine and [3H]nicotine bind to a common receptor in brain, the functional and chemical characteristics of the receptor(s) differ in some respects from peripheral nicotinic cholinergic receptors.
    [Abstract] [Full Text] [Related] [New Search]