Can I read Membrane‐Bound and solubilized brain 5HT~3~ receptors: Improved radioligand binding assays using bovine area postrema or rat cortex and the radioligands ^3^H‐Gr65630C, ^3^H‐BRl43694, and ^3^H‐LY278584 on EtoBox?

Membrane‐Bound and solubilized brain 5HT~3~ receptors: Improved radioligand binding assays using bovine area postrema or rat cortex and the radioligands ^3^H‐Gr65630C, ^3^H‐BRl43694, and ^3^H‐LY278584 by Keith Miller; Ellen Weisberg; Paul W. Fletcher; DR. Milt Teitler is a Neuroscience article available to read on EtoBox.

What is Membrane‐Bound and solubilized brain 5HT~3~ receptors: Improved radioligand binding assays using bovine area postrema or rat cortex and the radioligands ^3^H‐Gr65630C, ^3^H‐BRl43694, and ^3^H‐LY278584 about?

Bovine area postrema tissue was used as a convenient source of tissue for studies of brain 5HT3 receptors. 5HT3 receptor density was determined to be 97 5 5 fmoVmg and 124 k 10 fmoVmg of protein using the commercially available 5HT3 radioligands, 3H-GR65630 and 3H-BRL43694, respectively. The equilibrium dissociation constants (K,) for ,H-GR65630 and 3H-BRL43694 were 0.5 \* 0.1 nM and 1.7 \* 0.3 nM, respectively. The affinities of a series of drugs for the 5HT3 receptor using the two radioligands were essentially identical; the K, values and order of affinities of agonists and antagonists were very similar to data published in studies on radiolabeling of 5HT3 receptors in rat brain. 3H-LY278584 also labeled 5HT3 receptors in bovine area postrema homogenates with a K,, of 3.1 f 0.1 nM and a B,,, of 84 ? 6 fmol/mg. In rat cortical homogenates, 3H-LY278584 produced the most reliable specific signal of 72%, with a KD of 2.6 \* 0.3 nM and a B, , value of 10.5 ? 1 fmoVmg. At 1 1lM,~H-GR65630 or 3H-BRL43694 specific binding represented 28 and 50% of total radioligand binding, respectively. These data in bovine and rat brain tissues indicate that bovine area postrema can be used with 3H-GR6

Who reads Membrane‐Bound and solubilized brain 5HT~3~ receptors: Improved radioligand binding assays using bovine area postrema or rat cortex and the radioligands ^3^H‐Gr65630C, ^3^H‐BRl43694, and ^3^H‐LY278584?

Author

Keith Miller; Ellen Weisberg; Paul W. Fletcher; DR. Milt Teitler

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0887-4476)

Published

1992

Language

EN

Field

Neuroscience (Life Sciences)