3H-flunitrazepam binding to bovine retina and the effect of GABA thereon

John W. Regan; William R. Roeske; Henry I. Yamamura

doi:10.1016/0028-3908(80)90195-1

³H-flunitrazepam binding to bovine retina and the effect of GABA thereon

John W. Regan
, William R. Roeske
, Henry I. Yamamura

Research output: Contribution to journal › Article › peer-review

17 Scopus citations

Abstract

Bovine retinae were examined for their ability to bind ³H-flunitrazepam. Whole retinal homogenates revealed specific, high affinity, and saturable ³H-flunitrazepam binding (K_d, 1.1 nM; B_max, 19.5 fmoles/mg tissue). In washed membrane preparations, 10 μM GABA caused a dramatic decrease in the K_d (42 percent). The rank order of potency for the inhibition of ³H-flunitrazepam binding by different benzodiazepines was: clonazepam > clobazam ≫ Ro 5-4864. These results are supportive for the presence of benzodiazepine receptors in the bovine retina and indicate a likeness with the previously described benzodiazepine receptors of mammalian brain.

Original language	English (US)
Pages (from-to)	413-414
Number of pages	2
Journal	Neuropharmacology
Volume	19
Issue number	4
DOIs	https://doi.org/10.1016/0028-3908(80)90195-1
State	Published - Apr 1980

ASJC Scopus subject areas

Pharmacology
Cellular and Molecular Neuroscience

Access to Document

10.1016/0028-3908(80)90195-1

Cite this

@article{32844553c9fc4b46bb9b66557771ed08,

title = "3H-flunitrazepam binding to bovine retina and the effect of GABA thereon",

abstract = "Bovine retinae were examined for their ability to bind 3H-flunitrazepam. Whole retinal homogenates revealed specific, high affinity, and saturable 3H-flunitrazepam binding (Kd, 1.1 nM; Bmax, 19.5 fmoles/mg tissue). In washed membrane preparations, 10 μM GABA caused a dramatic decrease in the Kd (42 percent). The rank order of potency for the inhibition of 3H-flunitrazepam binding by different benzodiazepines was: clonazepam > clobazam ≫ Ro 5-4864. These results are supportive for the presence of benzodiazepine receptors in the bovine retina and indicate a likeness with the previously described benzodiazepine receptors of mammalian brain.",

author = "Regan, \{John W.\} and Roeske, \{William R.\} and Yamamura, \{Henry I.\}",

note = "Funding Information: Acknowledgements Henry I. Yamamura is a recipient of a United States Public Health Service Research Scientist Development Award, Type-II (MH-00095) from the National Tnstitutes of Mental Health. Portions of this research were supported by United States Public Health Service Grants MH-27257, MH-30626, and Program Project Grant HL-20984. We would like to thank Hoffman-LaRoche, Inc. for the clonazepam and the Ro S-4864. We would also like to thank Ms. Carol Corelis for secretarial assistance in typing of this manuscript. Portions of this work were presented at the Symposium on the Mechanism of Action of the Bensodiazepines. (August 27, 1979, A.S.P.E.T. meeting).",

year = "1980",

month = apr,

doi = "10.1016/0028-3908(80)90195-1",

language = "English (US)",

volume = "19",

pages = "413--414",

journal = "Neuropharmacology",

issn = "0028-3908",

publisher = "Elsevier Ltd",

number = "4",

}

TY - JOUR

T1 - 3H-flunitrazepam binding to bovine retina and the effect of GABA thereon

AU - Regan, John W.

AU - Roeske, William R.

AU - Yamamura, Henry I.

N1 - Funding Information: Acknowledgements Henry I. Yamamura is a recipient of a United States Public Health Service Research Scientist Development Award, Type-II (MH-00095) from the National Tnstitutes of Mental Health. Portions of this research were supported by United States Public Health Service Grants MH-27257, MH-30626, and Program Project Grant HL-20984. We would like to thank Hoffman-LaRoche, Inc. for the clonazepam and the Ro S-4864. We would also like to thank Ms. Carol Corelis for secretarial assistance in typing of this manuscript. Portions of this work were presented at the Symposium on the Mechanism of Action of the Bensodiazepines. (August 27, 1979, A.S.P.E.T. meeting).

PY - 1980/4

Y1 - 1980/4

N2 - Bovine retinae were examined for their ability to bind 3H-flunitrazepam. Whole retinal homogenates revealed specific, high affinity, and saturable 3H-flunitrazepam binding (Kd, 1.1 nM; Bmax, 19.5 fmoles/mg tissue). In washed membrane preparations, 10 μM GABA caused a dramatic decrease in the Kd (42 percent). The rank order of potency for the inhibition of 3H-flunitrazepam binding by different benzodiazepines was: clonazepam > clobazam ≫ Ro 5-4864. These results are supportive for the presence of benzodiazepine receptors in the bovine retina and indicate a likeness with the previously described benzodiazepine receptors of mammalian brain.

AB - Bovine retinae were examined for their ability to bind 3H-flunitrazepam. Whole retinal homogenates revealed specific, high affinity, and saturable 3H-flunitrazepam binding (Kd, 1.1 nM; Bmax, 19.5 fmoles/mg tissue). In washed membrane preparations, 10 μM GABA caused a dramatic decrease in the Kd (42 percent). The rank order of potency for the inhibition of 3H-flunitrazepam binding by different benzodiazepines was: clonazepam > clobazam ≫ Ro 5-4864. These results are supportive for the presence of benzodiazepine receptors in the bovine retina and indicate a likeness with the previously described benzodiazepine receptors of mammalian brain.

UR - https://www.scopus.com/pages/publications/0018909017

UR - https://www.scopus.com/pages/publications/0018909017#tab=citedBy

U2 - 10.1016/0028-3908(80)90195-1

DO - 10.1016/0028-3908(80)90195-1

M3 - Article

C2 - 6104311

AN - SCOPUS:0018909017

SN - 0028-3908

VL - 19

SP - 413

EP - 414

JO - Neuropharmacology

JF - Neuropharmacology

IS - 4

ER -

³H-flunitrazepam binding to bovine retina and the effect of GABA thereon

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this