GABA and benzodiazepine binding sites in spontaneously hypertensive rat

Rajee Thyagarajan; Tim Brennan; Maharaj K. Ticku

doi:10.1016/0014-2999(83)90130-9

GABA and benzodiazepine binding sites in spontaneously hypertensive rat

Rajee Thyagarajan, Tim Brennan, Maharaj K. Ticku

Department of Pharmacology

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

17 Scopus citations

Abstract

The binding of GABA to its central receptor sites and of benzodiazepines to central and peripheral types of binding sites was compared in age-matched spontaneously hypertensive rat (SHR) and normotensive (WKY) rat. The K_D and B_max values of GABA agonist binding were not significantly different between SHR and WKY rat in the forebrain, cerebellum or pons-medulla. The binding of [³H]flunitrazepam to central types of binding sites was also not different in 12 week-old SHR and WKY rat. However, the binding of [³H]flunitrazepam and [³H]RO5-4864 was significantly lower in the SHR kidney, as compared to WKY rat kidney. This decrease was due to a lower B_max in SHR kidney. In contrast, the binding of these radioligands in the hearts of the two strains was not different. These results indicate that the SHR has lower peripheral benzodiazepine binding sites in the kidney as compared to age-matched normotensive WKY rat kidney.

Original language	English (US)
Pages (from-to)	127-136
Number of pages	10
Journal	European Journal of Pharmacology
Volume	93
Issue number	3-4
DOIs	https://doi.org/10.1016/0014-2999(83)90130-9
State	Published - Sep 30 1983

Keywords

Brain
Central benzodiazepine sites
GABA receptors
Heart
Kidney
Peripheral benzodiazepine sites
Spontaneously hypertensive rats

ASJC Scopus subject areas

Pharmacology

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10.1016/0014-2999(83)90130-9

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title = "GABA and benzodiazepine binding sites in spontaneously hypertensive rat",

abstract = "The binding of GABA to its central receptor sites and of benzodiazepines to central and peripheral types of binding sites was compared in age-matched spontaneously hypertensive rat (SHR) and normotensive (WKY) rat. The KD and Bmax values of GABA agonist binding were not significantly different between SHR and WKY rat in the forebrain, cerebellum or pons-medulla. The binding of [3H]flunitrazepam to central types of binding sites was also not different in 12 week-old SHR and WKY rat. However, the binding of [3H]flunitrazepam and [3H]RO5-4864 was significantly lower in the SHR kidney, as compared to WKY rat kidney. This decrease was due to a lower Bmax in SHR kidney. In contrast, the binding of these radioligands in the hearts of the two strains was not different. These results indicate that the SHR has lower peripheral benzodiazepine binding sites in the kidney as compared to age-matched normotensive WKY rat kidney.",

keywords = "Brain, Central benzodiazepine sites, GABA receptors, Heart, Kidney, Peripheral benzodiazepine sites, Spontaneously hypertensive rats",

author = "Rajee Thyagarajan and Tim Brennan and Ticku, {Maharaj K.}",

note = "Funding Information: This study was supported by funds from the American Heart Association (Texas Affiliate).",

year = "1983",

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doi = "10.1016/0014-2999(83)90130-9",

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T1 - GABA and benzodiazepine binding sites in spontaneously hypertensive rat

AU - Thyagarajan, Rajee

AU - Brennan, Tim

AU - Ticku, Maharaj K.

N1 - Funding Information: This study was supported by funds from the American Heart Association (Texas Affiliate).

PY - 1983/9/30

Y1 - 1983/9/30

N2 - The binding of GABA to its central receptor sites and of benzodiazepines to central and peripheral types of binding sites was compared in age-matched spontaneously hypertensive rat (SHR) and normotensive (WKY) rat. The KD and Bmax values of GABA agonist binding were not significantly different between SHR and WKY rat in the forebrain, cerebellum or pons-medulla. The binding of [3H]flunitrazepam to central types of binding sites was also not different in 12 week-old SHR and WKY rat. However, the binding of [3H]flunitrazepam and [3H]RO5-4864 was significantly lower in the SHR kidney, as compared to WKY rat kidney. This decrease was due to a lower Bmax in SHR kidney. In contrast, the binding of these radioligands in the hearts of the two strains was not different. These results indicate that the SHR has lower peripheral benzodiazepine binding sites in the kidney as compared to age-matched normotensive WKY rat kidney.

AB - The binding of GABA to its central receptor sites and of benzodiazepines to central and peripheral types of binding sites was compared in age-matched spontaneously hypertensive rat (SHR) and normotensive (WKY) rat. The KD and Bmax values of GABA agonist binding were not significantly different between SHR and WKY rat in the forebrain, cerebellum or pons-medulla. The binding of [3H]flunitrazepam to central types of binding sites was also not different in 12 week-old SHR and WKY rat. However, the binding of [3H]flunitrazepam and [3H]RO5-4864 was significantly lower in the SHR kidney, as compared to WKY rat kidney. This decrease was due to a lower Bmax in SHR kidney. In contrast, the binding of these radioligands in the hearts of the two strains was not different. These results indicate that the SHR has lower peripheral benzodiazepine binding sites in the kidney as compared to age-matched normotensive WKY rat kidney.

KW - Brain

KW - Central benzodiazepine sites

KW - GABA receptors

KW - Heart

KW - Kidney

KW - Peripheral benzodiazepine sites

KW - Spontaneously hypertensive rats

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ER -

GABA and benzodiazepine binding sites in spontaneously hypertensive rat

Abstract

Keywords

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