[3H]Thienyl-phencyclidine ([3H]TCP) binds to two different sites in rat brain. Localization by autoradiographic and biochemical techniques

Vignon, Jacques; Privat, Alain; Chaudieu, Isabelle; Thierry, Alain R.; Kamenka, Jean-Marc; Chicheportiche, Robert

doi:10.1016/0006-8993(86)90294-5

Cited by 114 publications

(47 citation statements)

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“…In conclusion, this in vivo study confirms our previous in vitro studies Vignon et al, 1986Vignon et al, , 1989. It also supports the conclusion that 3H-TCP binding sites in the cerebrum and the cerebellum are different entities or, at least, are NMDNPCP receptors with different pharmacological properties.…”

Section: Discussionsupporting

confidence: 90%

“…This difference may reflect some regional differences in the drug pharmacokinetics. The level of binding in the cerebellum, however, is well correlated with our previous studies, where we have reported a high density of low affinity 'H-TCP binding sites (Vignon et al, 1986) and only a very small amount of high affinity 3H-TCP binding sites (Chicheportichc ct al., 1988;Viu mon et al, 1989). This last result was in agreement with the low level of 3H-TCP or 'H-glutamate binding generaly described by other groups in autoradiographic studies Maragos et al, 1988).…”

Section: Discussionsupporting

confidence: 89%

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In vivo labeling of phencyclidine (PCP) receptors with ³H‐TCP in the mouse brain

Maurice

Vignon

1990

J of Neuroscience Research

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The phencyclidine (PCP) derivative N-[1-(2-thienyl)cyclohexyl]-piperidine (3H-TCP) was used to label in vivo the N-methyl-D-aspartate (NMDA) receptor-associated ionic channel in the mouse brain. After the injection of a tracer dose of 3H-TCP, a spread labeling throughout the brain was observed, but was the highest in the cerebellum. Preadministration of unlabeled TCP (30 mg/kg) resulted in a 90% reduction of 3H-TCP binding. PCP, TCP, MK-801, dexoxadrol, ketamine, and SKF 10,047 isomers dose-dependently prevented the in vivo 3H-TCP binding. ID50 determined in the cerebrum and the cerebellum were respectively correlated with K0.5 for 3H TCP high (rat cortex) and low affinity (rat cerebellum) sites in vitro. The pharmacological specificity of the 3H-TCP binding site in the cerebellum was significantly different from that in the cerebrum. ID50 values were generally higher than in the cerebrum and, particularly, MK-801, the most potent drug in the cerebrum, was without significant effect in the cerebellum, at any time and at doses as high as 30 mg/kg. N-[1-(2-benzo(b) thiophenyl)cyclohexyl]piperidine (BTCP), desipramine, and atropine showed a more efficient prevention of 3H-TCP binding in the cerebellum than in the cerebrum. The prevention of the binding by TCP or PCP, at doses close to their ID50 values, was rapid and then decreased slowly. The effect of MK-801 was long-lasting. This study confirm previous in vitro studies: 3H-TCP is an efficient tool for the labeling of the NMDA receptor-associated ionic channel.(ABSTRACT TRUNCATED AT 250 WORDS)

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Section: Discussionsupporting

confidence: 90%

Section: Discussionsupporting

confidence: 89%

In vivo labeling of phencyclidine (PCP) receptors with ³H‐TCP in the mouse brain

Maurice

Vignon

1990

J of Neuroscience Research

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“…Interestingly, cerebellar NMDA receptors, which are unique in their low affinity for thienylphencyclidine at the NMDA ion channel (22), are also anomalous in being relatively insensitive to both agonists and antagonists (Fig. 2) …”

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confidence: 99%

Two classes of N-methyl-D-aspartate recognition sites: differential distribution and differential regulation by glycine.

Monaghan

Olverman

Nguyen

et al. 1988

Proc. Natl. Acad. Sci. U.S.A.

398

111

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The N-methyl-D-aspartate (NMDA) receptor, a subtype of excitatory amino acid receptor, mediates synaptic responses in many regions of the central nervous system. This receptor plays a critical role in the mechanisms of both synaptic plasticity and excitotoxicity. Although these receptors were generally thought to be a single homogeneous receptor population, we report observations indicating that two anatomically distinct forms of the NMDA-receptor complex exist. buffer, pH 7.0, preincubated at 30°C for 10 min, and then incubated for 10 min in ice-cold buffer containing 100 nM L-[3H]glutamate. NMDA receptors were selectively labeled by the inclusion of 100 ,uM 4-acetamido-4'-isothiocyanoatostilbene-2,2'-disulfonic acid, 5 ,uM amino-3-hydroxy-5-methylisoxazole-4-propionic acid, and 1 ,M kainic acid, which displace all detectable non-NMDA-receptor binding. Under these conditions the specific binding is fully displaced by NMDA agonists and antagonists at concentrations appropriate for NMDA receptors (12)(13)(14)(15)(16)(17)(18).Sections were then rinsed for 30 s, air dried, and placed against tritium-sensitive film along with tritium standards. Tissue sections in the experiments described in Fig. 2 9836The publication costs of this article were defrayed in part by page charge payment. This article must therefore be hereby marked "advertisement" in accordance with 18 U.S.C. §1734 solely to indicate this fact.

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“…In vitro pharmacology: binding assay. The binding assay using 3 H-TCP as a ligand and rat cerebral cortex as a receptor/site source was adapted from the procedure described by Vignon et al [37] and was performed by Cerep, an independent contract laboratory (Cerep, Bois l'Evêque, France), using 5 nM tritiated ligand and a 60 min incubation at 22 C, in the absence or in the presence of various concentrations of the selected benzamidine (EBAB). The analysis and expression of the binding assay results were as follows.…”

Section: Focal Intracerebral Injection Of Ibotenatementioning

confidence: 99%

1,2-Ethane bis-1-amino-4-benzamidine is active against several brain insult and seizure challenges through anti-NMDA mechanisms targeting the 3H-TCP binding site and antioxidant action

Vamecq

Maurois

Pagès

et al. 2010

European Journal of Medicinal Chemistry

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[3H]Thienyl-phencyclidine ([3H]TCP) binds to two different sites in rat brain. Localization by autoradiographic and biochemical techniques

Cited by 114 publications

References 20 publications

In vivo labeling of phencyclidine (PCP) receptors with ³H‐TCP in the mouse brain

In vivo labeling of phencyclidine (PCP) receptors with ³H‐TCP in the mouse brain

Two classes of N-methyl-D-aspartate recognition sites: differential distribution and differential regulation by glycine.

1,2-Ethane bis-1-amino-4-benzamidine is active against several brain insult and seizure challenges through anti-NMDA mechanisms targeting the 3H-TCP binding site and antioxidant action

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[3H]Thienyl-phencyclidine ([3H]TCP) binds to two different sites in rat brain. Localization by autoradiographic and biochemical techniques

Cited by 114 publications

References 20 publications

In vivo labeling of phencyclidine (PCP) receptors with 3H‐TCP in the mouse brain

In vivo labeling of phencyclidine (PCP) receptors with 3H‐TCP in the mouse brain

Two classes of N-methyl-D-aspartate recognition sites: differential distribution and differential regulation by glycine.

1,2-Ethane bis-1-amino-4-benzamidine is active against several brain insult and seizure challenges through anti-NMDA mechanisms targeting the 3H-TCP binding site and antioxidant action

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In vivo labeling of phencyclidine (PCP) receptors with ³H‐TCP in the mouse brain

In vivo labeling of phencyclidine (PCP) receptors with ³H‐TCP in the mouse brain