INT18088

Context Info Confidence 0.48 First Reported 1985 Last Reported 2010 Negated 1 Speculated 0 Reported most in Abstract Documents 26 Total Number 26 Disease Relevance 9.12 Pain Relevance 10.20

mitochondrion (Tspo) aging (Tspo) response to stress (Tspo)

Anatomy Link Frequency brain 4 striatum 1 spleen 1 dorsal horn 1 BZR 1 Tspo (Rattus norvegicus)

Pain Link Frequency Relevance Heat agonist 119 100.00 gABA 33 100.00 halothane 20 100.00 narcan 13 100.00 alcohol 209 99.92 Endogenous opioid 6 99.92 Cholecystokinin 84 99.90 dorsal root ganglion 12 99.60 Sciatic nerve 8 99.20 anesthesia 26 98.98

Disease Link Frequency Relevance Heat Ganglion Cysts 12 99.60 Anxiety Disorder 214 99.40 Injury 48 99.20 Sleep Disorders 50 98.26 Urological Neuroanatomy 52 97.64 Stress 213 97.60 Suicidal Behaviour 12 97.32 Herpes Simplex Encephalitis 246 93.32 Toxicity 6 92.64 Poisoning 3 92.08

Sentences Mentioned In

Key:

Protein

Mutation

Event

Anatomy

Negation

Speculation

Pain term

Disease term

The absence of an increase in the MAC of halothane in the presence of flumazenil suggests that halothane does not interact with the benzodiazepine receptor, directly or indirectly, to produce its anesthetic action.

benzodiazepine receptor Neg (not) Binding (interact) of associated with halothane

1) Confidence 0.48 Published 1989 Journal Anesthesiology Section Abstract Doc Link 2539028 Disease Relevance 0 Pain Relevance 0.67

This raises the possibility that the presence of a social companion precludes the release of an endogenous anxiogen that binds to the benzodiazepine receptor.

benzodiazepine receptor Binding (binds) of

2) Confidence 0.48 Published 1990 Journal Dev Psychobiol Section Abstract Doc Link 1964442 Disease Relevance 0 Pain Relevance 0.48

In contrast to [11C]-(R)-PK11195, [11C]-DPA-713 is even able to show specific binding to the low basal expression levels of TSPO in control rats.

TSPO Binding (binding) of

3) Confidence 0.46 Published 2009 Journal Mol Imaging Biol Section Body Doc Link PMC2763079 Disease Relevance 0.15 Pain Relevance 0

This higher uptake was shown to be selective TSPO binding.

TSPO Binding (binding) of

4) Confidence 0.46 Published 2009 Journal Mol Imaging Biol Section Body Doc Link PMC2763079 Disease Relevance 0.24 Pain Relevance 0.26

Pyrazolopyrimidines display high affinity for the TSPO and two compounds from this class have already been radiolabeled for use in PET.

TSPO Binding (affinity) of associated with positron emission tomography

5) Confidence 0.46 Published 2009 Journal Mol Imaging Biol Section Body Doc Link PMC2763079 Disease Relevance 0.45 Pain Relevance 0.38

However, FG 7142 is less potent than RO 15-4513 and has less affinity for the benzodiazepine receptor (BZR).

benzodiazepine receptor Binding (affinity) of in BZR

6) Confidence 0.42 Published 1990 Journal Pharmacol. Biochem. Behav. Section Abstract Doc Link 2111915 Disease Relevance 0 Pain Relevance 0.43

The effects of a benzodiazepine receptor agonist and an antagonist on the MAC of halothane required to achieve anesthesia were evaluated to explore the possible functional interaction between halothane and the benzodiazepine receptor.

benzodiazepine receptor Binding (interaction) of associated with anesthesia, antagonist, agonist and halothane

7) Confidence 0.37 Published 1989 Journal Anesthesiology Section Abstract Doc Link 2539028 Disease Relevance 0 Pain Relevance 0.70

In naïve animals, PBR mRNA, protein expression and ligand binding are undetectable in the DRG.

PBR mRNA Binding (binding) of in DRG associated with dorsal root ganglion

8) Confidence 0.36 Published 2004 Journal Eur. J. Neurosci. Section Abstract Doc Link 15255978 Disease Relevance 0.79 Pain Relevance 0.40

The pyrazolopyrimidines DPA-713 and DPA-714 have higher affinity for the TSPO in vitro (Ki?

TSPO Binding (affinity) of

9) Confidence 0.36 Published 2009 Journal Mol Imaging Biol Section Body Doc Link PMC2763079 Disease Relevance 0.41 Pain Relevance 0.32

It was concluded that [11C]-DPA-713 is a specific ligand for the TSPO and that it may be useful for studying changes in the density of TSPO binding sites.

TSPO Binding (ligand) of

10) Confidence 0.36 Published 2009 Journal Mol Imaging Biol Section Body Doc Link PMC2763079 Disease Relevance 0.31 Pain Relevance 0.27

The apparent discrepancy between the results of our study and those of the previous studies in the striatum lesion model might be due to differences in the affinity state of the receptor between both animal models. [18F]-DPA-714 is an agonist of the TSPO and an agonist usually binds only to the high affinity state of the receptor.

TSPO Binding (binds) of in striatum associated with agonist

11) Confidence 0.34 Published 2009 Journal Mol Imaging Biol Section Body Doc Link PMC2763079 Disease Relevance 0.22 Pain Relevance 0.10

PBR ligand binding also appears after injury in the superficial dorsal horn of the spinal cord.

PBR Binding (binding) of in dorsal horn associated with injury, dorsal horn and spinal cord

12) Confidence 0.31 Published 2004 Journal Eur. J. Neurosci. Section Abstract Doc Link 15255978 Disease Relevance 0.88 Pain Relevance 0.48

SSR180575 shows high affinity (IC(50), 2.5-3.5 nM) and selectivity for the rat and human PBR and potently inhibits the in vivo binding of [(3)H]alpidem to PBR in the rat brain and spleen after oral or i.p. administration (ID(50), 0.1-0.3 mg/kg).

PBR Binding (binding) of in brain

13) Confidence 0.31 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12023539 Disease Relevance 0.05 Pain Relevance 0.05

These include mediation via the GABA-benzodiazepine-ionophore complex, endogenous opioids, the hypothalamo-pituitary-adrenocortical axis and the noradrenergic system.

GABA-benzodiazepine-ionophore Binding (complex) of in pituitary associated with gaba and endogenous opioid

14) Confidence 0.31 Published 1990 Journal Alcohol Alcohol. Section Abstract Doc Link 1973897 Disease Relevance 0.61 Pain Relevance 0.37

Interactions between LY354740, a group II metabotropic agonist and the GABA(A)-benzodiazepine receptor complex in the rat elevated plus-maze.

benzodiazepine receptor Binding (Interactions) of associated with gaba, narcan and agonist

15) Confidence 0.27 Published 2001 Journal J. Psychopharmacol. (Oxford) Section Title Doc Link 11448091 Disease Relevance 0.38 Pain Relevance 0.64

Both constituents interact with a mitochondrial protein, the adenine nucleotide translocator, responsible for the ATP/ADP antiport and involved in mitochondrial membrane permeabilization.

translocator Binding (interact) of

16) Confidence 0.25 Published 2005 Journal J Ethnopharmacol Section Abstract Doc Link 15707749 Disease Relevance 1.09 Pain Relevance 0.17

These results indicate that the ability of alcohol to potentiate benzodiazepine-induced sedation is not simply an additive effect but may be related to the facilitation by alcohol of benzodiazepine receptor binding.

benzodiazepine receptor Binding (binding) of associated with sleep disorders and alcohol

17) Confidence 0.20 Published 1985 Journal Anesth. Analg. Section Abstract Doc Link 2857540 Disease Relevance 0.35 Pain Relevance 0.78

In contrast, DAA1097 and DAA1106 did not inhibit [3H]-flunitrazepam, the central benzodiazepine receptor (CBR) ligand, binding to membranes of rat whole brain (IC50>10,000nM).

central benzodiazepine receptor Binding (binding) of in brain

18) Confidence 0.17 Published 1999 Journal Life Sci. Section Abstract Doc Link 10321725 Disease Relevance 0.17 Pain Relevance 0.28

Benzodiazepine receptor binding following chronic treatment with naloxone, morphine and met-enkephalin in normal rats.

Benzodiazepine receptor Binding (binding) of associated with narcan, enkephalin and morphine

19) Confidence 0.15 Published 1993 Journal Brain Res. Section Title Doc Link 8392430 Disease Relevance 0 Pain Relevance 1.08

SSR180575 shows high affinity (IC(50), 2.5-3.5 nM) and selectivity for the rat and human PBR and potently inhibits the in vivo binding of [(3)H]alpidem to PBR in the rat brain and spleen after oral or i.p. administration (ID(50), 0.1-0.3 mg/kg).

PBR Binding (binding) of in spleen

20) Confidence 0.11 Published 2002 Journal J. Pharmacol. Exp. Ther. Section Abstract Doc Link 12023539 Disease Relevance 0.05 Pain Relevance 0.05

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