Ivermectin Interactions with Benzodiazepine Receptors in Rat Cortex and Cerebellum In Vitro

1984 ◽  
Vol 42 (3) ◽  
pp. 745-753 ◽  
Author(s):  
Michael Williams ◽  
Edwin A. Risley
Keyword(s):  
Benzodiazepine Receptors ◽  
Rat Cortex

SPECT Quantification of [123I]Iomazenil Binding to Benzodiazepine Receptors in Nonhuman Primates: II. Equilibrium Analysis of Constant Infusion Experiments and Correlation with in vitro Parameters

1994 ◽  
Vol 14 (3) ◽  
pp. 453-465 ◽  
Author(s):  
Marc Laruelle ◽  
Anissa Abi-Dargham ◽  
Mohammed S. AI-Tikriti ◽  
Ronald M. Baldwin ◽  
Yolanda Zea-Ponce ◽  
...  
Keyword(s):  
Specific Activity ◽  
Single Photon ◽  
Benzodiazepine Receptors ◽  
Photon Emission ◽  
Benzodiazepine Receptor ◽  
Equilibrium Analysis ◽  
Constant Infusion ◽  
Scatchard Analysis

In vivo benzodiazepine receptor equilibrium dissociation constant, KD, and maximum number of binding sites, Bmax, were measured by single photon emission computerized tomography (SPECT) in three baboons. Animals were injected with a bolus followed by a constant i.v. infusion of the high affinity benzodiazepine ligand [123I]iomazenil. Plasma steady-state concentration and receptor–ligand equilibrium were reached within 2 and 3 h, respectively, and were sustained for the duration (4–9 h) of the experiments (n = 15). At the end of the experiments, a receptor saturating dose of flumazenil (0.2 mg/kg) was injected to measure nondisplaceable activity. Experiments were carried out at various levels of specific activity, and Scatchard analysis was performed for derivation of the KD (0.59 ± 0.09 n M) and Bmax (from 126 n M in the occipital region to 68 n M in the striatum). Two animals were killed and [125I]iomazenil Bmax and KD were measured at 22 and 37°C on occipital homogenate membranes. In vitro values of Bmax (114 ± 33 n M) and 37°C KD (0.66 ± 0.16 n M) were in good agreement with in vivo values measured by SPECT. This study demonstrates that SPECT can be used to quantify central neuroreceptors density and affinity.

Potential Psychotropic Activity of Phlebotropic Drugs: Weak Interactions with Brain Benzodiazepine Receptors

1994 ◽  
Vol 9 (1) ◽  
pp. 32-36 ◽  
Author(s):  
W. Blätter ◽  
P. Schoch
Keyword(s):  
Weak Interactions ◽  
Benzodiazepine Receptors ◽  
Positive Influence ◽  
Binding Activity ◽  
Psychotropic Activity ◽  
Venous Disease ◽  
Receptor Binding Activity ◽  
Psychometric Studies ◽  
Organic Disorder

Background: Epidemiological and psychometric studies have provided evidence that some symptoms of venous disease might reflect a psychosomatic rather than organic disorder. Traditionally, plant extracts are prescribed to alleviate such symptoms. Since benzodiazepines (BZ) and BZ-like compounds are present in various plants, we studied potential interactions of ‘phlebotropic’ drugs with BZ receptors. Methods: Six drug preparations used in phlebology and extracts of hop and valerian were tested for neuronal and mitochondrial BZ receptor binding activity in vitro. In addition, plasma samples of volunteers who ingested phlebotropic drugs for 3 weeks were assayed for the presence of BZ-like activity. Results: All phlebotropic drug preparations interacted weakly with central and/or peripheral BZ receptors in vitro. Their diazepam-equivalent concentrations were, however, too low to be of pharmacological relevance. No binding activity was recovered in the blood of volunteers pretreated with phlebotropic drugs. Conclusion: The positive influence of so-called ‘phlebotropic’ drugs on the subjective symptoms of venous disease is not mediated through BZ receptors.

Aging, diazepam exposure and benzodiazepine receptors in rat cortex

1983 ◽  
Vol 270 (2) ◽  
pp. 376-379 ◽  
Author(s):  
P.M. Reeves ◽  
M.P. Schweizer
Keyword(s):  
Benzodiazepine Receptors ◽  
Rat Cortex

scholarly journals Immunomodulating effects of tofizopam (Grandaxin®) and diazepamin vitro

2002 ◽  
Vol 11 (1) ◽  
pp. 53-59 ◽  
Author(s):  
Sergey V. Kalashnikov ◽  
Elena A. Kalashnikova ◽  
Svetlana N. Kokarovtseva
Keyword(s):  
Lymphocyte Proliferation ◽  
Proliferative Response ◽  
Benzodiazepine Receptors ◽  
Interleukin 2 ◽  
Immune Functions ◽  
Peripheral Blood Mononuclear ◽  
Tnf Α ◽  
High Doses ◽  
Factor Α

Benzodiazepines (BDZs) are known to act not only in the central nervous system, but on peripheral cells and tissues binding to the peripheral-type benzodiazepine receptors. In the present study, the influence of two different BDZs (diazepam (Dz) and tofizopam (Tof)) on several immune functions has been examinedin vitro. Some differences between Dz and Tof in their effects on human lymphocyte proliferative response, changes in glucocorticoid-induced suppression of cell proliferation and influence on cytokine production (tumor necrosis factor-α (TNF-α) and interleukin-2 (IL-2)) have been determined. Dz suppressed mitogen-induced peripheral blood mononuclear cell (PBMC) proliferation, enhanced dexamethasone-induced inhibition of PBMC proliferative response, and suppressed lymphocyte production of TNF-α and IL-2. Tof usually enhanced PBMC proliferation and IL-2 production in low and moderate doses, but in high doses it suppressed both. Tof in all investigated doses enhanced dexamethasone-induced suppression of lymphocyte proliferation and depressed TNF-α production. Thus, both Dz and Tof are shown to have immunomodulating effectsin vitro. Tof, opposite to Dz even in the therapeutic doses, is able to enhancein vitromitogen-induced lymphocyte proliferation and IL-2 production.

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