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THE BENZODIAZEPINE RECEPTOR. A SUMMARY. Walter E. Müller Pharmakologisches Institut der Universität Mainz, Obere Zahl- bacher Straße 67, D-6500 Mainz, Federal Republic of Germany The Search for the Molecular Mechanism of Action of the Benzodiazepines. Although the benzodiazepines are the most frequently pre- scribed group of drugs today the molecular mechanism, respon- sible for the pharmacological activity of the benzodiazepines, remained unclear for a long period of time. The concept which found increasing experimental support during the last years was

Chemical Modification of Benzodiazepine Receptors of Cortical P2 Membranes Le Fei, Zhang Zhao-geng and Zhou Ting-chung (T.C. Chou) This paper is dedicated to Fritz Lipmann's Memorial Symposium. As you know, Fritz wrote a wonderful book "Wanderings of a Biochemist" and I had translated it into Chinese with his permission. I sent him a Chinese version of his book. Fritz answered me immediately with the following words: "This was one of the greatest pleasures of my life to see my book translated into Chinese, and as you say will be read by millions. I am

Radiochim. Acta 88, 2292232 (2000)  by Oldenbourg Wissenschaftsverlag, München Synthesis of substituted [123I]imidazo[1,2-a]pyridines as potential probes for the study of the peripheral benzodiazepine receptors using SPECT† By Andrew Katsifis*, Filomena Mattner, Branko Dikic and Vahan Papazian Radiopharmaceuticals Division R& D, ANSTO, PMB 1 Menai, NSW 2234, Australia (Received November 8, 1999; accepted in revised form January 14, 2000) Iodine2123 / Peripheral benzodiazepine receptors / Imidazo[1,2-a]pyridines / Iododestannylation / SPECT Summary. The imidazo[1

Radiochim. Acta 92, 305–309 (2004)  by Oldenbourg Wissenschaftsverlag, München Synthesis of [123I]iodine labelled imidazo[1,2-b] pyridazines as potential probes for the study of peripheral benzodiazepine receptors using SPECT By A. Katsifis1,∗, G. Barlin2, F. Mattner1 and B. Dikic1 1 Radiopharmaceuticals Division ANSTO, PMB 1 Menai, NSW 2234, Australia 2 Division of Neurosciences, John Curtin School of Medical Research, Australian National University, Canberra, Australia Dedicated to the memory of Prof. Dr. Dr. h.c. Gerhard L. Stöcklin (Received October 9, 2003

CHARACTERIZATION OF THE INTERACTION OF 3H-PROPYL-B-CARBOLINE- 3-CARBOXYLATE WITH THE BENZODIAZEPINE RECEPTOR IN THE BOVINE CENTRAL NERVOUS SYSTEM Klaus. J. Fehske and Walter E. Müller Pharmakologisches Institut der Universität Mainz, Obere Zahl- bacher Straße 67, D-6500 Mainz, Federal Republic of Germany- Introduction While the status of the B-carbolines as endogenous ligands of the benzodiazepine receptor is still unclear (see the chapter by W.E. Miiller in this volume) B-carbolines have become impor- tant experimental tools in another respect related to

mechanism of anxiolytic effect To investigate the serotonergic and GABAergic systems in the anxiolytic-like effect of HeMI, mice were pretreated with metergoline (4 mg/kg, i.p., 5-HT 1/2 receptor antagonist) [ 33 ] or flumazenil (benzodiazepine receptor antagonist) [ 33 ]. Fifteen minutes after, HeMI (12.50 mg/kg, p.o.; most effective dose) was administered. One hour post-treatment, the EPM test was carried out. Statistical analysis Data were analysed by Graphpad Prism version 6 software (Graphpad Inc., CA, USA) and values are expressed as mean±SEM (n=8). The statistical

describe a highly sensitive and non-invasive FCS assay to study in- teractions between the benzodiazepine receptor and the dye-labeled benzodiazepine, Ro7 – 1986/602, on the membranes of living cells. Results Ro-Alexa was obtained by labeling of Ro 7 – 1986/602 with the dye Alexa® Fluor 532 carboxylic acid succin- imidyl ester. The purity of the dye-labeled ligand was proven by HPLC to be >95%. Identity was confirmed by high-resolution mass spectrometry (Mr 940.5100 measured; 939.5093 calculated). The influence of the in- troduced dye on benzodiazepine functionality was

Papadopoulos, V. ( 2003 ). In vivo and in vitro peripheral-type benzodiazepine receptor polymerization: functional significance in drug ligand and cholesterol binding. Biochemistry 42 , 4506 –4519. Dombro , R.S., Bender, A.S., and Norenberg, M.D. ( 2000 ). Association between cell swelling and glycogen content in cultured astrocytes. Int. J. Dev. Neurosci. 18 , 161 –169. Fischer , R., Schliess, F., and Häussinger, D. ( 1997 ). Characterization of the hypo-osmolarity-induced Ca 2+ response in cultured rat astrocytes. Glia 20 , 51 –58. Flögel , U., Niendorf, T

management of patients with intractable epilepsy. 18 F- Flumazenil tracers for PET/CT of patients with epilepsy Gamma-aminobutyric acid (GABA) is the most important inhibitory neurotransmitter in the central nervous system. 40 - 43 Its main role consists of reducing neuronal excitability and regulating muscle tone. There are two types of GABA receptors: GABA A and GABA B ; benzodiazepine receptors are modulatory sites on GABA A receptors. Benzodiazepine distribution in the human brain includes the occipital cortex, temporal cortex, cerebellum, thalamus, and the pons

. Therefore, regula- tion of the permeability of both outer and inner mitochondrial membranes helps to induce neuroprotection. Through PTP control, mitochondria can to a large degree manage the intracellular calcium homeostasis, and thus con- trol the potent death cascade initiated by excess calcium. Here we summarize the evidence for the role of mitochondria in brain cell death. We describe the involvement of the 18- kDa translocator protein (TSPO; previously called peripheral benzodiazepine receptor), and of two new mitochondrial pro- teins, that is, 29,39-cyclic