Results 21 to 30 of about 12,549 (250)

Realising the therapeutic potential of neuroactive steroid modulators of the GABA_A receptor [PDF]

, 2020
In the 1980s particular endogenous metabolites of progesterone and of deoxycorticosterone were revealed to be potent, efficacious, positive allosteric modulators (PAMs) of the GABAA receptor (GABAAR).
Belelli, Delia, Gee, Kelvin W., Hogenkamp, Derk, Lambert, Jeremy J.   +3 more
core   +1 more source

Neuroactive steroids in depression and anxiety disorders: Clinical studies [PDF]

, 2006
Certain neuroactive steroids modulate ligand-gated ion channels via non-genomic mechanisms. Especially 3 alpha-reduced pregnane steroids are potent positive allosteric modulators of the gamma-aminobutyric acid type A (GABA(A)) receptor.
Akwa Y, Baghai TC, Baker ER, Barrett-Connor E, Bicikova M, Bitran D, Bloch M, Brambilla F, Brambilla F, Brambilla F, Cornelius Schüle, Crawley JN, Dalton K, Daniela Eser, Dennerstein L, Dong E, Elena Romeo, Eser D, Evans RM, Fabian TJ, Freeman E, Freeman EW, Friess E, George MS, Goodyer IM, Guidotti A, Heydari B, Heydary B, Kita A, Koszycki D, Lawrie TA, Maayan R, Magill PJ, Majewska MD, Majewska MD, Majewska MD, Matsumoto K, Meieran SE, Melchior CL, Melchior CL, Mensah-Nyagan AG, Mienville JM, Monnet FP, Padberg F, Papadopoulos V, Paul SM, Purdy RH, Rainer Rupprecht, Reddy DS, Reddy DS, Reddy DS, Rodgers RJ, Romeo E, Rupprecht R, Rupprecht R, Schmidt PJ, Schule C, Schule C, Semeniuk T, Serra M, Serra M, Strohle A, Strohle A, Strohle A, Strous RD, Takebayashi M, Thomas C. Baghai, Tollefson GD, Trauger JW, Urani A, Uzunov DP, Uzunova V, Uzunova V, Uzunova V, Vanselow W, Wieland S, Wolkowitz OM, Wolkowitz OM, Wu FS, Zwanzger P   +79 more
core   +1 more source

Synthetic epoxy-pregnan steroids: effects on anxiety behavior in rats [PDF]

, 2016
Neurosteroids like 3α-OH-5α-pregnan-20-one (allopregnanolone) and 3α-OH-5β-pregnan-20-one (pregnanolone) modulate the γ-aminobutyric acid-A (GABAA) receptor function and produce several effects that can be considered for therapeutical pruposes like ...
Coirini, Hector, Ghini, Alberto Antonio, Rey, Mariana   +2 more
core   +1 more source

Investigation of the Possible Allostery of Koumine Extracted From Gelsemium elegans Benth. And Analgesic Mechanism Associated With Neurosteroids

Frontiers in Pharmacology, 2021
Translocator protein 18 kDa (TSPO) is an evolutionarily conserved 5-transmembrane domain protein, and has been considered as an important therapeutic target for the treatment of pain.
Bojun Xiong, Bojun Xiong, Wenbing You, Yufei Luo, Guilin Jin, Guilin Jin, Minxia Wu, Ying Xu, Ying Xu, Jian Yang, Jian Yang, Huihui Huang, Changxi Yu, Changxi Yu   +13 more
doaj   +1 more source

Block of NMDA receptor channels by endogenous neurosteroids: implications for the agonist induced conformational states of the channel vestibule [PDF]

, 2015
N-methyl-D-aspartate receptors (NMDARs) mediate synaptic plasticity, and their dysfunction is implicated in multiple brain disorders. NMDARs can be allosterically modulated by numerous compounds, including endogenous neurosteroid pregnanolone sulfate ...
A Malayev, A Sali, A Villarroel, AI Sobolevskii, AI Sobolevsky, AI Sobolevsky, AI Sobolevsky, BO Dubrovsky, C Beck, CE Weaver, CE Weaver Jr., CH Lee, CL Kussius, CT Smothers, CT Smothers, E Karakas, E Stastna, EE Baulieu, G Abdrachmanova, GQ Chen, H Havlikova, HR Chang, I Cerny, J Borovska, J Dai, J Zuo, JA Kemp, K Kashiwagi, K Vales, L Nowak, L Rambousek, L Vyklicky Jr., LM Arnostova, LP Wollmuth, M Benveniste, M Hollmann, M Horak, M Korinek, M Park-Chung, M Park-Chung, M Park-Chung, M Petrovic, M Sheng, M Xu, MA Larkin, MA Lomize, MA Lynch, MF Sanner, ML Mayer, MM Zarei, N Kashiwabuchi, NJ Sucher, PA Lapchak, R Kancheva, R Kazi, R Sprengel, RH Evans, S Schreier, SE Murthy, SF Traynelis, SH Mellon, SI Mota   +61 more
core   +1 more source

Neurosteroids in Schizophrenia: Pathogenic and Therapeutic Implications

Frontiers in Psychiatry, 2018
Neurosteroids are a group of important endogenous molecules affecting many neural functions in the brain. Increasing evidence suggests a possible role of these neurosteroids in the pathology and symptomatology of schizophrenia (SZ) and other mental ...
HuaLin Cai, HuaLin Cai, Ting Cao, Ting Cao, Xiang Zhou, Xiang Zhou, Jeffrey K. Yao, Jeffrey K. Yao, Jeffrey K. Yao   +8 more
doaj   +1 more source

Neurosteroids as Selective Inhibitors of Glycine Receptor Activity: Structure-Activity Relationship Study on Endogenous Androstanes and Androstenes

Frontiers in Molecular Neuroscience, 2020
The ability of androstane and androstene neurosteroids with modifications at C-17, C-5, and C-3 (compounds 1-9) to influence the functional activity of inhibitory glycine and γ-aminobutyric acid (GABA) receptors was estimated.
Julia V. Bukanova, Elena I. Solntseva, Eva Kudova   +2 more
doaj   +1 more source

Allopregnanolone Decreases Evoked Dopamine Release Differently in Rats by Sex and Estrous Stage

Frontiers in Pharmacology, 2021
Mesolimbic dopamine transmission is dysregulated in multiple psychiatric disorders, including addiction. Previous studies found that the endogenous GABAergic steroid (3α,5α)-3-hydroxy-5-pregnan-20-one (allopregnanolone) modulates dopamine levels in the ...
Ana Paula S. Dornellas, Ana Paula S. Dornellas, Giovana C. Macedo, Giovana C. Macedo, Minna H. McFarland, Alexander Gómez-A, Todd K. O’Buckley, Claudio Da Cunha, A. Leslie Morrow, A. Leslie Morrow, A. Leslie Morrow, Donita L. Robinson, Donita L. Robinson   +12 more
doaj   +1 more source

Midazolam inhibits hippocampal long-term potentiation and learning through dual central and peripheral benzodiazepine receptor activation and neurosteroidogenesis [PDF]

, 2010
Benzodiazepines (BDZs) enhance GABA(A) receptor inhibition by direct actions on central BDZ receptors (CBRs). Although some BDZs also bind mitochondrial receptors [translocator protein (18 kDa) (TSPO)] and promote the synthesis of GABA-enhancing ...
Izumi, Yukitoshi, O\u27Dell, Kazuko A, Tokuda, Kazuhiro, Zorumski, Charles F   +3 more
core   +2 more sources

Neurosteroids and epilepsy [PDF]

Current Opinion in Neurology, 2010
Neurosteroids are a family of compounds synthesized directly in the brain by transforming cholesterol into pregnenolone, which is then converted to compounds such as allopregnanolone and allotetrahydrodeoxycorticosterone. In view of their ability to modulate neurotransmission, neurosteroids may influence the clinical course of epileptic disorders.
Giuseppe Biagini, Gabriella Panuccio, AVOLI, Massimo   +2 more
openaire   +4 more sources