Tetrazolyl isoxazole amino acids as ionotropic glutamate receptor antagonists: Synthesis, modelling and molecular pharmacology

2005 ◽  
Vol 13 (18) ◽  
pp. 5391-5398 ◽  
Author(s):  
Bente Frølund ◽  
Jeremy R. Greenwood ◽  
Mai M. Holm ◽  
Jan Egebjerg ◽  
Ulf Madsen ◽  
...  
Keyword(s):  
Amino Acids ◽  
Glutamate Receptor ◽  
Ionotropic Glutamate Receptor ◽  
Molecular Pharmacology ◽  
Receptor Antagonists ◽  
Glutamate Receptor Antagonists

scholarly journals Discovery of a New Class of Ionotropic Glutamate Receptor Antagonists by the Rational Design of (2S,3R)-3-(3-Carboxyphenyl)-pyrrolidine-2-carboxylic Acid

2010 ◽  
Vol 2 (2) ◽  
pp. 107-114 ◽  
Author(s):  
Ann M. Larsen ◽  
Raminta Venskutonytė ◽  
Elena Antón Valadés ◽  
Birgitte Nielsen ◽  
Darryl S. Pickering ◽  
...  
Keyword(s):  
Carboxylic Acid ◽  
Glutamate Receptor ◽  
Rational Design ◽  
Ionotropic Glutamate Receptor ◽  
Receptor Antagonists ◽  
New Class ◽  
Glutamate Receptor Antagonists

Effects of ionotropic glutamate receptor antagonists on responses of vagal mechanosensitive afferents innervating the rat stomach

2003 ◽  
Vol 124 (4) ◽  
pp. A250
Author(s):  
Jaime Petersen ◽  
Shachar Peles ◽  
David D. Gutterman ◽  
Reza Shaker ◽  
Jyoti N. Sengupia
Keyword(s):  
Glutamate Receptor ◽  
Ionotropic Glutamate Receptor ◽  
Rat Stomach ◽  
Receptor Antagonists ◽  
Glutamate Receptor Antagonists

scholarly journals Preoptic area cooling increases the sympathetic outflow to brown adipose tissue and brown adipose tissue thermogenesis

2018 ◽  
Vol 315 (4) ◽  
pp. R609-R618 ◽  
Author(s):  
Mazher Mohammed ◽  
Christopher J. Madden ◽  
Kim J. Burchiel ◽  
Shaun F. Morrison
Keyword(s):  
Adipose Tissue ◽  
Brown Adipose Tissue ◽  
Glutamate Receptor ◽  
Preoptic Area ◽  
Hypothalamic Nucleus ◽  
Ionotropic Glutamate Receptor ◽  
Receptor Antagonists ◽  
Efferent Pathway ◽  
Brown Adipose ◽  
Glutamate Receptor Antagonists

Modest cold exposures are likely to activate autonomic thermogenic mechanisms due to activation of cutaneous thermal afferents, whereas central thermosensitive neurons set the background tone on which this afferent input is effective. In addition, more prolonged or severe cold exposures that overwhelm cold defense mechanisms would directly activate thermosensitive neurons within the central nervous system. Here, we examined the involvement of the canonical brown adipose tissue (BAT) sympathoexcitatory efferent pathway in the response to direct local cooling of the preoptic area (POA) in urethane-chloralose-anesthetized rats. With skin temperature and core body temperature maintained between 36 and 39°C, cooling POA temperature by ~1–4°C evoked increases in BAT sympathetic nerve activity (SNA), BAT temperature, expired CO2, and heart rate. POA cooling-evoked responses were inhibited by nanoinjections of ionotropic glutamate receptor antagonists or the GABAA receptor agonist muscimol into the median POA or by nanoinjections of ionotropic glutamate receptor antagonists into the dorsomedial hypothalamic nucleus (bilaterally) or into the raphe pallidus nucleus. These results demonstrate that direct cooling of the POA can increase BAT SNA and thermogenesis via the canonical BAT sympathoexcitatory efferent pathway, even in the face of warm thermal input from the skin and body core.

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