GABAA receptor negative allosteric modulator - significado y definición. Qué es GABAA receptor negative allosteric modulator
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Qué (quién) es GABAA receptor negative allosteric modulator - definición


GABAA receptor negative allosteric modulator         
A GABAA receptor negative allosteric modulator is a negative allosteric modulator (NAM), or inhibitor, of the GABAA receptor, a ligand-gated ion channel of the major inhibitory neurotransmitter γ-aminobutyric acid (GABA). They are closely related and similar to GABAA receptor antagonists.
GABAA receptor positive allosteric modulator         
  • Fig 9. Common R group positions of Benzodiazepines
  • Fig 8. R-group position of [[Barbiturates]]
  • Fig 3. Binding sites of different therapeutic chemical groups on a GABAA receptor
  • Fig 4. GABAergic synapse. The synaptic anchoring protein [[Gephyrin]] is indirectly linked to the GABAA receptors.
  • Fig 10. Different R-group analogs for neurosteroids. Groups 1–4 and 10 have significant therapeutic value.
  • Fig 7. Synthesis and discovery of [[chlordiazepoxide]]
A SUBSTANCE THAT DOES NOT ACT AS AGONIST OR ANTAGONIST BUT DOES AFFECT THE GAMMA-AMINOBUTYRIC ACID RECEPTOR-IONOPHORE COMPLEX
GABAA receptor positive allosteric modulators; GABAA receptor PAM; GABA modulator; GABA modulators; GABAkine; GABAkines; GABAA receptor potentiator; GABAA receptor potentiators; GABAAR potentiators; GABAAR potentiator; GABA-A receptor potentiator; GABA-A receptor potentiators
In pharmacology, GABAA receptor positive allosteric modulators are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system.
Allosteric modulator         
  • CX614, a PAM for an AMPA receptor binding to an allosteric site and stabilizing the closed conformation
  • Orthosteric agonist (A) binds to orthosteric site (B) of a receptor (E). Allosteric modulator (C) binds to allosteric site (D). Modulator increases/lowers the affinity (1) and/or efficacy (2) of an agonist. Modulator may also act as an agonist and yield an agonistic effect (3). Modulated orthosteric agonist affects the receptor (4). Receptor response (F) follows.
SUBSTANCE THAT BINDS TO A REGULATORY SITE DISTINCT FROM THE ACTIVE SITE ON A PROTEIN, RESULTING IN CONFORMATIONAL CHANGES THAT MAY INFLUENCE PROTEIN FUNCTION
Allosteric modulation; Positive allosteric modulator; Negative allosteric modulator; Negative allosteric modulation; Positive allosteric modulation; Positive allosteric modulators; Negative allosteric modulators; Positive modulator; Positive modulators; Negative modulator; Negative modulators
In pharmacology and biochemistry, allosteric modulators are a group of substances that bind to a receptor to change that receptor's response to stimulus. Some of them, like benzodiazepines, are drugs.