Allosteric Receptors after 30 Years

Allosteric Receptors after 30 Years Review

Allosteric Modulation of Muscarinic Acetylcholine Receptors

An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.g., acetylcholine). Since the identification of gallamine as the first allosteric modulator of muscarinic receptors in 1976, this unique mode ...

Allosteric Modulation of Muscarinic Acetylcholine Receptors

An allosteric modulator is a ligand that binds to an allosteric site on the receptor and changes receptor conformation to produce increase (positive cooperativity) or decrease (negative cooperativity) in the binding or action of an orthosteric agonist (e.g., acetylcholine). Since the identification of gallamine as the first allosteric modulator of muscarinic receptors in 1976, this unique mode ...

The antinociceptive effect of 17β-estradiol in the paragigantocellularis lateralis of male rats is mediated by estrogenic receptors

Introduction: 17β-Estradiol is a neuroactive steroid and its pain modulatory role has been well studied previously. 17β-Estradiol modulates nociception by binding to its receptors and also by allosteric interaction with other membrane - bound receptors such as glutamate and GABAA receptors. Paragigantocellularis lateralis (LPGi) is also involved in pain modulation and perception, in addition...

The antinociceptive effect of 17β-estradiol in the nucleus paragigantocellularis lateralis of male rats may be mediated by the NMDA receptors

Introduction: The nucleus paragigantocellularis lateralis (LPGi) is involved in the descending pain modulation. The neurostreoid, 17β-estradiol found in the PGi nucleus and modulates nociception by binding to estrogen receptors and also by allosteric interaction with NMDA receptors. In this study, the role of NMDA receptors in the 17β-estradiol-induced pain modulation was investig...