Modulator | Effect | EC50 | Maximal Effect3-a | |
---|---|---|---|---|
Dynorphin | Inhibition | 0.3 μM3-b | 100% | Chen et al., 1995 a, b; Brauneis et al., 1996; Zhang et al., 1997; Chen and Huang, 1998 |
Osmotic pressure | Inhibition | 75% | Paoletti and Ascher, 1994 | |
Oxidizing agents | Inhibition | 70%3-c | Aizenman et al., 1989, 1990, 1992; Tang and Aizenman, 1993 a,b | |
Protons | Inhibition | 50–200 nM3-d | 100% | reviewed by Traynelis, 1998 |
Sulfated steroids | Inhibition | 150 μM3-e | 100% | Park-Chung et al., 1994, 1997 |
Zinc | Inhibition | 0.2–2 μM3-g | 100–80% | Smart et al., 1994; Williams, 1996; Chen et al., 1997; Paoletti et al., 1997; Traynelis et al., 1998 |
Arachidonic acid | Potentiation | 10 μM | 2-fold | Miller et al., 1992; Petrou et al., 1993; Horimoto et al., 1996; Mishikawa et al., 1994; Tabuchi et al., 1997 |
PACAP3-g | Potentiation | <1 μM | 3-fold | Liu and Madsen, 1997; Wu and Dunn, 1997 |
Polyamines, histamine | Potentiation | 100 μM3-h | 2-fold | Johnson, 1996; Williams, 1997a,b |
Reducing agents | Potentiation | 3-fold | Aizenman et al., 1989, 1990, 1992; Tang and Aizenman, 1993 a,b | |
Sulfated steroids | Potentiation | 12 μM3-i | 2.5-fold | Park-Chung et al., 1997 |
↵3-a Other exogenous modulators have been described: ethanol (Peoples and Weight, 1995, 1998; Masood et al., 1994; Peoples et al., 1997); ifenprodil (Legendre and Westbrook, 1991; Kew et al., 1996; Mott et al., 1998), and conanotokins (Zhou et al., 1996). Maximal inhibition (100% is full inhibition) or x-fold potentiation.
↵3-b Dynorphin A 1-32.
↵3-c The response of fully reduced receptors (e.g., dithiothreitol treated) is decreased by 70% by oxidizing agents.
↵3-d Proton inhibition depends on subunit composition.
↵3-e 3β-hydroxy-5β-pregnan-20-one sulfate.
3-f NR2A-containing receptors are much more sensitive to extracellular Zn2+ than receptors containing other subunits; NR2C and NR2D are much less sensitive to Zn2+.
↵3-g Pituitary adenylyl cyclase-activating peptide.
↵3-h Spermine.
↵3-i Pregnanalone sulfate.