LNP-911

LNP-911 (10^-10-10^-3 M; 60 min) exhibits low affinity for human α₂A, α₂B and α₂C adrenergic receptors expressed on CHO cell membranes, with K_i values ranging from 1750 nM to ≥10,000 nM; it shows low affinity for I₂ binding sites in rabbit kidney cell membranes (K_i = 25,428 nM)^[1].
LNP-911 (10^-10-10^-3 M; 30 min) binds to I₁ imidazoline receptors on PC-12 cell membranes, with a high-affinity K_i value of 0.2 nM (accounting for 38% of binding sites) and a low-affinity K_i value of 10000 nM^[1].
[¹²⁵I]-labeled LNP-911 (0.05-6.6 nM; 60 min) binds to a single high-affinity site on PC-12 cell membranes, with a K_d value of 1.4 nM and a B_max value of 398 fmol/mg protein^[1].
LNP‑911 acts as an allosteric potentiator in PC‑12 cells, dose‑dependently enhancing the inhibitory effect of I1 receptor agonists on forskolin‑stimulated cAMP production and exerting no independent influence on cAMP levels^[1].
LNP-911 binds with high affinity to I₁-imidazoline receptors on PC12 cell membranes, with K_i values of 1.4 nM (using [¹²⁵I]LNP 911 as the radioligand)^[2].
LNP-911 exists mainly as a stable non-planar imine tautomer (IIB) in both gas and aqueous phases^[3].