(+)-Niguldipine hydrochloride

(+)-Niguldipine binds with high and roughly comparable affinity to the 1,4-dihydropyridine receptors associated with L-type Ca²⁺ channels in the cell membranes of guinea pig skeletal muscle (K_i = 85 pmol/L), brain (K_i = 140 pmol/L) and heart (K_i = 45 pmol/L), and is approximately 40 times more potent than its (-)-enantiomer^[1].
(+)-Niguldipine (8-19 different concentrations; 45 min) binds to α₁-adrenergic receptors in rat liver cell membranes, with a K_i value of 78 nmol/L, and its potency is comparable to that of its (-)-enantiomer^[1].
(+)-Niguldipine (8-19 different concentrations; 45-60 min) binds highly selectively to α₁A-adrenergic receptors in rat cerebral cortex cell membranes (relative to α₁B-adrenergic receptors), with a selectivity index of 617 against [³H]prazosin and 230 against [¹²⁵I]HEAT; when using [³H]prazosin, its K_h = 52 pmol/l, and it is over 40 times more potent at the α₁A subtype than its (-)-enantiomer^[1].
(+)-Niguldipine (variable dose; 20 min incubation) displaces the specific binding of [³H]prazosin to rabbit ventricular myocardial membrane fractions at 23.1% of the binding sites with high affinity (K_i = 64.6 pmol/L), while it exhibits low affinity (K_i = 7.08 nmol/L) for the remaining sites^[2].

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