MOLECULAR PHARMACOLOGY
MOLECULAR PHARMACOLOGY
| STUDY | IQB-9302 | BUPIVACAINE |
| Blockade of neuronal voltage dependent Na+ Channels | IC50 = 134 mM
Blocking effects faster t = 1,8 sec Recovery slower (*) |
IC50 = 95 mM
Blocking effects slower t = 2.2 sec Faster recovery |
| Blockade of voltage-dependent Ca++ | IC 50 = 310 mM | IC 50 = 110 mM |
| Nicotinic receptor blockade | IC50 = 9.11 mM (**) | IC50 = 0.32 mM |
| a3b4 neuronal nicotinic receptors expressed in oocytes | IC 50 = 1.4 mM
Faster and complete recovery (**) |
IC 50 = 3.0 mM
Slower and partial recovery |
(*)
could explain longer duration of anesthesia seen in some animal experiments
and clinical trials
(**)
In the case of systemic accidental injection the hypotension derived from
ganglionic blockade should be much less with IQB-9302 than with bupivacaine.