ω-Agatoxin IVA

ω-Agatoxin IVA is a potent, selective P/Q type Ca²⁺ (Cav2.1) channel blocker with IC₅₀ values of 2 nM and 90 nM. ω-Agatoxin IVA inhibits glutamate exocytosis and calcium influx elicited by high potassium. ω-Agatoxin IVA inhibits Capsaicin (HY-10448)-induced CGRP release and vasodilation. ω-Agatoxin IVA can be used for the research of neurological and cardiovascular disease^[1][2][3]. IC50 & Target:IC50: 2 nM (P-type Ca²⁺ channels), 90 nM (Q-type Ca²⁺ channels)^[1] In Vitro:ω-Agatoxin IVA potently inhibits somatic P-type calcium channels in rat cerebellar Purkinje neurons with an IC₅₀ of 2 nM^[1].
ω-Agatoxin IVA inhibits Q-type calcium channels in rat cerebellar granule neurons with an IC₅₀ of 90 nM, which is 45-fold less potent than its activity against P-type channels^[1].
ω-Agatoxin IVA inhibits high potassium-induced glutamate exocytosis and calcium influx in rat cortical synaptosomes with IC₅₀ values ranging from 30 nM to 225 nM^[1].
ω-Agatoxin IVA (200 nM) inhibits cloned rat brain rbA-I and rbA-II calcium channel isoforms by only 20%^[1].
ω-Agatoxin IVA (100 nM) does not inhibit voltage-dependent calcium currents in cultured rat sympathetic neurons^[2].
ω-Agatoxin IVA (100 nM; 30 min) does not alter frequency-dependent neurogenic excitatory responses in isolated rabbit pulmonary artery ring preparations^[2].
ω-Agatoxin IVA (100 nM; 30 min) does not significantly inhibit neurogenic cholinergic excitatory responses in isolated guinea-pig myenteric plexus preparations^[2].
ω-Agatoxin IVA (100 nM; 30 min) does not significantly inhibit neurogenic noradrenergic excitatory responses in isolated rat vas deferens preparations^[2].
ω-Agatoxin IVA (100 nM; 30 min) does not significantly inhibit neurogenic excitatory responses in isolated rat bladder strip preparations^[2].
ω-Agatoxin IVA (100 nM; 30 min) does not significantly inhibit neurogenic noradrenergic excitatory responses in isolated rat anococcygeus muscle preparations^[2].
ω-Agatoxin IVA (100 nM; 30 min) does not significantly alter neurogenic NANC inhibitory responses in isolated Atropine (HY-B1205)/Guanethidine (HY-B1251)-treated rat anococcygeus muscle and jejunum preparations preparations^[2].
ω-Agatoxin IVA (0.1 μmol/L; 30 min) potently inhibits Capsaicin (HY-10448)-induced CGRP release from isolated rat pial arteries^[3]. In Vivo:ω-Agatoxin IVA (0.1 μmol/L; topical suffusion; 30 minutes before and during exposure/induction) significantly inhibits Capsaicin (HY-10448)-induced vasodilation, and severely attenuates cerebral autoregulatory vasodilation and vasoconstriction responses to acute stepwise hypotension in rats^[3].