Formulation: A solid
Formal Name: N-[(1R)-1,2,3,4-tetrahydro-1-naphthalenyl]-1H-benzimidazol-2-amine, monohydrochloride
Purity: ≥98%
Formula Markup: C17H17N3 • HCl
Formula Weight: 299,8
Shelf life (days): 1460
CAS Number: 875755-24-1
Notes: NS 8593 is an inhibitory gating modifier of small-conductance calcium-activated potassium (KCa2/SK) channels (Kds = 0.42, 0.6, and 0.73 μM for KCa2.1/SK1, KCa2.2/SK2, and KCa2.3/SK3, respectively, in the presence of calcium) that decreases the calcium sensitivity of SK channels.{53292} It is selective for KCa2/SK channels over intermediate- (KCa3.1/IKCa1) and large-conductance (BK) potassium channels at 10 μM. NS 8593 induces relaxation of potassium- or acetylcholine chloride-precontracted isolated tracheal rings from wild-type mice (IC50s = 8.9 and 39.8 μM, respectively) or from mice in an ovalbumin-induced model of allergic asthma (IC50s = 16.4 and 32.2 μM, respectively).{53293} It inhibits aerosolized acetylcholine chloride-induced increases in respiratory system resistance in mice when administered as an aerosol at a dose of 500 μM. NS 8593 (5 mg/kg) decreases the duration of burst-pacing-induced atrial fibrillation in normotensive and spontaneously hypertensive rats.{53294}
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