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. Author manuscript; available in PMC: 2013 Dec 1.
Published in final edited form as: Hear Res. 2012 Aug 31;294(0):153–165. doi: 10.1016/j.heares.2012.08.002

Table 1.

Drugs from an FDA-approved drug library that protect hair cells from toxin-induced cell death

Protective Drug CAS #a Ototoxinb Optimal Concentrationc (μM) Pretreatd (min) Uptakee MIC/MBCf FDA targetg
Neo 1hr Gent 1hr Gent 6hr Kan 24hr Cis 24hr
Estrogen-related
raloxifene 82640-04-8 P P P 10 0 <.001 normal SERM
tamoxifen 10540-29-1 P P 10 0 n.s. normal SERM
Serotonin and dopamine-related
paroxetine 110429-35-1 P P P P 10 0 n.s. normal SSRI
fluoxetine 56296-78-7 P P 50 0 n.s. normal SSRI
methiothepin 74611-28-2 P P P 10 60 n.s. normal Serotonin and dopamine agonist
fluspirilene 1841-19-6 P P 10 0 n.s. normal Dopamine antagonist
Adenoreceptor-related
phenoxybenzamine 63-92-3 P P P 50 15 <.05 normal antagonist at alpha adrenoceptor
ractopamine 90274-24-1 P P P P 50 0 <.01 normal agonist at beta adrenoceptor
Other classes
loperamide 34552-83-5 P P P P 10 0 n.s. normal μ-opioid receptor agonist
benzamil 161804-20-2 P P P P P 50 0 <.05 MBC increased Na/Ca channel blocker
a

CAS # is the Chemical Abstract Service Registry number.

b

Shaded box with letter P indicates that a protective effect was observed with that protective compound-toxin combination. Neo=neomycin 1 hr exposure, Gent 1=gentamicin 1 hr exposure, Gent 6=gentamicin 6 hr exposure, Kan=kanamycin 24 hr exposure, Cis=cisplatin 24 hr exposure.

c

The lowest concentration of protective compound tested that confers the maximum protection against toxins.

d

The pretreatment time in minutes before toxin exposure that is needed to observe effective protection.

e

Whether gentamicin-Texas Red is able to enter cells in the presence of protective drug based on our fluorescence assay. The level of significance is indicated for drugs with altered uptake relative to GTTR only; n.s. = gentamicin entry not significantly different from GTTR only control. All drugs had uptake that was significantly different from embryo media only (EM) except for ractopamine and raloxifene.

f

Shows whether protective drug affected minimum inhibitory concentration (MIC) or minimum bactericidal concentration (MBC), where an increase in MIC or MBC indicates that neomycin is less effective at killing bacteria in presence of hair cell protective drug.

g

The accepted target of the drug in the literature, which may or may not describe the mode of action when protecting hair cells. SERM = selective estrogen receptor modulator; SSRI = selective serotonin reuptake inhibitor.