Download 6 blockers

Sodium channel modulators
Compound
Amiloride hydrochloride
3,5-Diamino-N-(aminoiminomethyl)- 6-chloropyrazinecarboxamide
M.W 266.11 Store at RT Soluble in water
Flecainide acetate
N-(2-Piperidylmethyl)-2,5- bis-(2,2,2-trifluoroethoxy)
benzamide acetate
M.W. 474.40 Desiccate at +4°C Soluble to 50 mM in water
Flunarizine dihydrochloride
(E)-1-[Bis(4-fluorophenyl)methyl]- 4-(3-phenyl-2propenyl)piperazine
M.W. 477.43 Store at RT Soluble to 5 mM in ethanol
QX 222
2-[(2,6-Dimethylphenyl)amino]- N,N,N-trimethyl-2oxoethanaminium chloride
M.W. 256.78 Store at RT Soluble to 100 mM in water
QX 314
N-(2,6-Dimethylphenyl carbamoylmethyl)triethylammonium
bromide
M.W. 343.31 Desiccate at +4°C Soluble to 100 mM in water
Riluzole hydrochloride
2-Amino-6-trifluoromethoxy benzothiazole
M.W. 270.66 Store at Soluble to 100 mM in DMSO
Tetrodotoxin
Octahydro-12-(hydroxymethyl)- 2-imino-5,9:7,10a-dimethano10aH-[1,3]dioxocino[6,5-d]pyrimidine- 4,7,10,11,12-pentol
M.W. 319.27 Desiccate at +4°C Soluble in acidic buffer (pH
4.8)
Tetrodotoxin citrate
Octahydro-12-(hydroxymethyl)- 2-imino-5,9:7,10a-dimethano10aH-[1,3]dioxocino[6,5-d] pyrimidine-4,7,10,11,12-pentol
M.W. 511.40 Desiccate at +4°C Soluble in water
Vinpocetine
(3a,16a)-Eburnamenine-14-carboxylic acid ethyl ester
M.W. 350.46 Store at RT Soluble in DMSO and ethanol
Pharmacological Action
Na+ channel blocker. Affinity for, or lack of, defines the I2Aamiloride sensitive and I2B-amiloride insensitive imidazoline
binding sites.
Open Na+ channel blocker that inhibits fast Na+ current in
cardiac muscle in a use- and concentration-dependent manner.
Orally-active class lc antiarrhythmic agent.
Dual Na+/Ca2+ channel blocker; a cerebral and peripheral
vasodilator. Neuroprotective.
Sodium channel blocker.
Membrane impermeable quaternary derivative of lidocaine, a
blocker of voltage-activated Na+ channels.
Novel psychotropic agent with anticonvulsant, hypnotic,
anxiolytic, anti-ischaemic and anaesthetic properties. Riluzole
is able to act as a glutamate release inhibitor, blocks voltage
dependent Na+ channels and inhibits GABA uptake by striatal
synaptosomes.
Selective inhibitor of Na+ channel conductance. Binding is
reversible and of high affinity (Kd = 1-10 nM). Blocks in a
use-dependent manner.
Highly selective, reversible sodium channel blocker; citrate
salt of tetrodotoxin.
Phosphodiesterase inhibitor, selective for PDE1 (IC50 = 21
µM). Also blocks voltage-gated Na+ channels.
Potassium channel modulators
Compound
N-[2-(Acetoxy)ethyl]-3-pyridinecarboxamide
M.W. 207.20 Desiccate at +4°C Soluble in water
AM 92016 hydrochloride
1-(4-Methanesulphonamidophenoxy)- 3-(N-methyl-3,4dichlorophenylethylamino)-2-propanol
M.W. 483.84 Store at RT Soluble to 100 mM in water and to
100 mM in ethanol
4-Aminopyridine
M.W. 94.12 Store at RT Soluble in DMSO
Charybdotoxin
M.W. 4295.90 Desiccate at -20°C Solubility: see Peptides
Chromanol 293B
trans-N-[6-Cyano-3,4-dihydro- 3-hydroxy-2,2-dimethyl-2H-1benzopyran-4-yl]-N-methyl- ethanesulfonamide
M.W. 324.39 Store at RT Soluble in DMSO
(-)-[3R,4S]-Chromanol 293B
N-[(3R,4S)-6-Cyano-3,4-dihydro- 3-hydroxy-2,2-dimethyl2H-1- benzopyran-4-yl]-N-methyl
M.W. 324. Store at RT Soluble to 1 mM in ethanol and 1 mM
in DMSO
Pharmacological Action
Analogue of nicorandil. A nitrate-free coronary vasodilator;
activates K+ channels.
A specific blocker of the time dependent delayed rectifier
potassium current, devoid of any b-adrenoceptor blocking
activity.
K+-channel blocker.
Specific inhibitor of the high conductance Ca2+-activated K+
channel.
Blocker of the slow delayed rectifier K+ current (IKs) (IC50 =
1-10 mM). Also blocks the CFTR chloride current (ICFTR)
(IC50 =19 mM).
Enantiomer that selectively inhibits the slow component of
delayed rectifier K+ current (IKs). Block is use-dependent and
7-fold more potent than the (+)-(3S,4R) enantiomer (IC50
values are 1.36 and 9.6 µM respectively). Has negligible
inhibitory action at hERG channels (IC50 > 30 µM).
CP 339818 hydrochloride
N-[1-(Phenylmethyl)-4(1H)- quinolinylidene]-1 pentanamine
hydrochloride
M.W. 340.89 Store at RT Soluble to 20 mM in water
Cromakalim
BRL 34915 / trans-3,4-dihydro-3-hydroxy-2,2- dimethyl-4-(2oxo-1-pyrrolidinyl)- 2H-1-benzopyran-6-carbonitrile
M.W. 286.33 Store at RT Soluble to 20 mM in DMSO
Dequalinium dichloride
1,1´-(1,10-Decanediyl)bis (4-amino-2-methylquinolinium)
chloride
M.W. 527.58 Store at RT Slightly soluble in water
Diazoxide
7-Chloro-3-methyl-2H-1,2,4- benzothiadiazine 1,1-dioxide
M.W. 230.67Store at RT Soluble to 100 mM in DMSO
1-EBIO
1-Ethyl-2-benzimidazolinone
M.W. 162.19 Store at RT Soluble to 100 mM in DMSO
Glibenclamide
Glyburide / 5-Chloro-N-[2-[4- [[[(Cylcohexylamino)carbonyl]
amino]sulphonyl]phenyl]ethyl]- 2-methoxybenzamide
M.W. 494.01 Store at RT Soluble to 5 mM in ethanol
Iberiotoxin
M.W. 4230 Desiccate at -20°C Solubility: see Peptides
Levcromakalim
BRL 38227 / (3S,4R)-3,4-dihydro-3-hydroxy- 2,2-dimethyl-4(2-oxo-1-pyrrolidinyl)- 2H-1-benzopyran-6-carbonitrile
M.W. 286.33 Store at RT Soluble to 10 mM in DMSO
Minoxidil
6-(1-Piperidinyl)-2,4- pyrimidinediamine 3-oxide
M.W. 209.25 Store at RT Soluble in ethanol
P1075
N-Cyano-N´-(1,1- dimethylpropyl)-N´´-3- pyridylguanidine
M.W. 231.30 Store at RT Soluble to 100 mM in 1 eq. HCl
and to 50 mM in ethanol
Pinacidil
N-Cyano-N´-4-pyridinyl-N´´- (1,2,2-trimethylpropyl)guanidine
M.W. 245.33 Store at RT Soluble to 100 mM in ethanol and to
100 mM in DMSO
Tertiapin-Q
M.W. 2452.00 Desiccate at -20°C Solubility: see Peptides
YS-035 hydrochloride
N,N-Bis-(3,4- dimethoxyphenylethyl)-N-methylamine
M.W. 395.90 Desiccate at RT Soluble to 100 mM in water
ZM 226600
N-(4-Phenylsulphonylphenyl)- 3,3,3-trifluoro-2-hydroxy-2methylpropanamide
M.W. 373.35 Store at RT Soluble in ethanol
Potent, non-peptide Kv1.3 channel antagonist that
preferentially binds to the C-type inactivated state of the
channel (IC50 ~ 200 nM). Inhibits Kv1.4 with an IC50 of ~
300 nM. Selective over Kv1.1, Kv1.2, Kv1.5, Kv1.6, Kv3.1-4
and Kv4.2.
Prototypical KATP channel opener. Relaxes rabbit isolated
portal vein with an IC50 value of 21 nM. Potent, orally active
and hypotensive in vivo.
A potent and selective non-peptide blocker of the apaminsensitive small conductance Ca2+-activated K+ channel.
Antihypertensive. Activates ATP-dependent K+ channels;
blocks desensitization of AMPA receptors.
The first activator of epithelial Kca channels to be identified,
across T84 monolayers it stimulates a large and sustained
trans-epithelial chloride secretory response.
Blocks ATP-dependent K+ channels in the pancreas, causing
an increase in intracellular Ca2+ and insulin secretion.
Selective blocker of the high conductance Ca2+-activated K+
channel.
Active enantiomer of the prototypical KATP channel opener
cromakalim. Hypotensive and airways relaxant. IC50 = 490
nM in guinea pig trachea.
Antihypertensive. Antialopecia agent. K+ channel activator.
Potent KATP channel opener (EC50 for relaxation of rat aorta
= 7.5 nM). Binds to SUR2A and SUR2B with high affinity
(Kd values are 17 and 3 nM respectively).
K+ channel opener and vasodilator. Activates KATP channels
(IC50 for relaxation of coronary arteries = 1.26 µM). Clinically
used antihypertensive agent.
A high affinity inhibitor for inward-rectifier K+ channels, this
compound is a stable derivative of the bee venom toxin
tertiapin. Binds to ROMK1 and GIRK1/4 channels with high
affinity (Ki values are 1.3 and 13.3 nM respectively) and is
selective over IRK1 channels.
A Ca2+ blocker that strikingly prolongs cardiac action
potentials by inhibiting pacemaker current and K+ outward
currents.
Potent KATP channel opener (EC50 = 0.5 µM), devoid of antiandrogen properties.
Calcium channel modulators
Compound
Diltiazem hydrochloride
(2S-cis)-3-(Acetyloxy)-5-[2- (dimethylamino)ethyl]-2,3dihydro-2- (4-methoxyphenyl)-1,5- benzothiazepin-4(5H)-one
M.W. 450.99 Store at RT Soluble in water
Pharmacological Action
Antihypertensive and cardioprotective agent; an inhibitor of Ltype Ca2+ channels.
Gabapentin hydrochloride
1-(Aminomethyl) cyclohexaneacetic acid
M.W. 207.70 Desiccate at + 4°C Soluble to 100 mM in water
Gabapentin
1-(Amino-[3H]-methyl)- [2,3,5,6-3H]-cyclohexaneacetic acid
M.W. 171.20 Solvent: ethanol:water (1:1)
Shipped in dry ice
Nifedipine
1,4-Dihydro-2,6-dimethyl-4- (2nitrophenyl)-3,5pyridinedicarboxylic acid dimethyl ester
M.W. 346.33 Store at RT Soluble to 100 mM in DMSO
(R)(-)-Niguldipine hydrochloride
M.W. 646.18 Desiccate at -20°C Soluble to 10 mM in water
(S)(+)-Niguldipine hydrochloride
M.W. 646.18 Desiccate at -20°C Soluble to 10 mM in water
Nimodipine
1,4-Dihydro-2,6-dimethyl-4- (3-nitrophenyl)-3,5pyridinedicarboxylic acid 2-methyloxyethyl 1-methylethyl
ester
M.W. 418.45 Store at RT Soluble to 100 mM in ethanol
Nitrendipine
1,4-Dihydro-2,6-dimethyl-4- (3-nitrophenyl)-3,5-pyridine
dicarboxylic acid ethyl methyl ester
M.W. 360.37 Store at RT Soluble in ethanol and DMSO
Verapamil hydrochloride
a-[3-[[2-(3,4-Dimethoxyphenyl) ethyl]methylamino]propyl]3,4- dimethoxy-a-(1-methylethyl) benzeneacetonitrile
M.W. 491.04 Store at RT Soluble in water and ethanol
Loperamide hydrochloride
4-(4-Chlorophenyl)-4-hydroxy- N,N-dimethyl-a,a-diphenyl-1piperidinebutanamide
M.W. 513.51 Store at RT Soluble in ethanol
w-Conotoxin GVIA
M.W. 3037 Desiccate at -20°C Solubility : see Peptides
w-Conotoxin MVIIC
M.W. 2755 Desiccate at -20°C Solubility : see Peptides
Ruthenium Red
Ammoniated ruthenium oxychloride
M.W. 786.35 Store at RT Soluble to 50 mM in water
SKF 96365 hydrochloride
1-[2-(4-Methoxyphenyl)-2-[3- (4-methoxyphenyl)propoxy]
ethyl-1H-imidazole
M.W. 402.92 Store at RT Soluble to 100 mM in water
Anticonvulsant with several possible mechanisms of action.
Gabapentin increases GABA in the brain and binds to a novel
site associated with voltage-sensitive Ca2+ channels. Prevents
neuronal death and is antinociceptive and anxiolytic.
Binds to the a2d subunit of voltage-dependent Ca2+ channels
(Kd = 37.5 nM) and competes with large neutral amino acids,
such as L-leucine, for uptake into rat synaptosomes (KM = 160
mM).
L-type calcium channel blocker.
L-type Ca2+ channel blocker and a1A-adrenoceptor
antagonist; less active enantiomer.
L-type Ca2+ channel blocker and a1A-adrenoceptor
antagonist; more active enantiomer
L-type Ca2+ channel blocker.
L-type calcium channel blocker.
L-type calcium channel blocker. Vasodilator, adrenergic
antagonist.
Antidiarrhoeal agent with high affinity for both peripheral and
central opioid receptors. Also a Ca2+ channel blocker; at low
micromolar concentrations it blocks broad spectrum neuronal
HVA Ca2+ channels and at higher concentrations it reduces
Ca2+ flux through NMDA receptor operated channels.
Peptide neurotoxin; selectively and reversibly blocks N-type
calcium channels.
Peptide neurotoxin; wide spectrum blocker of N, P and Q-type
calcium channels.
Blocks Ca2+ uptake and release from mitochondria and Ca2+
release from ryanodine-sensitive intracellular stores. Also
blocks cell membrane-located capsaicin-activated cation
channels (IC50 = 14 nM) and voltage-sensitive Ca2+ channels
to inhibit neurotransmitter release.
An inhibitor of receptor-mediated calcium influx.
Chloride channel modulators
Compound
9-AC
9-Anthracenecarboxylic acid
M.W. 222.24 Store at RT Soluble to 100 mM in DMSO and to
10 mM in ethanol
Chromanol 293B
trans-N-[6-Cyano-3,4-dihydro- 3-hydroxy-2,2-dimethyl-2H-1benzopyran-4-yl]-N-methyl- ethanesulfonamide
M.W. 324.39 Store at RT Soluble in DMSO
DCEBIO
5,6-Dichloro-1-ethyl-1,3-dihydro- 2H-benzimidazol-2-one
M.W. 231.08 Store at RT Soluble in DMSO
Pharmacological Action
Cl- transport inhibitor with a moderate to strong inhibitory
action on PKA activated cardiac
Blocker of the slow delayed rectifier K+ current (IKs) (IC50 =
1-10 mM). Also blocks the CFTR chloride current (ICFTR)
(IC50 = 19 mM).
Stimulates Cl- secretion via activation of hlK1 K+ channels
and the activation of an apical Cl- conductance. More potent
than its analogue 1-EBIO.
NPPB
5-Nitro-2-(3-phenylpropylamino) benzoic acid
M.W. 300.31 Store at RT Soluble in DMSO and ethanol
Very potent chloride channel blocker.
Source Tocris On-line Catalogue (http://www.tocris.com/cat/icm.html) 27 June, 2002