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Ca2+ Modulators
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ALX-400-045 Revised 31-Aug-07
2-Aminoethoxydiphenyl borate
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SYNONYMS 2-APB
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-400-045-M100   100 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C14H16BNO
MW: 225.1
CAS NUMBER: 524-95-8
RTECS: ED6150000
PURITY: ≥98%
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in DMSO, dimethyl formamide or 100% ethanol; also soluble in PBS, pH 7.2.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. Stock solutions are stable for 2 months at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Hygroscopic. Packaged under inert gas.

Product Description
Cell permeable modulator of Ins(1,4,5)-P3-induced Ca2+ release. A prototype drug for a group of structurally related calcium channel blockers in human platelets. Has been shown, in the absence of other stimuli, to activate TRPV1, V2 and V3, but not TRPV4, V5 and V6 expressed in HEK 293 cells.
Product Specific Literature References
2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release: T. Maruyama, et al.; J. Biochem. 122, 498 (1997) Abstract
Inhibition of SERCA Ca2+ pumps by 2-aminoethoxydiphenyl borate (2-APB). 2-APB reduces both Ca2+ binding and phosphoryl transfer from ATP, by interfering with the pathway leading to the Ca2+-binding sites: J.G. Bilmen, et al.; Eur. J. Biochem. 269, 3678 (2002) Abstract
2-aminoethoxydiphenyl borate (2-APB) is a reliable blocker of store-operated Ca2+ entry but an inconsistent inhibitor of InsP3-induced Ca2+ release: M.D. Bootman, et al.; FASEB J. 16, 1145 (2002) Abstract
Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives: H. Watanabe, et al.; J. Biol. Chem. 277, 13569 (2002) Abstract
2-Aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2 and TRPV3: H.Z. Hu, et al.; J. Biol. Chem. 279, 35741 (2004) Abstract; Full Text
TRPV4 calcium entry channel: a paradigm for gating diversity: B. Nilius, et al.; Am. J. Physiol. Cell Physiol. 286, C195 (2004) Abstract
2APB- and JTV519(K201)-sensitive micro Ca2+ waves in arrhythmogenic Purkinje cells that survive in infarcted canine heart: P.A. Boyden, et al.; Heart Rhythm 1, 218 (2004) Abstract
Inhibition of glutamate-induced delayed calcium deregulation by 2-APB and La3+ in cultured cortical neurones: C. Chinopoulos, et al.; J. Neurochem. 91, 471 (2004) Abstract
2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3: M.K. Chung, et al.; J. Neurosci. 24, 5177 (2004) Abstract; Full Text
The blocking of capacitative calcium entry by 2-aminoethyl diphenylborate (2-APB) and carboxyamidotriazole (CAI) inhibits proliferation in Hep G2 and Huh-7 human hepatoma cells: A. Enfissi, et al.; Cell Calcium 36, 459 (2004) Abstract
Induction of cholestasis in the perfused rat liver by 2-aminoethyl diphenylborate, an inhibitor of the hepatocyte plasma membrane Ca2+ channels: R.B. Gregory, et al.; J. Gastroenterol. Hepatol. 19, 1128 (2004) Abstract
2-aminoethoxydiphenyl borate inhibits agonist-induced Ca2+ signals by blocking inositol trisphosphate formation in acutely dissociated mouse pancreatic acinar cells: J. Wu, et al.; Pflugers Arch. 448, 592 (2004) Abstract
2-aminoethoxydiphenyl borate stimulates pulmonary C neurons via the activation of TRPV channels: Q. Gu, et al.; Am. J. Physiol. Lung Cell Mol. Physiol. 288, L392 (2005) Abstract
2-Aminoethoxydiphenyl borate perturbs hormone-sensitive calcium stores and blocks store-operated calcium influx pathways independent of cytoskeletal disruption in human A549 lung cancer cells: S. Padar, et al.; Biochem. Pharmacol. 69, 1177 (2005) Abstract
Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect: S.Z. Xu, et al.; Br. J. Pharmacol. 145, 405 (2005) Abstract; Full Text
2-Aminoethoxydiphenyl borate (2-APB) stimulates a conformationally coupled calcium release pathway in the NG115-401L neuronal cell line: D.D. Bose & D.W. Thomas; Neuropharmacology 50, 532 (2006) Abstract
2-aminoethoxydiphenyl borate as a prototype drug for a group of structurally related calcium channel blockers in human platelets: Y. Dobrydneva, et al.; Mol. Pharmacol. 69, 247 (2006) Abstract
 
 
ALX-550-237 Revised 18-Jan-05
Bepridil . hydrochloride
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SYNONYMS 1-Isobutoxy-2-pyrrolidino-3-(N-benzylanilino)propane . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-550-237-M010   10 mg 25.00 USD Add To Cart
ALX-550-237-M025   25 mg 55.00 USD Add To Cart
Product Specification
FORMULA: C24H34N2O . HCl
MW: 366.6 . 36.5
CAS NUMBER: 74764-40-2
MERCK INDEX: 14: 1150
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in 100% ethanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Store tightly sealed.

Product Description
Non-selective Ca2+ channel blocker. Stimulates the binding of 1,4-dihydropyridine-based drugs to Ca2+ channels. Inhibits Na+/Ca2+ exchange.
Product Specific Literature References
Characterization and photoaffinity labeling of receptor sites for the Ca2+ channel inhibitors d-cis-diltiazem, (+/-)-bepridil, desmethoxyverapamil, and (+)-PN 200-110 in skeletal muscle transverse tubule membranes: J.P. Galizzi, et al.; J. Biol. Chem. 261, 1393 (1986) Abstract; Full Text
Drug action and cellular calcium regulation: R. Janis, et al.; Adv. Drug Res. 16, 309 (1987)
Bepridil as an antisickling agent: membrane internalization and cell rigidity: R.M. Johnson, et al.; Am. J. Hematol. 46, 310 (1994) Abstract
Intracellular Ca2+ mediates the cytotoxicity induced by bepridil and benzamil in human brain tumor cells: Y.S. Lee, et al.; Cancer Lett. 88, 87 (1995) Abstract
 
 
ALX-550-322 Revised 11-Nov-08
Caffeine
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SYNONYMS 1,3,7-Trimethylxanthine
3,7-Dihydro-1,3,7-trimethyl-1H-purine-2,6-dione
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-550-322-G005   5 g 10.00 USD Add To Cart
Product Specification
FORMULA: C8H10N4O2
MW: 194.2
CAS NUMBER: 58-08-2
MERCK INDEX: 14: 1636
SOURCE/HOST: Found in tea leaves, coffee beans, cocoa beans, maté leaves, guarana paste and kola nuts.
PURITY: ≥99%
APPEARANCE: White to colorless powder.
SOLUBILITY: Soluble in chloroform, 100% alcohol or hot water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: HARMFUL.
IDENTITY: Identity determined by NIR.

Product Description
CNS stimulant. Blocks adenosine A1 and A2A receptors. cAMP phosphodiesterase inhibitor. Interferes with the uptake and storage of Ca2+ by the sarcoplasmic reticulum in skeletal muscle. Prevents apoptosis and cell cycle effects induced by various chemicals. Inhibits cellular DNA repair mechanisms. Anti-inflammatory.
Product Specific Literature References
Analogues of caffeine and theophylline: effect of structural alterations on affinity at adenosine receptors: J.W. Daly, et al.; J. Med. Chem. 29, 1305 (1986) Abstract
Caffeine as an analgesic adjuvant: a review of pharmacology and mechanisms of action: J. Sawynok & T.L. Yaksh; Pharmacol. Rev. 45, 43 (1993) Abstract
Caffeine prevents apoptosis and cell cycle effects induced by camptothecin or topotecan in HL-60 cells: F. Traganos, et al.; Cancer Res. 53, 4613 (1993) Abstract
Multiple effects of caffeine on calcium current in rat ventricular myocytes: I. Zahradnik & P. Palade; Pfluegers Arch. 424, 129 (1993) Abstract
Acute effects of caffeine on arterial stiffness, wave reflections, and central aortic pressures: T.G. Papaioannou, et al.; Am. J. Hypertens. 18, 129 (2005), (Review) Abstract
Caffeine and the dopaminergic system: O. Cauli & M. Morelli; Behav. Pharmacol. 16, 63 (2005), (Review) Abstract
Immunomodulatory effects of caffeine: friend or foe: L. A. Horrigan, et al.; Pharmacol. Ther. 111, 877 (2006), (Review) Abstract
Novel neuroprotection by caffeine and adenosine A(2A) receptor antagonists in animal models of Parkinson’s disease: A. Kalda, et al.; J. Neurol. Sci. 248, 9 (2006), (Review) Abstract
The enigmatic effects of caffeine in cell cycle and cancer: A. M. & Bode and Z. Dong; Cancer Lett. 247, 26 (2007), (Review) Abstract
 
 
ALX-550-072 Revised 28-Jan-05
Dantrolene . sodium salt
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-550-072-M010   10 mg 14.00 USD Add To Cart
ALX-550-072-M050   50 mg 32.00 USD Add To Cart
Product Specification
FORMULA: C14H9N4O5Na
MW: 336.2
CAS NUMBER: 14663-23-1
MERCK INDEX: 14: 2816
PURITY: ≥99%
APPEARANCE: Orange solid.
SOLUBILITY: Soluble in DMSO; insoluble in dilute aqueous base or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Inhibitor of Ca2+ release from intracellular stores, probably by binding to the ryanodine receptor. Intracellularly acting muscle relaxant.
Product Specific Literature References
1-[(5-arylfurfurylidene)amino]hydantoins. A new class of muscle relaxants: Snyder, et al.; J. Med. Chem. 10, 807 (1967) Abstract
Dantrolene. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in malignant hyperthermia, the neuroleptic malignant syndrome and an update of its use in muscle spasticity: A. Ward, et al.; Drugs 32, 130 (1986) Abstract
Dantrolene sodium diminishes exercise-induced muscle damage in the rat: G.J. Amelink, et al.; Eur. J. Pharmacol. 179, 187 (1990) Abstract
Inhibitory action of dantrolene on Ca-induced Ca2+ release from sarcoplasmic reticulum in guinea pig skeletal muscle: T. Ohta, et al.; Eur. J. Pharmacol. 178, 11 (1990) Abstract
Mobilization of dantrolene-sensitive intracellular calcium pools is involved in the cytotoxicity induced by quisqualate and N-methyl-D-aspartate but not by 2amino3(3hydroxy5methylisoxazol4yl)propionate and kainate in cultured cerebral cortical neurons: A. Frandsen & A. Schousboe; PNAS 89, 2590 (1992) Abstract
Increased intracellular Ca2+: a critical link in the pathophysiology of sepsis?: S.K. Song, et al.; PNAS 90, 3933 (1993) Abstract
Possible mechanism of dantrolene stabilization of cultured neuroblastoma cell plasma membranes: T. Hayashi, et al.; J. Neurochem. 63, 1849 (1994) Abstract
NMDA receptor-dependent excitotoxicity: the role of intracellular Ca2+ release: I. Mody & J.F. McDonald; TIPS 16, 356 (1995), (Review) Abstract
 
 
ALX-550-264 Revised 13-Nov-02
Dotarizine
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SYNONYMS 1-(Diphenylmethyl)-4-[3-(2-phenyl-1,3-dioxolan-2-yl)]piperazine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-550-264-M005   5 mg 80.00 USD Add To Cart
ALX-550-264-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C29H34N2O2
MW: 442.6
CAS NUMBER: 84625-59-2
MERCK INDEX: 14: 3428
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Blocks Ca2+ entry through Ca2+ channels.
Product Specific Literature References
Effects of dotarizine on 45Ca2+ movements and contractile responses in vascular smooth muscle: T. Tejerina, et al.; Eur. J. Pharmacol. 239, 75 (1993) Abstract
 
 
ALX-340-010 Revised 28-Feb-07
ETYA
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SYNONYMS 5,8,11,14-Eicosatetraynoic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Lipoxygenases / Related Products
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ALX-340-010-M005   5 mg 40.00 USD Add To Cart
ALX-340-010-M025   25 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C20H24O2
MW: 296.5
CAS NUMBER: 1191-85-1
PURITY: ≥95%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, DMSO, acetone or acetonitrile.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: We do not recommend storing the solutions for more than one day.
HANDLING: Protect from light and oxygen.
HAZARD: TOXIC.

Product Description
Inhibits arachidonic acid uptake. Inhibitor of lipoxygenases, cyclooxygenases (COX), phospholipase A2 and cytochrome P450. Modulates Ca2+ entry into cells. Stimulates luteinizing hormone release from cultured pituitary cells. PPAR agonist.
Product Specific Literature References
Structural requirements of acetylenic fatty acids for inhibition of soybean lipoxygenase and prostaglandin synthetase: D.T. Downing, et al.; Biochim. Biophys. Acta 280, 343 (1972) Abstract
The effect of 5,8,11,14-eicosatetraynoic acid on lipid metabolism: L.D. Tobias & J.G. Hamilton; Lipids 14, 181 (1979) Abstract
An inhibitor of arachidonic acid metabolism stimulates luteinizing hormone (LH) release from cultured pituitary cells: P.M. Conn, et al.; Prostaglandins 19, 873 (1980) Abstract
Evidence for inhibition of leukotriene A4 synthesis by 5,8,11,14-eicosatetraynoic acid in guinea pig polymorphonuclear leukocytes: G.M. Bokoch & P.W. Reed; J. Biol. Chem. 256, 4156 (1981) Abstract; Full Text
Phospholipase A2-induced rat mast cell secretion. Role of arachidonic acid metabolites: E.Y. Chi, et al.; Lab. Invest. 47, 579 (1982) Abstract
Epoxyeicosatrienoic acids stimulate glucagon and insulin release from isolated rat pancreatic islets: J.R. Falck, et al.; BBRC 114, 743 (1983) Abstract
The mechanism of inactivation of lipoxygenases by acetylenic fatty acids: H. Kühn, et al.; Eur. J. Biochem. 139, 577 (1984) Abstract
Comparative effects of indomethacin, acetylenic acids, 15-HETE, nordihydroguaiaretic acid and BW755C on the metabolism of arachidonic acid in human leukocytes and platelets: H. Salari, et al.; Prostagl. Leukotr. Med. 13, 53 (1984) Abstract
Incorporation of 5,8,11,14-eicosatetraynoic acid (ETYA) into cell lipids: competition with arachidonic acid for esterification: A.S. Taylor, et al.; Prostaglandins 29, 449 (1985) Abstract
Inhibition of U937 eicosanoid and DNA synthesis by 5,8,11,14- eicosatetraynoic acid, an inhibitor of arachidonic acid metabolism and its partial reversal by leukotriene C4: F. Ondrey, et al.; Cancer Res. 49, 1138 (1989) Abstract
Effects of 5,8,11,14-eicosatetraynoic acid on thapsigargin-induced calcium entry, and intracellular pH in thyroid FRTL-5 cells: E. Ekokoski & K. Tornquist; Biochim. Biophys. Acta 1223, 274 (1994) Abstract
 
 
ALX-157-003 Revised 03-Mar-05
Galanin (human)
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PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Galanin & Galanin Receptor / Related Products
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ALX-157-003-PC05   0.5 mg* 190.00 USD Add To Cart
ALX-157-003-P001   1 mg* 280.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-His-Ala-Val-Gly-Asn-His-Arg-Ser-Phe-Ser-Asp-Lys-Asn-Gly-Leu-Thr-Ser-OH
FORMULA: C139H210N42O43
MW: 3157.4
CAS NUMBER: 119418-04-1
QUANTITY: *Sold as net peptide weight.
PURITY: ≥98%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Specific Literature References
Galanin: profile of a new neuropeptide: L.W. Haynes; TIPS 7, 214 (1986), (Review)
Galanin - a newly isolated biologically active neuropeptide: A. Rökaeus; Trends Neurosci. 10, 158 (1987)
Galanin and the endocrine pancreas: B. Ahren, et al.; FEBS Lett. 229, 233 (1988) Abstract
Galanin. A selective inhibitor of insulin secretion?: J. Dupré; Pancreas 3, 119 (1988) Abstract
Co-existence of galanin and acetylcholine: is galanin involved in memory processed and dementia?: J.N. Crawley & G.L. Wenk; TINS 12, 278 (1989) Abstract
Inhibitory action of galanin on gastric acid secretion in pentobarbital-anesthetized rats: W.J. Rossowski & D.H. Coy; Life Sci. 44, 1807 (1989) Abstract
Galanin in the porcine pancreas: T. Messell, et al.; Regul. Pept. 28, 161 (1990) Abstract
Human galanin: primary structure and identification of two molecular forms: M. Bersani, et al.; FEBS Lett. 283, 189 (1991) Abstract
Isolation and primary structure of pituitary human galanin, a 30- residue nonamidated neuropeptide: W.E. Schmidt, et al.; PNAS 88, 11435 (1991) Abstract
Human galanin: molecular cloning reveals a unique structure: H.F. Evans & J. Shine; Endocrinology 129, 1682 (1991) Abstract
Further Categories Containing This Product:
PeptidesCa2+ ModulatorsNeuropeptides & Receptors Other Products
 
 
ALX-157-004 Revised 29-Nov-02
Galanin (pig)
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PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Galanin & Galanin Receptor / Related Products
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ALX-157-004-PC05   0.5 mg* 180.00 USD Add To Cart
ALX-157-004-P001   1 mg* 290.00 USD Add To Cart
Product Specification
SEQUENCE: H-Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-His-Ala-Ile-Asp-Asn-His-Arg-Ser-Phe-His-Asp-Lys-Tyr-Gly-Leu-Ala-NH2
FORMULA: C146H213N43O40
MW: 3210.6
CAS NUMBER: 88813-36-9
QUANTITY: *Sold as net peptide weight.
PURITY: ≥98%
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
Product Description
For reviews see Galanin (human) (Prod. No. ALX-157-003).
Product Specific Literature References
Galanin - a novel biologically active peptide from porcine intestine: K. Tatemoto, et al.; FEBS Lett. 164, 124 (1983) Abstract
Further Categories Containing This Product:
PeptidesCa2+ Modulators
 
 
ALX-550-270 Revised 22-May-07
Glibenclamide
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SYNONYMS Glyburide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY K+ Channel Blockers & Inhibitors
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ALX-550-270-G001   1 g 17.00 USD Add To Cart
Product Specification
FORMULA: C23H28ClN3O5S
MW: 494.0
CAS NUMBER: 10238-21-8
MERCK INDEX: 14: 4478
RTECS: YS4725200
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (25mg/ml) or 100% ethanol (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Solutions are stable for up to 3 months when stored at -20°C.
HAZARD: HARMFUL.

Product Description
ATP-dependent K+ channel blocker in the pancreas, which in turn causes intracellular Ca2+ levels to rise and for insulin to be secreted. Antidiabetic. High affinity binding sites have been identified in the cardiovascular system, the CNS, and pancreatic beta cells. Large potency differences are observed between pancreatic tissue and vascular tissue.
Product Specific Literature References
Glipizide: a review of its pharmacological properties and therapeutic use: R.N. Brogden, et al.; Drugs 18, 329 (1979) Abstract
Intracellular ATP directly blocks K+ channels in pancreatic B-cells: D.L. Cook & C.N. Hales; Nature 311, 271 (1984) Abstract
Antidiabetic sulfonylureas control action potential properties in heart cells via high affinity receptors that are linked to ATP-dependent K+ channels: M. Fosset, et al.; J. Biol. Chem. 263, 7933 (1988) Abstract; Full Text
In vitro effects of sulfonylurea on glucose transport and translocation of glucose transporters in adipocytes from streptozocin-induced diabetic rats: D.R. Jacobs, et al.; Diabetes 38, 205 (1989) Abstract
Glyburide blocks the relaxation response to BRL 34915 (cromakalim), minoxidil sulfate and diazoxide in vascular smooth muscle: R.J. Winquist, et al.; J. Pharmacol. Exp. Ther. 248, 149 (1989) Abstract
Potassium channel modulators: scientific applications and therapeutic p