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Chemical Compound Review

Procorum     5-[2-(3,4- dimethoxyphenyl)ethyl- methyl...

Synonyms: Gallopamil HCl, AGN-PC-00JXDY, SureCN194931, AG-E-16062, CHEMBL1256940, ...
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  • Calcium uptake produced by a potassium contracture in isolated frog twitch fibers was 6.7 +/- 0.8 pmol in 0.7 cm of fiber (mean +/- SEM, 21 observations) in the presence of 30 microM D600 [1].
  • 4. The rate-dependent acidosis was inhibited by the organic calcium antagonist D600 (20 mumol l-1) which also inhibited twitch tension [2].
  • The Ca2+ channel blockers D600 and verapamil reversed the suppressive effects of hypoxia [3].
  • Blocking Ca(2+) influx by D600 did not diminish secretagogue-associated toxicity [4].
  • The differential inhibitory effects of D600 on antigen-induced mediator release vs the smooth muscle effects of the various agonists may suggest multiple mechanisms of release or sources of mediators in human airway anaphylaxis [5].

High impact information on GALLOPAMIL HYDROCHLORIDE

  • Based on this information, we have identified two aspartic acid residues in RAG1 (D600 and D708) that function specifically in catalysis [6].
  • Lanthanum and D600, under conditions in which their access to the plasmalemma has been facilitated by pretreating the cells with cutinase, also markedly extend metaphase and in several instances permanently arrest cells [7].
  • Charge movement in skeletal muscle fibers paralyzed by the calcium-entry blocker D600 [8].
  • We analyzed two conditional RAG-1 mutants that affect residues quite close in the primary sequence to an active site amino acid (D600), and we found that they exhibit severely impaired recombination in the presence of certain cleavage site sequences [9].
  • Partial inhibition of Ca2+ current by methoxyverapamil (D600) reveals spatial nonuniformities in [Ca2+]i during excitation-contraction coupling in cardiac myocytes [10].

Chemical compound and disease context of GALLOPAMIL HYDROCHLORIDE



  • D600-induced depression of Isi is shown to be greater after a depolarization (action potential or clamp pulse) than before [14].
  • The nicotinic receptor antagonist tubocurarine (4 x 10(-7) M) and the Ca2+ channel blocker D600 (10(-5) M) prevent the subsequent rise of Penk mRNA levels after challenge with nicotine, when given within the lag phase (0-6 h), suggesting the need of continuous receptor occupation and Ca2+ entry for induction of gene expression [15].
  • Activation of 28Mg efflux by Na+/o follows hyperbolic kinetics, with Mg2+/o reducing the affinity of the system for Na+/o. Lanthanum and D600 reversibly inhibit Mg efflux [16].
  • KCl stimulated Ser-133 phosphorylation of cAMP response element-binding protein (CREB) in chromaffin cells, and CREB phosphorylation was blocked by both ascomycin and D600 [17].
  • The Ca2+ channel blocker D600 decreased both the cell fusion and the normal rise in cGMP levels [18].


  • Mechanism of calcium channel block by D600 in single smooth muscle cells from rabbit ear artery [19].
  • These findings are compatible with the hypothesis that the primary mode of action of D600 is to inhibit Ca2+ entry in the B-cell [20].
  • The association of 125I-labelled LDL with HeLa cells was increased in proportion to the concentration of D600, and 125I-labelled LDL was accumulated in lysosomal fractions as assessed by Percoll density gradient analysis [21].
  • Although D600 is not now considered a specific blocker, its effect has suggested the involvement of Ca2+ channels in the acrosome reaction [22].
  • Veratridine increased 45Ca uptake into the isolated neurohypophysis and the increase could be prevented by addition of tetrodotoxin or D600 to the medium [23].

Associations of GALLOPAMIL HYDROCHLORIDE with other chemical compounds

  • The recognition of glucose by the B-cell was also unaffected by D600 as judged by the effect of the sugar upon both 45calcium efflux and net uptake in the isolated islets [20].
  • The mechanism by which the phenylalkylamines, verapamil and D600, and related compounds, block inactivating delayed rectifier K+ currents in rat alveolar epithelial cells, was investigated using whole-cell tight-seal recording [24].
  • Redistribution of PKC in response to Buserelin is inhibited by the calcium ion channel antagonist methoxyverapamil (D600), suggesting that redistribution of PKC activity, like GnRH-stimulated gonadotropin release, requires the influx of extracellular calcium [25].
  • LH synthesis and release were measured after a 4-h treatment of cells with gallopamil hydrochloride (D600; 1 and 100 microM), a Ca2+ channel blocker, or pimozide (0.5 and 5.0 microM), a calmodulin inhibitor, with or without 1 nM GnRH [26].
  • The P/Q-type Ca(2+) channel blocker omega-agatoxin TK (500 nM) and the L-type Ca(2+) channel blocker nifedipine (20 microM) had no effect on the Ca(2+) transient, whereas the L-type Ca(2+) channel blocker methoxyverapamil (D600, 0.5-1 mM) irreversibly reduced the Ca(2+) transient by 37% in axons and by 42% in dendrites [27].


  • Although treatment with either 1 mM 8Br-cAMP or 1 mM 8Br-GMP failed to increase mAChR number, treatment with either the inorganic Ca2+ channel blocker Co2+ (1 mM) or the organic Ca2+ channel antagonist D600 (10-100 microM) produced 40-80% increases in mAChR number [28].
  • The time course and efficacy of LH release in response to GnRH and to MTX are similar; both secretagogues require extracellular Ca2+ and are inhibited by the selective Ca2+ ion channel antagonist methoxyverapamil (D600) [29].
  • Treatment of cells with D600 partially blocked CRF-stimulated elevation of POMC mRNA and forskolin-stimulated elevation of PRL mRNA [30].
  • An oxytocin antagonist (1 mumol/l solution) significantly reduced basal oxytocin release and blocked the stimulatory effect normally induced by exogenous oxytocin, as did gallopamil hydrochloride (D600, 10 mumol/l solution), a Ca2+ channel blocker, or incubation in a Ca2+-free medium [31].
  • This increase in ProEnk A and PNMT mRNA levels was however less affected by D600 [32].

Analytical, diagnostic and therapeutic context of GALLOPAMIL HYDROCHLORIDE

  • This effect was not dependent on the presence of D600 (methoxyverapamil) or continuous coronary perfusion [33].
  • This study investigated the action of the calcium antagonist D600 on calcium channel currents recorded in high barium solution from single, enzymatically isolated smooth muscle cells from the rabbit ear artery using the whole cell configuration of the patch-clamp technique [19].
  • First, in static cultures we used a specific Ca+2 ion channel blocker, methoxyverapamil (D600), to block entry of extracellular Ca+2 into pituitary cell cultures to determine if brief elevation of intracellular Ca+2 (whether derived from external or internal sources) could support continued gonadotropin release [34].
  • D890, a derivative of the Ca2+ channel antagonist D600, was intracellularly applied from conventional microelectrodes into pyramidal neurons of neocortical slices [35].
  • Methoxyverapamil (D600) in zero Ca2+o did not affect HV in lamprey DA, nor did it prevent further constriction when Ca2+o was restored during hypoxia in hagfish DA [36].


  1. Calcium influx in contracting and paralyzed frog twitch muscle fibers. Curtis, B.A., Eisenberg, R.S. J. Gen. Physiol. (1985) [Pubmed]
  2. Mechanism of rate-dependent pH changes in the sheep cardiac Purkinje fibre. Bountra, C., Kaila, K., Vaughan-Jones, R.D. J. Physiol. (Lond.) (1988) [Pubmed]
  3. Effects of D600 on hypoxic suppression of K+ currents in isolated type I carotid body cells of the neonatal rat. Peers, C. FEBS Lett. (1990) [Pubmed]
  4. Beta-cell toxicity of ATP-sensitive K+ channel-blocking insulin secretagogues. Rustenbeck, I., Krautheim, A., Jörns, A., Steinfelder, H.J. Biochem. Pharmacol. (2004) [Pubmed]
  5. Mode of action of calcium antagonists on responses to spasmogens and antigen challenge in human airway smooth muscle. Kannan, M.S., Davis, C. Respiration physiology. (1988) [Pubmed]
  6. Identification of two catalytic residues in RAG1 that define a single active site within the RAG1/RAG2 protein complex. Fugmann, S.D., Villey, I.J., Ptaszek, L.M., Schatz, D.G. Mol. Cell (2000) [Pubmed]
  7. Calcium restriction prolongs metaphase in dividing Tradescantia stamen hair cells. Hepler, P.K. J. Cell Biol. (1985) [Pubmed]
  8. Charge movement in skeletal muscle fibers paralyzed by the calcium-entry blocker D600. Hui, C.S., Milton, R.L., Eisenberg, R.S. Proc. Natl. Acad. Sci. U.S.A. (1984) [Pubmed]
  9. Conditional RAG-1 mutants block the hairpin formation step of V(D)J recombination. Kale, S.B., Landree, M.A., Roth, D.B. Mol. Cell. Biol. (2001) [Pubmed]
  10. Partial inhibition of Ca2+ current by methoxyverapamil (D600) reveals spatial nonuniformities in [Ca2+]i during excitation-contraction coupling in cardiac myocytes. Cheng, H., Cannell, M.B., Lederer, W.J. Circ. Res. (1995) [Pubmed]
  11. Potassium and caffeine contractures in fast and slow muscles of the chicken. Huerta, M., Stefani, E. J. Physiol. (Lond.) (1981) [Pubmed]
  12. The tension-depolarization relationship of frog atrial trabeculae as determined by potassium contractures. Chapman, R.A., Tunstall, J. J. Physiol. (Lond.) (1981) [Pubmed]
  13. Effects of papaverine on isolated rabbit papillary muscle. Endoh, M., Schümann, H.J. Eur. J. Pharmacol. (1975) [Pubmed]
  14. Interval- and voltage-dependent effects of the calcium channel-blocking agents D600 and AQA 39 on mammalian ventricular muscle. Trautwein, W., Pelzer, D., McDonald, T.F. Circ. Res. (1983) [Pubmed]
  15. Mechanisms involved in the transcriptional activation of proenkephalin gene expression in bovine chromaffin cells. Farin, C.J., Kley, N., Höllt, V. J. Biol. Chem. (1990) [Pubmed]
  16. Axoplasmic free magnesium levels and magnesium extrusion from squid giant axons. De Weer, P. J. Gen. Physiol. (1976) [Pubmed]
  17. A calcium-initiated signaling pathway propagated through calcineurin and cAMP response element-binding protein activates proenkephalin gene transcription after depolarization. Hahm, S.H., Chen, Y., Vinson, C., Eiden, L.E. Mol. Pharmacol. (2003) [Pubmed]
  18. Involvement of cyclic GMP in the fusion of chick embryonic myoblasts in culture. Choi, S.W., Baek, M.Y., Kang, M.S. Exp. Cell Res. (1992) [Pubmed]
  19. Mechanism of calcium channel block by D600 in single smooth muscle cells from rabbit ear artery. Hering, S., Bolton, T.B., Beech, D.J., Lim, S.P. Circ. Res. (1989) [Pubmed]
  20. Calcium-antagonists and islet function. IV. Effect of D600. Malaisse, W.J., Devis, G., Pipeleers, D.G., Somers, G. Diabetologia (1976) [Pubmed]
  21. The effect of calcium antagonists on the proteolytic degradation of low-density lipoprotein in HeLa cells. Akiyama, S., Tomita, K., Kuwano, M. Exp. Cell Res. (1985) [Pubmed]
  22. High pH-induced acrosome reaction and Ca2+ uptake in sea urchin sperm suspended in Na+-free seawater. García-Soto, J., Darszon, A. Dev. Biol. (1985) [Pubmed]
  23. Effects of veratridine on Ca fluxes and the release of oxytocin and vasopressin from the isolated rat neurohypophysis. Nordmann, J.J., Dyball, R.E. J. Gen. Physiol. (1978) [Pubmed]
  24. Mechanism of K+ channel block by verapamil and related compounds in rat alveolar epithelial cells. DeCoursey, T.E. J. Gen. Physiol. (1995) [Pubmed]
  25. Hormone-stimulated redistribution of gonadotrope protein kinase C in vivo: dependence on Ca2+ influx. McArdle, C.A., Conn, P.M. Mol. Pharmacol. (1986) [Pubmed]
  26. Synthesis and release of luteinizing hormone in vitro by rat anterior pituitary cells: effects of gallopamil hydrochloride (D600) and pimozide. Liu, T.C., Jackson, G.L. Endocrinology (1985) [Pubmed]
  27. Calcium transients in subcompartments of the leech Retzius neuron as induced by single action potentials. Beck, A., Lohr, C., Deitmer, J.W. J. Neurobiol. (2001) [Pubmed]
  28. Regulation of muscarinic acetylcholine receptor number in cultured neuronal cells by chronic membrane depolarization. Liles, W.C., Nathanson, N.M. J. Neurosci. (1987) [Pubmed]
  29. Homologous desensitization with gonadotropin-releasing hormone (GnRH) also diminishes gonadotrope responsiveness to maitotoxin: a role for the GnRH receptor-regulated calcium ion channel in mediation of cellular desensitization. Conn, P.M., Staley, D.D., Yasumoto, T., Huckle, W.R., Janovick, J.A. Mol. Endocrinol. (1987) [Pubmed]
  30. Calcium-independent and calcium-dependent mechanisms regulate corticotropin-releasing factor-stimulated proopiomelanocortin peptide secretion and messenger ribonucleic acid production. Dave, J.R., Eiden, L.E., Lozovsky, D., Waschek, J.A., Eskay, R.L. Endocrinology (1987) [Pubmed]
  31. Release of oxytocin and vasopressin by magnocellular nuclei in vitro: specific facilitatory effect of oxytocin on its own release. Moos, F., Freund-Mercier, M.J., Guerné, Y., Guerné, J.M., Stoeckel, M.E., Richard, P. J. Endocrinol. (1984) [Pubmed]
  32. Coordinate and differential regulation of proenkephalin A and PNMT mRNA expression in cultured bovine adrenal chromaffin cells: responses to secretory stimuli. Wan, D.C., Marley, P.D., Livett, B.G. Brain Res. Mol. Brain Res. (1991) [Pubmed]
  33. Synchronized repolarization after defibrillation shocks. A possible component of the defibrillation process demonstrated by optical recordings in rabbit heart. Dillon, S.M. Circulation (1992) [Pubmed]
  34. Calcium mobilization in the pituitary gonadotrope: relative roles of intra- and extracellular sources. Bates, M.D., Conn, P.M. Endocrinology (1984) [Pubmed]
  35. Effect of D890 on membrane properties of neocortical neurons. Deisz, R.A., Prince, D.A. Brain Res. (1987) [Pubmed]
  36. Intracellular and extracellular calcium utilization during hypoxic vasoconstriction of cyclostome aortas. Russell, M.J., Pelaez, N.J., Packer, C.S., Forster, M.E., Olson, K.R. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2001) [Pubmed]
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