Different modes of action of the imidazoline compound RX871024 in pancreatic β-cells. Blocking of K+ channels, mobilization of Ca2+ from endoplasmic reticulum, and interaction with exocytotic machinery

Annals of the New York Academy of Sciences

Volumn 881, Issue , 1999, Pages 241-252

  Zaitsev, Sergei ^a,c   Efanov, A M ^a,c   Raap, A ^b   Efanova, I B ^a,c   Schloos, J ^b   Steckel Hamann, B ^b   Larsson, O ^a   Ostenson C G ^a   Berggren, P O ^a   Mest, H J ^b   Efendic, S ^a  

^a KAROLINSKA UNIVERSITY HOSPITAL   (Sweden)

^b BEIERSDORF AG   (Germany)

^c MOSCOW STATE UNIVERSITY   (Russian Federation)

Author keywords

[No Author keywords available]

Indexed keywords

2 (N PHENYLINDOYL)IMIDAZOLE; ALPHA 2 ADRENERGIC RECEPTOR; CALCIUM ION; CYTOCHROME P450; GLIBENCLAMIDE; GLUCOSE; IMIDAZOLINE DERIVATIVE; IMIDAZOLINE I1 RECEPTOR; IMIDAZOLINE I2 RECEPTOR; INSULIN; POTASSIUM CHANNEL; THAPSIGARGIN; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; BLOOD PRESSURE; CALCIUM CELL LEVEL; CALCIUM MOBILIZATION; CELL MEMBRANE POTENTIAL; CONFERENCE PAPER; CONTROLLED STUDY; DRUG MECHANISM; ENDOPLASMIC RETICULUM; EXOCYTOSIS; GLUCOSE BLOOD LEVEL; HEART RATE; INSULIN RELEASE; INTRAVENOUS DRUG ADMINISTRATION; MALE; MOUSE; NONHUMAN; PANCREAS ISLET BETA CELL; PROTEIN PHOSPHORYLATION; RAT;

ANIMALIA;

EID: 0032770202     PISSN: 00778923     EISSN: None     Source Type: Book Series    
DOI: 10.1111/j.1749-6632.1999.tb09366.x     Document Type: Conference Paper

References (26)

1. 2+ and pancreatic B-cell function. Biochem. Soc. Trans. 22: 12-18.
2. Ashcroft, S. J. H. 1994. Protein phosphorylation and beta-cell function. Diabetologia 37: S21-S29.
3. Ämmälä, C. et al. 1994. Activation of protein kinases and inhibition of protein phosphatases play a central role in the regulation of exocytosis in mouse pancreatic beta cells. Proc. Natl. Acad. Sci. USA 91: 4343-4347.
4. 2+ concentration and insulin secretion as evidenced from measurements in mouse single pancreatic islets. Proc. Natl. Acad. Sci. USA 92: 9412-9416.
5. Cerasi, E. et al. 1969. Role of adrenergic receptors in glucose-induced insulin secretion in man. Lancet 2: 301-302.
6. Efendic, S. et al. 1973. Effect of blockade of the alpha-adrenergic receptors on insulin response to glucose infusion in prediabetic subjects. Acta Endocrinol. 74: 542-547.
7. Efendic, S. et al. 1975. Effect of phentolamine and preperfusion with glucose on insulin release from the isolated perfused pancreas from fasted and fed rats. Diabetologia 11: 407-410.
8. Östenson, C. G. et al. 1988. Alpha 2-adrenoceptor blockade does not enhance glucose-induced insulin release in normal subjects or patients with noninsulin-dependent diabetes. J. Clin. Endocrinol. Metab. 67: 1054-1059.
9. Östenson, C. G. et al. 1989. Alpha-adrenoreceptors and insulin release from pancreatic islets of normal and diabetic rats. Am. J. Physiol. 257: E439-E443.
10. Schulz, A. & A. Hasselblatt. 1989. An insulin-releasing property of imidazoline derivatives is not limited to compounds that block alpha-adrenoceptors. Naunyn-Schmiedeberg's Arch. Pharmacol. 340: 321-327.
11. Schulz, A. & A. Hasselblatt. 1989. Dual action of clonidine on insulin release: Suppression, but stimulation when alpha 2-adrenoceptors are blocked. Naunyn-Schmiedeberg's Arch. Pharmacol. 340: 712-714.
12. 2-sites. Br. J. Pharmacol. 112: 1065-1070.
13. + channels in mouse pancreatic β-cells. Br. J. Pharmacol. 101: 115-120.
14. ATP channels in insulin secreting cells. Eur. J. Pharmacol. 204: 41-48.
15. Brown, C. A. et al. 1993. Antagonism of the stimulatory effects of efaroxan and glibenclamide in rat pancreatic islets by the imidazoline, RX801080. Br. J. Pharmacol. 110: 1017-1022.
16. ATP channels is mediated by Kir6.2. Proc. Natl. Acad. Sci. USA 94: 11716-11720.
17. ATP channels and interaction with exocytotic machinery. Diabetes 45: 1610-1618.
18. 2+, cyclic AMP, a phorbol ester and noradrenaline. Biochem. J. 254: 397-403.
19. Ashcroft, S. J. & M. Stubbs. 1987. The glucose sensor in HIT cells is the glucose transporter. FEBS Lett. 219: 311-315.
20. Efanov, A. M. et al. 1998. Signalling and sites of interaction for imidazoline and sulfonylurea in the stimulation of insulin release. Am. J. Physiol. 274 (Endocrinol. Metab. 37): E751-E757.
21. Tibirica, E. et al. 1991. An imidazoline-specific mechanism for the hypotensive effect of clonidine: A study with yohimbine and idazoxan. J. Pharmacol. Exp. Ther. 256: 606-613.
22. 1-imidazoline agonist. Cardiovasc. Drug Ther. 8: 27-41.
23. Rorsman, P. et al. 1992. Cytoplasmic calcium transients due to single action potentials and voltage-clamp depolarizations in mouse pancreatic B-cells. EMBO J. 8: 2877-2884.
24. 2+ mobilization from thapsigargin-sensitive stores in mouse pancreatic β-cells. Diabetes 47: 211-218.
25. + channels in mouse B cells. J. Clin. Invest. 89: 1288-1295.
26. 2+ and cyclic AMP in addition to inhibiting protein kinase C in rat islets of Langerhans. Mol. Cell. Endocrinol. 94: 55-60.