PMID- 1713576 OWN - NLM STAT- MEDLINE DCOM- 19910830 LR - 20190918 IS - 0162-3109 (Print) IS - 0162-3109 (Linking) VI - 21 IP - 1 DP - 1991 Jan-Feb TI - Role of endoplasmic reticulum, an intracellular Ca2+ store, in histamine release from rat peritoneal mast cell. PG - 13-21 AB - By means of the Ca-antimonate precipitation technique, it was revealed that Ca2+ accumulates in the endoplasmic reticulum (ER) of rat peritoneal mast cells. The ER of rat mast cells was isolated using Percoll density gradient centrifugation, and its characteristics were studied. Although the uptake of 45Ca into the ER was enhanced by adenosine 5'-triphosphate (ATP) at concentrations lower than 2 mM, at higher concentrations ATP induced 45Ca release from the ER, suggesting that bidirectional translocation of Ca2+ takes place in the ER membrane. When apyrase was added to the reaction mixture to decompose all ATP molecules, the amount of 45Ca in the ER was decreased, indicating that ATP is necessary to retain Ca2+ in the ER. Not only inositol 1,4,5-trisphosphate (IP3) but also guanosine 5'-triphosphate (GTP) was effective in releasing Ca2+ from the ER at concentrations higher than 2 microM, while guanosine 5'-[gamma-thio]-triphosphate (GTP-gamma S), a non-hydrolysable analogue of GTP, was not effective. This may indicate that a hydrolysis of GTP is necessary for Ca2+ release from the ER. Intracellular Ca2+ blockers such as 8-(N,N-diethylamino)octyl-3,4,5-trimethoxybenzoate (TMB-8) and dantrolene sodium were effective in inhibiting Ca2+ release from ER induced by IP3. The Ca2+ release due to IP3 was also inhibited by flunarizine, a Ca2+ channel blocker, and by oxatomide, an antiallergic drug. Since these two compounds are diphenylpiperazine derivatives, it is suggested that a diphenylpiperazine moiety may be effective in inhibiting Ca2+ release from the ER. FAU - Yoshii, N AU - Yoshii N AD - Department of Pharmacology, Faculty of Pharmaceutical Sciences, Okayama University, Japan. FAU - Mio, M AU - Mio M FAU - Akagi, M AU - Akagi M FAU - Tasaka, K AU - Tasaka K LA - eng PT - Journal Article PL - Netherlands TA - Immunopharmacology JT - Immunopharmacology JID - 7902474 RN - 0 (Calcium Channel Blockers) RN - 86-01-1 (Guanosine Triphosphate) RN - 8L70Q75FXE (Adenosine Triphosphate) RN - SY7Q814VUP (Calcium) SB - IM MH - Adenosine Triphosphate/pharmacology MH - Animals MH - Calcium/*metabolism MH - Calcium Channel Blockers/pharmacology MH - Endoplasmic Reticulum/drug effects/physiology MH - Guanosine Triphosphate/pharmacology MH - Histamine Release/drug effects/*physiology MH - In Vitro Techniques MH - Male MH - Mast Cells/drug effects/immunology/*physiology MH - Rats MH - Rats, Inbred Strains EDAT- 1991/01/01 00:00 MHDA- 1991/01/01 00:01 CRDT- 1991/01/01 00:00 PHST- 1991/01/01 00:00 [pubmed] PHST- 1991/01/01 00:01 [medline] PHST- 1991/01/01 00:00 [entrez] AID - 0162-3109(91)90003-H [pii] AID - 10.1016/0162-3109(91)90003-h [doi] PST - ppublish SO - Immunopharmacology. 1991 Jan-Feb;21(1):13-21. doi: 10.1016/0162-3109(91)90003-h.