Histamine affects release and biosynthesis of opioid peptides primarily via H1-receptors in bovine chromaffin cells.
Histamine is a potent secretagogue for opioid pentapeptides (Met- and Leu-enkephalin) in adrenal chromaffin cells in vitro. This effect is dependent on extracellular Ca2+ and is reduced by Ca2+ channel blockers such as Co2+, D 600, and nifedipine. Moreover, histamine also produced a profound compensatory increase in cellular peptide content after 48 h of exposure, most likely caused by a four- to fivefold increase in the mRNA levels coding for the proenkephalin A precursor. All the histamine-induced effects (acute release, changes in peptide cell content, proenkephalin A mRNA levels) are antagonized by the H1-receptor antagonist, clemastine, whereas the H2-receptor antagonists, ranitidine and cimetidine, were less effective (approximately 20% inhibition).
Bommer
M
M
Department of Neuropharmacology, Max-Planck-Institut für Psychiatrie, Martinsried, F.R.G.
Liebisch
D
D
Kley
N
N
Herz
A
A
Noble
E
E
D000311:Adrenal Glands / Q000187:drug effects / Q000378:metabolism*; D000818:Animals; D002118:Calcium / Q000502:physiology; D002417:Cattle; D002478:Cells, Cultured; D002838:Chromaffin System / Q000187:drug effects / Q000378:metabolism*; D002927:Cimetidine / Q000494:pharmacology; D002974:Clemastine / Q000494:pharmacology; D003035:Cobalt / Q000494:pharmacology; D004743:Enkephalin, Leucine / Q000096:biosynthesis*; D004744:Enkephalin, Methionine / Q000096:biosynthesis*; D004745:Enkephalins / Q000235:genetics; D005711:Gallopamil / Q000494:pharmacology; D006632:Histamine / Q000494:pharmacology*; D006633:Histamine Antagonists / Q000494:pharmacology; D009543:Nifedipine / Q000494:pharmacology; D011498:Protein Precursors / Q000235:genetics; D011738:Pyrilamine / Q000494:pharmacology; D012333:RNA, Messenger / Q000378:metabolism; D011899:Ranitidine / Q000494:pharmacology; D011968:Receptors, Histamine / Q000502:physiology*; D011969:Receptors, Histamine H1 / Q000502:physiology*
D004745:Enkephalins; D006633:Histamine Antagonists; D011498:Protein Precursors; D012333:RNA, Messenger; D011968:Receptors, Histamine; D011969:Receptors, Histamine H1; C029992:proenkephalin; D005711:Gallopamil; D003035:Cobalt; D004744:Enkephalin, Methionine; D004743:Enkephalin, Leucine; D002927:Cimetidine; D006632:Histamine; D011899:Ranitidine; D002974:Clemastine; C018021:cobaltous chloride; D011738:Pyrilamine; D009543:Nifedipine; D002118:Calcium