title: Autoregulation of histamine release via the histamine H3 receptor on mast cells in the rat skin.
abstract: The autoregulation of the histamine release via the histamine H3 receptor in the periphery was studied in vivo and in vitro. Antidromic electrical stimulation of the sciatic nerve caused a significant increase in histamine release in the subcutaneous perfusate in the rat hindpaw. (R)alpha-methylhistamine, a specific H3 receptor agonist, significantly and dose-dependently inhibited the increase in release of histamine by antidromic stimulation at intravenous doses of 0.25-2 mg/kg. Thioperamide (2 mg/kg, intraperitoneally), a specific H3 antagonist, prevented the inhibitory effect of (R)alpha-methylhistamine. Substance P perfusion (5-50 microM) also elicited a significant increase in histamine, and a significant inhibition by (R)alpha-methylhistamine and the antagonism of thioperamide were observed. (R)alpha-methylhistamine inhibited the histamine release by substance P from rat peritoneal mast cells in vitro, and thioperamide reduced the response to (R)alpha-methylhistamine. These data suggest that mast cells may have histamine H3 receptors, and that histamine probably modulates its own release through the H3 receptor in neurogenic inflammation.
authors.affiliation: Department of Pharmacology, Fukuoka Dental College, Japan.
authors.forename: T
authors.initials: T
authors.lastname: Ohkubo
authors.forename: M
authors.initials: M
authors.lastname: Shibata
authors.forename: M
authors.initials: M
authors.lastname: Inoue
authors.forename: H
authors.initials: H
authors.lastname: Kaya
authors.forename: H
authors.initials: H
authors.lastname: Takahashi
mesh_terms: D000704:Analysis of Variance; D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004305:Dose-Response Relationship, Drug; D004558:Electric Stimulation; D017442:Histamine Agonists / Q000008:administration & dosage / Q000494:pharmacology; D006633:Histamine Antagonists; D006636:Histamine Release / Q000187:drug effects*; D006706:Homeostasis; D007274:Injections, Intraperitoneal; D007275:Injections, Intravenous; D007279:Injections, Subcutaneous; D008297:Male; D008407:Mast Cells / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D008761:Methylhistamines / Q000008:administration & dosage / Q000494:pharmacology; D010880:Piperidines / Q000008:administration & dosage / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D018100:Receptors, Histamine H3 / Q000502:physiology*; D012584:Sciatic Nerve / Q000187:drug effects / Q000502:physiology; D012867:Skin / Q000187:drug effects / Q000378:metabolism; D013237:Stereoisomerism; D013373:Substance P / Q000494:pharmacology
chemical_list: D017442:Histamine Agonists; D006633:Histamine Antagonists; D008761:Methylhistamines; D010880:Piperidines; D018100:Receptors, Histamine H3; D013373:Substance P; C069357:alpha-methylhistamine; C052075:thioperamide