title: Antihistaminic activity of carane derivatives in isolated guinea pig ileum.
abstract: Local anesthetics (LAs) inhibit membrane depolarization by reducing sodium and potassium conductance, and subsequent displacement of calcium ions from binding sites seems to occur. Histamine release appears to be a secretory process in which calcium couples the stimulus to the exocytosis of histamine-containing granules. Furthermore, LAs are structurally similar to histamine H(1)-receptor antagonists. Thus, LAs can be considered antihistaminic drugs. Previous pharmacological investigations have shown strong local anesthetic, anti-inflammatory and analgesic activity of the carane derivative KP-23. As it has previously been demonstrated that KP-23R,S and its R,S-diasteroisomers have an inhibitory effect on guinea pig ileum contractions, the aim of the present study was to determine and compare the antihistaminic effects of KP-23R,S and its individual isomers KP-23R and KP-23S on isolated guinea pig ileum.
authors.affiliation: Department of Pharmacodynamics, Jagiellonian University, Medical College, Faculty of Pharmacy, Medyczna 7, PL 30-688 Kraków, Poland. mflibrow@kinga.cyf-kr.edu.pl
authors.forename: Tadeusz
authors.initials: T
authors.lastname: Librowski
authors.forename: Karolina
authors.initials: K
authors.lastname: Pytka
authors.forename: Marcin
authors.initials: M
authors.lastname: Szaleniec
mesh_terms: D000779:Anesthetics, Local / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000081008:Bicyclic Monoterpenes; D003514:Cyclohexylamines / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D006168:Guinea Pigs; D006633:Histamine Antagonists / Q000737:chemistry / Q000494:pharmacology*; D007082:Ileum / Q000187:drug effects* / Q000378:metabolism; D066298:In Vitro Techniques; D008012:Lidocaine / Q000494:pharmacology; D008297:Male; D011433:Propranolol / Q000494:pharmacology; D013237:Stereoisomerism
chemical_list: D000779:Anesthetics, Local; D000081008:Bicyclic Monoterpenes; D003514:Cyclohexylamines; D006633:Histamine Antagonists; C079300:4-(2-hydroxy-3-(N-isopropylamino)propoxyimino)carane; D008012:Lidocaine; D011433:Propranolol