Search results for "Impromidine"

showing 2 items of 2 documents

Responses to histamine and selective H2-receptor agonists in lung parenchymal strips from normal and sensitized guinea-pigs.

1989

Histamine produces concentration-dependent contractions of lung parenchyma strips obtained from normal and sensitized guinea-pigs. The responsiveness of the sensitized lung strips to histamine was significantly increased compared to normal tissues. Clemizole (0.1 microM) was equally effective as an H1-antagonist in normal (dose-ratio 9.12) and sensitized (dose-ratio 9.77) tissues. The concentration-response curves to histamine were displaced to the left by cimetidine (0.1 microM to 0.1 mM) with similar dose-ratios in normal and sensitized tissues. Cimetidine enhanced maximal responses to histamine only in normal lung strips. The effects of submaximal equieffective concentrations of histamin…

Malemedicine.medical_specialtyImmunologyGuinea PigsToxicologyGuanidineschemistry.chemical_compoundImpromidineHistamine H2 receptorDimapritInternal medicineParenchymamedicineAnimalsPharmacology (medical)Receptors Histamine H2CimetidineLungPharmacologyLungDose-Response Relationship Drugbusiness.industryMethylhistaminesImidazolesIsoproterenolThioureaMuscle SmoothImpromidineDimapritClemizolemedicine.anatomical_structureEndocrinologychemistryBenzimidazolesbusinessCimetidineHistaminemedicine.drugHistamineMuscle ContractionAgents and actions
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Histamine analogues. 32nd communication: synthesis and pharmacology of sopromidine, a potent and stereoselective isomer of the achiral H2-agonist imp…

1989

Abstract Synthesis and pharmacology of sopromidine (( R )-7) and ( S )- 7 , 2 position isomers of impromidine derived from the enantiomeric α-methylhistamines, are reported. The enantiomers of 7 show high stereoselectivity at the atrial H 2 -receptor of the guinea-pig. ( R )- 7 is revealed to be a full H 2 -agonist with 7.4-fold potency relative to histamine, while ( S )- 7 is a competitive H 2 -antagonist.

PharmacologyAgonistChemistrymedicine.drug_classStereochemistryOrganic ChemistryBiological activityGeneral MedicinePharmacologychemistry.chemical_compoundImpromidineDrug DiscoverymedicinePotencyStereoselectivityEnantiomerReceptorHistaminemedicine.drugEuropean Journal of Medicinal Chemistry
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