title: 1-[(IMIDAZOLIN-2-YL)AMINO]INDOLINE AND 1-[(IMIDAZOLIN-2 YL)AMINO] 1,2,3,4-TETRAHYDROQUINOLINE DERIVATIVES: NEW INSIGHTS INTO THEIR CIRCULATORY ACTIVITIES.
abstract: N-[(Imidazolin-2-yl)amino]indolines and N-[(imidazolin-2-yl)amino]-1,2,3,4-tetrahydroquinolines, previously described in patent literature as hypertensive agents, were synthesized and tested in viny for their affinities to α1- and α2-adrenoceptors as well as imidazoline I, and I2 receptors. The compounds most potent at either α1- or α2-adrenoceptors were administered intravenously to normotensive Wistar rats to determine their effects on mean arterial blood pressure and heart rate. Upon intravenous administration at dose of 0.1 mg/kg to normotensive male Wistar rats, the initial transient pressor effect was followed by long-lasting hypotension and bradycardia. In view of the above results the 1-[(imidazolin-2-yl)amino]indolines and [(imidazolin-2-yl)amino]-1,2,3,4-tetrahydroquinolines are now found to possess circulatory profile characteristic of the centrally acting clonidine-like hypotensive imidazolines.
authors.forename: Franciszek
authors.initials: F
authors.lastname: Sączewskf
authors.forename: Aleksandra
authors.initials: A
authors.lastname: Wasilewska
authors.forename: Alan L
authors.initials: AL
authors.lastname: Hudson
authors.forename: Mehnaz
authors.initials: M
authors.lastname: Ferdousi
authors.forename: Apolonia
authors.initials: A
authors.lastname: Rybczyńska
authors.forename: Konrad
authors.initials: K
authors.lastname: Boblewski
authors.forename: Artur
authors.initials: A
authors.lastname: Lehmann
mesh_terms: D000818:Animals; D001794:Blood Pressure / Q000187:drug effects*; D006339:Heart Rate / Q000187:drug effects*; D054755:Imidazoline Receptors / Q000378:metabolism; D048288:Imidazolines / Q000494:pharmacology*; D007211:Indoles / Q000494:pharmacology; D008297:Male; D011804:Quinolines / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley; D011942:Receptors, Adrenergic, alpha / Q000378:metabolism
chemical_list: D054755:Imidazoline Receptors; D048288:Imidazolines; D007211:Indoles; D011804:Quinolines; D011942:Receptors, Adrenergic, alpha; C057812:indoline