Characterization of postsynaptic alpha-adrenoceptors in rat aortic strips and portal veins. 1983

K G Digges, and R J Summers

Postsynaptic alpha-adrenoceptors in rat isolated aortic strips and portal veins have been examined using a number of agonist and antagonist drugs which have varying selectivity for alpha 1- and alpha 2-adrenoceptors. In both tissues (-)-noradrenaline [-)-NA), (-)-adrenaline [-) Adr) (-)-alpha-methyl noradrenaline [-)-alpha-Me-NA) and (-)-phenylephrine [-)-PE) were full agonists, while clonidine, oxymetazoline and (2-(2,6-dichlorophenyl)-5,6-dihydroimidazo(2,1,b) thiazole (44,549) were partial agonists. Guanfacine was a full agonist in aortic strips but only a partial agonist in portal veins. In aortic strips, pA2 values for prazosin and yohimbine were not significantly different using (-)-NA, (-)-PE or guanfacine as the agonist, suggesting a single population of alpha-adrenoceptors. The order of potency of the antagonists, prazosin = 2-(beta-(4-hydroxyphenyl)-ethylaminomethyl)-tetralone (BE2254) greater than phentolamine greater than yohimbine greater than rauwolscine, is indicative of an alpha 1-type of receptor. In portal veins, the order of potency of the antagonists was prazosin greater than BE2254 greater than phentolamine greater than yohimbine greater than rauwolscine, again indicating an alpha 1-type of receptor. The mean pA2 value for yohimbine was not significantly different in either tissue. However, mean pA2 values for prazosin, BE-2254 and phentolamine were approximately one order of magnitude lower in portal veins than in aortic strips, suggesting that the receptors in the two tissues may not be identical.

UI MeSH Term Description Entries
D008297 Male Males
D008771 Nordefrin A norepinephrine derivative used as a vasoconstrictor agent. Methylnorepinephrine,3,4-Dihydroxynorephedrine,4-(2-Amino-1-hydroxypropyl)-1,2-benzenediol,4-(2-Amino-1-hydroxypropyl)-1,2-benzenediol Hydrochloride, (R*,R*)-(+,-)-Isomer,4-(2-Amino-1-hydroxypropyl)-1,2-benzenediol Hydrochloride, (R*,S*)-(+-)-Isomer,4-(2-Amino-1-hydroxypropyl)-1,2-benzenediol Tartrate, (R*,R*), (R*,R*)-Isomer,4-(2-Amino-1-hydroxypropyl)-1,2-benzenediol Tartrate, (R*,S*), (R*,R*)-Isomer,4-(2-Amino-1-hydroxypropyl)-1,2-benzenediol, (R*,R*)-Isomer,4-(2-Amino-1-hydroxypropyl)-1,2-benzenediol, (R*,S*)-Isomer,Cobefrine,Corbadrine,Levonordefrin,Neo-Cobefrin,Nordefrin Hydrochloride,Nordefrin Hydrochloride, (R*,R*)-(+,-)-Isomer,Nordefrin Hydrochloride, (R*,S*)-(+,-)-Isomer,Nordefrin Tartrate, (R*,R*), (R*,R*) Isomer,Nordefrin Tartrate, (R*,S*), (R*,R*) Isomer,Nordefrin, (R*,R*)-Isomer,Nordefrin, (R*,S*)-Isomer,Norephrine,alpha-Methylnoradrenaline,alpha-Methylnorepinephrine,3,4 Dihydroxynorephedrine,Hydrochloride, Nordefrin,Neo Cobefrin,NeoCobefrin,alpha Methylnoradrenaline,alpha Methylnorepinephrine
D009131 Muscle, Smooth, Vascular The nonstriated involuntary muscle tissue of blood vessels. Vascular Smooth Muscle,Muscle, Vascular Smooth,Muscles, Vascular Smooth,Smooth Muscle, Vascular,Smooth Muscles, Vascular,Vascular Smooth Muscles
D010109 Oxymetazoline A direct acting sympathomimetic used as a vasoconstrictor to relieve nasal congestion. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1251) Oxymetazoline Hydrochloride,Hydrochloride, Oxymetazoline
D010627 Phenethylamines A group of compounds that are derivatives of beta- aminoethylbenzene which is structurally and pharmacologically related to amphetamine. (From Merck Index, 11th ed) Phenylethylamines
D011169 Portal Vein A short thick vein formed by union of the superior mesenteric vein and the splenic vein. Portal Veins,Vein, Portal,Veins, Portal
D011224 Prazosin A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION. Furazosin,Minipress,Pratsiol,Prazosin HCL,Prazosin Hydrochloride,HCL, Prazosin,Hydrochloride, Prazosin
D011919 Rats, Inbred Strains Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding. August Rats,Inbred Rat Strains,Inbred Strain of Rat,Inbred Strain of Rats,Inbred Strains of Rats,Rat, Inbred Strain,August Rat,Inbred Rat Strain,Inbred Strain Rat,Inbred Strain Rats,Inbred Strains Rat,Inbred Strains Rats,Rat Inbred Strain,Rat Inbred Strains,Rat Strain, Inbred,Rat Strains, Inbred,Rat, August,Rat, Inbred Strains,Rats Inbred Strain,Rats Inbred Strains,Rats, August,Rats, Inbred Strain,Strain Rat, Inbred,Strain Rats, Inbred,Strain, Inbred Rat,Strains, Inbred Rat
D011942 Receptors, Adrenergic, alpha One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation. Adrenergic alpha-Receptor,Adrenergic alpha-Receptors,Receptors, alpha-Adrenergic,alpha-Adrenergic Receptor,alpha-Adrenergic Receptors,Receptor, Adrenergic, alpha,Adrenergic alpha Receptor,Adrenergic alpha Receptors,Receptor, alpha-Adrenergic,Receptors, alpha Adrenergic,alpha Adrenergic Receptor,alpha Adrenergic Receptors,alpha-Receptor, Adrenergic,alpha-Receptors, Adrenergic
D003000 Clonidine An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION. Catapres,Catapresan,Catapressan,Chlophazolin,Clofelin,Clofenil,Clonidine Dihydrochloride,Clonidine Hydrochloride,Clonidine Monohydrobromide,Clonidine Monohydrochloride,Clopheline,Dixarit,Gemiton,Hemiton,Isoglaucon,Klofelin,Klofenil,M-5041T,ST-155,Dihydrochloride, Clonidine,Hydrochloride, Clonidine,M 5041T,M5041T,Monohydrobromide, Clonidine,Monohydrochloride, Clonidine,ST 155,ST155

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