previous in vitro work on rabbit knee joint vessels showed that vasoconstrictor effects of nerve stimulation and administration of α-adrenoceptor agonists were mediated predominantly by α1-adrenoceptors5,9 the present experiments were performed to assess the nature of α-adrenoceptor subtypes within these blood vessels in vivo. dose/response relationships for adrenaline and noradrenaline produce...

leptin affects paraventricular nucleus of hypothalamus and reduces appetite while activation of α2-adrenoceptors at this site has opposite action. the reducing effect of α2-adrenoceptors inhibition on body weight and appetite and also enhancing effects on lipolysis, sympathetic activation and plasma insulin levels in animals have been reported. we studied the effect of yohimbine treatment (2 mg...

agonist, phenylephrine, showed 2 opposite effects on ICa (transient decrease followed by sustained increase). However, selective 1A-adrenoceptor stimulation ( 0.1 mol/L A61603) only potentiated ICa, and selective 1B-adrenoceptor stimulation (10 mol/L phenylephrine with 2 mol/L WB4101) only deceased ICa. The positive effect by 1A-adrenoceptor stimulation was blocked by the inhibition of phosphol...

BACKGROUND AND PURPOSE CGP 12177 not only inhibits agonist effects mediated through the catecholamine site of the β1 -adrenoceptor with high affinity, but also exhibits agonist effects of its own at higher concentrations through a secondary, low-affinity β1 -adrenoceptor site or conformation. β-blocker affinities for this 'CGP 12177' site of the human β1 -adrenoceptor have thus far only been ch...

α(1)-Adrenoceptors are involved in numerous physiological functions, including micturition. However, the pharmacological profile of the α(1)-adrenoceptor subtypes remains controversial. Here, we review the literature regarding α(1)-adrenoceptors in the lower urinary tract from the standpoint of α(1L) phenotype pharmacology. Among three α(1)-adrenoceptor subtypes (α(1A), α(1B) and α(1D)), α(1a)-...

The effect of 24-h pretreatment with epinephrine (EPI) or norepinephrine (NE) on alpha(2)- and beta-adrenoceptor agonist-induced, cAMP responses and G(i3)alpha-protein expression was studied in primary cultures of rat superior cervical ganglionic (SCG) neurons. SCG neurons, 10 to 12 days in culture, accumulated cAMP when stimulated with the beta-adrenoceptor agonist isoproterenol and the prefer...

The β1-adrenoceptor exists in two agonist conformations/states: 1) a high-affinity state where responses to catecholamines and other agonists (e.g., cimaterol) are potently inhibited by β1-adrenoceptor antagonists, and 2) a low-affinity secondary conformation where agonist responses, particularly CGP12177 [(-)-4-(3-tert-butylamino-2-hydroxypropoxy)-benzimidazol-2-one] are relatively resistant t...

OBJECTIVE The present study investigated whether activation of phosphatidylinositol 3-kinase (PI3-kinase) is involved in the stimulation of hypertrophic growth of adult ventricular cardiomyocytes under alpha- or beta-adrenoceptor stimulation. METHODS Adult ventricular rat cardiomyocytes were used either directly after isolation (day 1 culture) or after cultivation for 6 days in presence of 20...

a case of acute extrapyramidal manifestations consisting of dystonia and akathisia following abrupt discontinuation of propranolol is reported. she responded well to oral propranolol and intramuscular diazepam. extrapyramidal symptoms have commonly been associated with acute or chronic administration of neuroleptic drugs. there have been reports of a substantial number of cases with similar cli...

Correction to the article “Peculiar Aspects in Influence of α1-Adrenoceptor Stimulation on Isolated Rat Heart,” by T. L. Zefirov, I. Khabibrakhmanov, N. Ziyatdinova, and A. Vol. 162, No. 1, pp. 4-6, November 2016