These tools will no longer be maintained as of December 31, 2024. Archived website can be found here. PubMed4Hh GitHub repository can be found here. Contact NLM Customer Service if you have questions.


Pubmed for Handhelds

PUBMED FOR HANDHELDS

Search MEDLINE/PubMed

  • Title: Evidence that alpha(1B)-adrenoceptors are involved in noradrenaline-induced contractions of rat tail artery.
    Author: Jähnichen S, Eltze M, Pertz HH.
    Journal: Eur J Pharmacol; 2004 Mar 19; 488(1-3):157-67. PubMed ID: 15044047.
    Abstract:
    The present study characterizes the alpha(1)-adrenoceptor subtypes mediating contractions to noradrenaline in isolated ring preparations of rat tail artery. Concentration-response (E/[A]) curves to noradrenaline were apparently monophasic (pEC(50) 6.47) but became biphasic in the presence of the selective alpha(1A)-adrenoceptor antagonist (+/-)-1,3,5-trimethyl-6-[[3-[4-((2,3-dihydro-2-hydroxymethyl)-1,4-benzodioxin-5-yl)-1-piperazinyl]propyl]amino]-2,4(1H,3H)-pyrimidinedione (B8805-033). Whereas the first phase of contraction to noradrenaline remained nearly unaffected in the presence of B8805-033 (0.03-3 microM), the second phase was concentration-dependently shifted to the right (pK(B) 8.06). In the presence of B8805-033 (3 microM), noradrenaline-induced contractions (pEC(50) 6.55) were antagonized in a competitive manner by prazosin (pK(B) 9.24), tamsulosin (pK(B) 8.55), 2-(2,6-dimethoxyphenoxyethyl)aminomethyl-1,4-benzodioxane (WB 4101; pK(B) 7.81), spiperone (pK(B) 7.69), 4-amino-2-[4-[1-(benzyloxycarbonyl)-2(S)-[[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6,7-dimethoxyquinazoline (L-765,314; pK(B) 7.31), 5-methylurapidil (pK(B) 6.55), 8-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-8-azaspiro[4.5]decane-7,9-dione (BMY 7378; pK(B) 6.43), and 8-[2-(1,4-benzodioxan-2-ylmethylamino)ethyl]-8-azaspiro[4.5]decane-7,9-dione (MDL 73005EF; pK(B) 5.71), and were also antagonized by 100 microM chloroethylclonidine. N-[2-(2-cyclopropylmethoxyphenoxy)ethyl]-5-chloro-alpha,alpha-dimethyl-1H-indole-3-ethanamine (RS-17053) behaved as a noncompetitive antagonist (apparent pA(2) 6.55). Antagonist affinities obtained under these experimental conditions correlated highly with affinities at native and cloned alpha(1B)-adrenoceptors. Pretreatment of arterial rings with B8805-033 (3 microM) followed by receptor inactivation with chloroethylclonidine (100 microM) yielded monophasic E/[A] curves to noradrenaline (pEC(50) 6.14). Noradrenaline-induced contractions were competitively antagonized by tamsulosin (pK(B) 10.32), 5-methylurapidil (pK(B) 8.66), RS-17053 (pK(B) 8.44), B8805-033 (pK(B) 7.87), BMY 7378 (pK(B) 6.54), and L-765,314 (pK(B) 6.41). Antagonist affinities obtained under these experimental conditions correlated highly with affinities at native and cloned alpha(1A)-adrenoceptors. It is concluded that the contraction to noradrenaline in rat tail artery is mediated by both alpha(1B)- and alpha(1A)-adrenoceptors, each component of contraction being separable by use of selective alpha(1A)-adrenoceptor blockade and alpha(1B)-adrenoceptor alkylation, respectively.
    [Abstract] [Full Text] [Related] [New Search]