CHLOROETHYLCLONIDINE UNMASKS A NON-ALPHA-ADRENOCEPTOR NORADRENALINE BINDING-SITE IN THE RAT AORTA

被引:33
|
作者
ORIOWO, MA
BEVAN, JA
机构
[1] UNIV VERMONT,COLL MED,DEPT PHARMACOL,GIVEN MED BLDG,BURLINGTON,VT 05405
[2] UNIV VERMONT,COLL MED,VERMONT CTR VASC RES,BURLINGTON,VT 05405
关键词
Chloroethylclonidine; Non-α-adrenoceptor site; α[!sub]1[!/sub]-Adrenoceptors;
D O I
10.1016/0014-2999(90)90482-L
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effect of chloroethylclonidine on nodrenaline-induced contractions of the rat aorta was studied. Chloroethylclonidine (1.5 × 10-5 M) shifted noradrenaline dose-response curve to the right approximately 5000-fold without depressing the maximum. The response to noradrenaline after chloroethylclonidine was not antagonized by phenoxybenzamine (10-7 M), prazosin (10-7 M), WB 4101 (10-7 M) nor yohimbine (10-5 M) and is therefore not mediated via α1-adrenoceptors. These results would suggest that there is a homogenous population of chloroethylclonidine-sensitive α1-adrenoceptors in the rat aorta and that chloroethylclonidine treatment reveals a non-α-adrenoceptor noradrenaline binding site in this tissue. © 1990.
引用
收藏
页码:243 / 246
页数:4
相关论文
共 50 条
  • [31] BINDING OF SULFOBROMOPHTHALEIN TO RAT AND HUMAN LIGANDINS - CHARACTERIZATION OF A BINDING-SITE PEPTIDE
    BHARGAVA, MM
    DASGUPTA, A
    BIOCHIMICA ET BIOPHYSICA ACTA, 1988, 955 (03) : 296 - 300
  • [32] COMPARISON OF ALPHA-2-ADRENOCEPTOR ANTAGONISTS ON BACKGROUND CORTICAL EEG IN THE CONSCIOUS RAT - A ROLE FOR THE NON-ALPHA-2-IDAZOXAN-BINDING-SITE
    DICKINSON, SL
    GADIE, B
    EUROPEAN JOURNAL OF PHARMACOLOGY, 1990, 183 (02) : 449 - 450
  • [33] EFFECTS OF COOLING ON ALPHA-1-ADRENOCEPTOR MECHANISMS IN RAT AORTA
    TAKAYANAGI, I
    KOIKE, K
    NAKAMURA, M
    HORIE, Y
    COMPARATIVE BIOCHEMISTRY AND PHYSIOLOGY C-PHARMACOLOGY TOXICOLOGY & ENDOCRINOLOGY, 1988, 90 (01): : 95 - 99
  • [34] FUNCTIONAL AND RADIOLIGAND BINDING EVIDENCE FOR AN ALPHA(1D)-ADRENOCEPTOR SUBTYPE MEDIATING CONTRACTION IN THE RAT AORTA
    BUCKNER, SA
    OHEIM, K
    MORSE, P
    KNEPPER, S
    HANCOCK, AA
    KERWIN, JF
    FASEB JOURNAL, 1995, 9 (03): : A105 - A105
  • [35] The expression of alpha(1) adrenoceptor subtypes changes with age in the rat aorta
    Gurdal, H
    Tilakaratne, N
    Brown, RD
    Fonseca, M
    Friedman, E
    Johnson, MD
    JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 1995, 275 (03): : 1656 - 1662
  • [36] ALPHA-1-ADRENOCEPTOR BLOCKING PROPERTIES OF SPIROXATRINE IN RAT AORTA
    TERRON, JA
    RANSANZ, V
    IBARRA, M
    HONG, E
    VILLALON, CM
    LIFE SCIENCES, 1992, 51 (01) : PL1 - PL6
  • [37] Effects of dicentrine on the subtypes of alpha(1)-adrenoceptor of the rat aorta and spleen
    Mustafa, MR
    Mohamad, R
    Achike, F
    FASEB JOURNAL, 1997, 11 (03): : 1536 - 1536
  • [38] CHARACTERIZATION OF A FUNCTIONAL ALPHA(1D) ADRENOCEPTOR ON RAT AORTA
    KENNY, BA
    CHALMERS, DH
    NAYLOR, AM
    BRITISH JOURNAL OF PHARMACOLOGY, 1995, 114 : P25 - P25
  • [39] ALPHA-1-ADRENOCEPTOR SUBTYPE AFFINITIES OF DRUGS FOR THE TREATMENT OF PROSTATIC HYPERTROPHY - EVIDENCE FOR HETEROGENEITY OF CHLOROETHYLCLONIDINE-RESISTANT RAT RENAL ALPHA-1-ADRENOCEPTOR
    MICHEL, MC
    BUSCHER, R
    KERKER, J
    KRANEIS, H
    ERDBRUGGER, W
    BRODDE, OE
    NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY, 1993, 348 (04) : 385 - 395
  • [40] BINDING-SITE OF ALPHA-2-PLASMIN INHIBITOR TO PLASMINOGEN
    SUGIYAMA, N
    SASAKI, T
    IWAMOTO, M
    ABIKO, Y
    BIOCHIMICA ET BIOPHYSICA ACTA, 1988, 952 (01) : 1 - 7