SELECTIVITY OF ANTIMUSCARINIC COMPOUNDS FOR MUSCARINIC RECEPTORS OF HUMAN BRAIN AND HEART

被引:26
|
作者
LARSON, EW
PFENNING, MA
RICHELSON, E
机构
[1] MAYO CLIN JACKSONVILLE,4500 SAN PABLO RD,JACKSONVILLE,FL 32224
[2] MAYO CLIN & MAYO FDN,DEPT PHARMACOL,ROCHESTER,MN 55905
[3] MAYO CLIN & MAYO FDN,DEPT PSYCHIAT & PSYCHOL,ROCHESTER,MN 55905
关键词
PARKINSONISM DRUGS; PIRENZEPINE; M1-RECEPTOR AND M2-RECEPTOR;
D O I
10.1007/BF02244197
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
Seven antimuscarinic compounds, used mostly for the treatment of extrapyramidal problems, were tested in vitro in radioligand binding assays for evidence of selectivity for two different pharmacological subtypes of the human muscarinic receptor, M1, a predominant form in brain, and M2, a predominant form in heart. Although biperiden, scopolamine, procyclidine, and benztropine showed significant selectivity in the in vitro assays, it is likely that in clinical practice biperiden would be the drug of choice to avoid any antimuscarinic effects on the heart.
引用
收藏
页码:162 / 165
页数:4
相关论文
共 50 条
  • [1] IMAGING AND QUANTIFICATION OF MUSCARINIC RECEPTORS IN THE HUMAN HEART AND BRAIN IN-VIVO
    DUBOIS, EA
    VERMEULEN, RJ
    JANSSEN, AFM
    [J]. BRITISH JOURNAL OF PHARMACOLOGY, 1995, 114 : P142 - P142
  • [2] Adrenergic and muscarinic receptors in the human heart
    Brodde, OE
    Michel, MC
    [J]. PHARMACOLOGICAL REVIEWS, 1999, 51 (04) : 651 - 689
  • [3] Muscarinic receptors subtypes in human heart
    Nello, C
    Castañeda, D
    Bonfante-Cabarcas, R
    [J]. JOURNAL OF MOLECULAR AND CELLULAR CARDIOLOGY, 2001, 33 (06) : A84 - A84
  • [4] Muscarinic receptors in the failing human heart
    Giessler, C
    Dhein, S
    Pönicke, K
    Brodde, OE
    [J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1999, 375 (1-3) : 197 - 202
  • [5] SELECTIVITY OF BETHANECHOL ON MUSCARINIC RECEPTORS
    BURLEIGH, DE
    [J]. JOURNAL OF PHARMACY AND PHARMACOLOGY, 1978, 30 (06) : 398 - 399
  • [6] ANTAGONISM BY ANTIMUSCARINIC AND NEUROLEPTIC COMPOUNDS AT THE 5 CLONED HUMAN MUSCARINIC CHOLINERGIC RECEPTORS EXPRESSED IN CHINESE-HAMSTER OVARY CELLS
    BOLDEN, C
    CUSACK, B
    RICHELSON, E
    [J]. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 1992, 260 (02): : 576 - 580
  • [7] COCAINE INHIBITS MUSCARINIC CHOLINERGIC RECEPTORS IN HEART AND BRAIN
    SHARKEY, J
    RITZ, MC
    SCHENDEN, JA
    HANSON, RC
    KUHAR, MJ
    [J]. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 1988, 246 (03): : 1048 - 1052
  • [8] IMAGING OF MUSCARINIC RECEPTORS IN THE HUMAN HEART AND BRAIN USING [I-123] IODODEXETIMIDE
    DUBOIS, EA
    PFAFFENDORF, M
    JANSSEN, AGM
    DEBRUIN, K
    VANROYEN, EA
    VANZWIETEN, PA
    [J]. LIFE SCIENCES, 1995, 56 (11-12) : 1049 - 1049
  • [9] Ocular effects of antimuscarinic compounds: Is clinical effect determined by binding affinity for muscarinic receptors or melanin pigment?
    German, EJ
    Wood, D
    Hurst, MA
    [J]. JOURNAL OF OCULAR PHARMACOLOGY AND THERAPEUTICS, 1999, 15 (03) : 257 - 269
  • [10] RAT-BRAIN AND HEART MUSCARINIC RECEPTORS - MODIFICATION WITH TETRANITROMETHANE
    GURWITZ, D
    SOKOLOVSKY, M
    [J]. BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1985, 131 (03) : 1124 - 1131