Receptor Theories and Quantitative Effect Versus Dose-Concentration Relationship
作者:
TallaridaR. J.,
期刊:
Drug Metabolism Reviews
(Taylor Available online 1984)
卷期:
Volume 15,
issue 1-2
页码: 345-363
ISSN:0360-2532
年代: 1984
DOI:10.3109/03602538409015071
出版商: Taylor&Francis
数据来源: Taylor
摘要:
Abstract1. Both in vivo and in vitro, the dissociation constant K&D50. This was shown for morphine in vivo and for several vasoconstrictors in isolated vascular smooth muscle.3. Values of K obtained from pharmacologic methods can discriminate among receptor subtypes.4. A proper determination of K permits knowledge of the stimulus-response relation, a drug-independent property of the effector system.5. A perturbation of the drug-receptor equilibrium is a way of determining both k1and k2; so far, however, we have been successful only withα-adrenergic vasoconstrictors in which UV light is a suitable stimulus.6. Radiolabeled binding appears to be a precise way of determining K's for agonists and antagonists. However, it does not measure an effect; hence we do not know that such binding sites are true receptors unless we can find a correlation between the values obtained for a series of drugs with this method and those obtained with appropriate pharmacologic methods.
点击下载:
PDF (740KB)
返 回