MolPharm xPharm- The Comprehensive Pharmacology Reference

Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
QUICK SEARCH:   [advanced]


     

This Article
Right arrow Full Text (PDF)
Right arrow Submit a response
Right arrow Alert me when this article is cited
Right arrow Alert me when eLetters are posted
Right arrow Alert me if a correction is posted
Services
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Download to citation manager
Citing Articles
Right arrow Citing Articles via HighWire
Right arrow Citing Articles via Google Scholar
Google Scholar
Right arrow Articles by BURT, D. R.
Right arrow Articles by SNYDER, S. H.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by BURT, D. R.
Right arrow Articles by SNYDER, S. H.

Molecular Pharmacology, Vol 12, 631-638, Copyright © 1976 by the American Society for Pharmacology and Experimental Therapeutics

Binding Interactions of Lysergic Acid Diethylamide and Related Agents with Dopamine Receptors in the Brain

DAVID R. BURT 1, IAN CREESE 1, and SOLOMON H. SNYDER 1

1 Departments of Pharmacology and Experimental Therapeutics and of Psychiatry and Behavioral Sciences, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205

In most brain regions saturable binding of d-[3H]lysergic acid diethylamide ([3H]LSD) appears to involve postsynaptic serotonin receptors. In calf caudate, however, a portion of [3H]LSD binding involves postsynaptic dopamine receptors. Thus, in the hippocampus of calf brain, dopamine competes for [3H]LSD binding sites with a single low-affinity component, while in the caudate dopamine competition for [3H]LSD binding displays both high- and low-affinity components. The high-affinity component, accounting for 15-20% of [3H]LSD binding, displays a Ki value for dopamine of about 30 nM, similar to the KD for the binding of [3H]dopamine itself to postsynaptic dopamine receptors in the calf caudate. Addition of serotonin to the incubations increases the proportion of [3H]LSD binding in the caudate competed for by dopamine with high affinity, presumably by occupying serotonin receptors. d-LSD competes stereospecifically for [3H]dopamine binding in the caudate, consistent with the conclusion that LSD binds to dopamine receptors. Of numerous serotonin agonists and antagonists examined, several ergot alkaloids have high affinity for [3H]dopamine receptor binding in calf caudate, with Ki values similar to that of d-LSD.

Note:
ACKNOWLEDGMENTS We thank Janet Ryan for excellent technical assistance.

Submitted on December 10, 1975




This article has been cited by other articles:


Home page
 Br. J. PsychiatryHome page
X. XIBERAS, J. L. MARTINOT, L. MALLET, E. ARTIGES, C. LOC'H, B. MAZIERE, and M. L. PAILLERE-MARTINOT
Extrastriatal and striatal D2 dopamine receptor blockade with haloperidol or new antipsychotic drugs in patients with schizophrenia
The British Journal of Psychiatry, December 1, 2001; 179(6): 503 - 508.
[Abstract] [Full Text] [PDF]

Home page
 ScienceHome page
I Creese, D. Burt, and S. Snyder
Dopamine receptor binding enhancement accompanies lesion-induced behavioral supersensitivity
Science, August 5, 1977; 197(4303): 596 - 598.
[Abstract] [PDF]

Home page
 ScienceHome page
I. CREESE, D. R. BURT, and S. H. SNYDER
Dopamine Receptors and Average Clinical Doses
Science, October 29, 1976; 194(4264): 546 - 546.
[PDF]


Home Help [Feedback] [For Subscribers] [Archive] [Search] [Contents]
All ASPET Journals Molecular Pharmacology Pharmacological Reviews
Molecular Interventions Drug Metabolism and Disposition

Copyright © 1976 by the American Society for Pharmacology and Experimental Therapeutics