Species variations in dopamine receptor binding

Ian Creese, Kim Stewart, Solomon H Snyder

Research output: Contribution to journalArticle

Abstract

Binding of 3H-spiroperidol, 3H-apomorphine and 3H-ADTN (2-amino-6,7-dihydroxytetrahydronaphthalene) associated with dopamine receptors has been evaluated in corpus striatal membranes of calf, rat and human brains. Substantial species differences are apparent for numerous agonists and antagonists in competing for receptor binding. In general, dopamine receptor antagonists are more potent in rat and agonists more potent in calf. In competing for 3H-spiroperidol binding sulpiride, molindone and metaclopramide show the most pronounced species differences, being 3-10 times more potent in rat and human than in calf. In all three species agonists compete for 3H-spiroperidol binding with Hill coefficients less than one while antagonists inhibit 3H-spiroperidol binding with Hill coefficients of about 1.0. Conversely, 3H-apomorphine and 3H-ADTN binding in all three species is inhibited by antagonists with Hill coefficients less than 1.0 while agonists display Hill coefficients of about 1.0 In general agonists are more potent in competing for binding of 3H-apomorphine and 3H-ADTN than 3H-spiroperidol. However, a small component of dopamine, apomorphine and ADTN inhibition of 3H-spiroperidol binding displays very high affinity (IC50 about 1 nM). In human amygdala 3H-spiroperidol appears to label serotonin receptors predominantly.

Original languageEnglish (US)
Pages (from-to)55-66
Number of pages12
JournalEuropean Journal of Pharmacology
Volume60
Issue number1
DOIs
StatePublished - Nov 23 1979

Fingerprint

Spiperone
Dopamine Receptors
Apomorphine
Molindone
Corpus Striatum
Sulpiride
Metoclopramide
Dopamine Antagonists
Serotonin Receptors
Amygdala
Inhibitory Concentration 50
Dopamine
Membranes
ADTN
Brain

Keywords

  • Adenylate cyclase
  • ADTN
  • Apomorphine
  • Dopamine receptor
  • Serotonin receptor
  • Spiroperidol

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

Species variations in dopamine receptor binding. / Creese, Ian; Stewart, Kim; Snyder, Solomon H.

In: European Journal of Pharmacology, Vol. 60, No. 1, 23.11.1979, p. 55-66.

Research output: Contribution to journalArticle

Creese, Ian ; Stewart, Kim ; Snyder, Solomon H. / Species variations in dopamine receptor binding. In: European Journal of Pharmacology. 1979 ; Vol. 60, No. 1. pp. 55-66.
@article{6b3ed6ac19a14f7ba376cbe5e9cc11af,
title = "Species variations in dopamine receptor binding",
abstract = "Binding of 3H-spiroperidol, 3H-apomorphine and 3H-ADTN (2-amino-6,7-dihydroxytetrahydronaphthalene) associated with dopamine receptors has been evaluated in corpus striatal membranes of calf, rat and human brains. Substantial species differences are apparent for numerous agonists and antagonists in competing for receptor binding. In general, dopamine receptor antagonists are more potent in rat and agonists more potent in calf. In competing for 3H-spiroperidol binding sulpiride, molindone and metaclopramide show the most pronounced species differences, being 3-10 times more potent in rat and human than in calf. In all three species agonists compete for 3H-spiroperidol binding with Hill coefficients less than one while antagonists inhibit 3H-spiroperidol binding with Hill coefficients of about 1.0. Conversely, 3H-apomorphine and 3H-ADTN binding in all three species is inhibited by antagonists with Hill coefficients less than 1.0 while agonists display Hill coefficients of about 1.0 In general agonists are more potent in competing for binding of 3H-apomorphine and 3H-ADTN than 3H-spiroperidol. However, a small component of dopamine, apomorphine and ADTN inhibition of 3H-spiroperidol binding displays very high affinity (IC50 about 1 nM). In human amygdala 3H-spiroperidol appears to label serotonin receptors predominantly.",
keywords = "Adenylate cyclase, ADTN, Apomorphine, Dopamine receptor, Serotonin receptor, Spiroperidol",
author = "Ian Creese and Kim Stewart and Snyder, {Solomon H}",
year = "1979",
month = "11",
day = "23",
doi = "10.1016/0014-2999(79)90052-9",
language = "English (US)",
volume = "60",
pages = "55--66",
journal = "European Journal of Pharmacology",
issn = "0014-2999",
publisher = "Elsevier",
number = "1",

}

TY - JOUR

T1 - Species variations in dopamine receptor binding

AU - Creese, Ian

AU - Stewart, Kim

AU - Snyder, Solomon H

PY - 1979/11/23

Y1 - 1979/11/23

N2 - Binding of 3H-spiroperidol, 3H-apomorphine and 3H-ADTN (2-amino-6,7-dihydroxytetrahydronaphthalene) associated with dopamine receptors has been evaluated in corpus striatal membranes of calf, rat and human brains. Substantial species differences are apparent for numerous agonists and antagonists in competing for receptor binding. In general, dopamine receptor antagonists are more potent in rat and agonists more potent in calf. In competing for 3H-spiroperidol binding sulpiride, molindone and metaclopramide show the most pronounced species differences, being 3-10 times more potent in rat and human than in calf. In all three species agonists compete for 3H-spiroperidol binding with Hill coefficients less than one while antagonists inhibit 3H-spiroperidol binding with Hill coefficients of about 1.0. Conversely, 3H-apomorphine and 3H-ADTN binding in all three species is inhibited by antagonists with Hill coefficients less than 1.0 while agonists display Hill coefficients of about 1.0 In general agonists are more potent in competing for binding of 3H-apomorphine and 3H-ADTN than 3H-spiroperidol. However, a small component of dopamine, apomorphine and ADTN inhibition of 3H-spiroperidol binding displays very high affinity (IC50 about 1 nM). In human amygdala 3H-spiroperidol appears to label serotonin receptors predominantly.

AB - Binding of 3H-spiroperidol, 3H-apomorphine and 3H-ADTN (2-amino-6,7-dihydroxytetrahydronaphthalene) associated with dopamine receptors has been evaluated in corpus striatal membranes of calf, rat and human brains. Substantial species differences are apparent for numerous agonists and antagonists in competing for receptor binding. In general, dopamine receptor antagonists are more potent in rat and agonists more potent in calf. In competing for 3H-spiroperidol binding sulpiride, molindone and metaclopramide show the most pronounced species differences, being 3-10 times more potent in rat and human than in calf. In all three species agonists compete for 3H-spiroperidol binding with Hill coefficients less than one while antagonists inhibit 3H-spiroperidol binding with Hill coefficients of about 1.0. Conversely, 3H-apomorphine and 3H-ADTN binding in all three species is inhibited by antagonists with Hill coefficients less than 1.0 while agonists display Hill coefficients of about 1.0 In general agonists are more potent in competing for binding of 3H-apomorphine and 3H-ADTN than 3H-spiroperidol. However, a small component of dopamine, apomorphine and ADTN inhibition of 3H-spiroperidol binding displays very high affinity (IC50 about 1 nM). In human amygdala 3H-spiroperidol appears to label serotonin receptors predominantly.

KW - Adenylate cyclase

KW - ADTN

KW - Apomorphine

KW - Dopamine receptor

KW - Serotonin receptor

KW - Spiroperidol

UR - http://www.scopus.com/inward/record.url?scp=0018651565&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0018651565&partnerID=8YFLogxK

U2 - 10.1016/0014-2999(79)90052-9

DO - 10.1016/0014-2999(79)90052-9

M3 - Article

C2 - 520417

AN - SCOPUS:0018651565

VL - 60

SP - 55

EP - 66

JO - European Journal of Pharmacology

JF - European Journal of Pharmacology

SN - 0014-2999

IS - 1

ER -