3H-Dopamine Binding Sites Differ in Rat Striatum and Pituitary

Overview

Journal Naunyn Schmiedebergs Arch Pharmacol

Specialty Pharmacology

Date 1984 Sep 1

PMID 6493362

Citations 11

Authors

P Sokoloff

M P Martres

M Delandre

K Redouane

J C Schwartz

Affiliations

Soon will be listed here.

Abstract

3H-Domperidone (3H-DOMP) binding sites were compared in rat striatum and pituitary, regarding the effects of the non-hydrolysable GTP analog, Gpp(NH)p and inhibition by various dopamine (DA) antagonists. Gpp(NH)p (0.1 mM) elicited in both tissues a rightward shift in DA concentration-inhibition curves, but the changes in either IC50 values or pseudo-Hill coefficients were larger in pituitary than in striatum. Computer analysis of the data showed that, in the presence of Gpp(NH)p, the curve obtained in striatum is best explained by the presence of two classes of binding site, a high-affinity site (Ki = 95 nM, 27% of total binding) and a low-affinity site (Ki = 5, 100 nM, 73% of total binding), whereas in pituitary only a low-affinity site (Ki = 5,070 nM) could be detected. In striatum, several discriminant benzamide derivatives (DBD), (-)-sulpiride and recently developed compounds, allowed to distinguish two components among 3H-DOMP binding sites: a high-affinity site representing one-third of total binding and a low-affinity component displaying a 8-17 fold lower affinity. Classical neuroleptics like haloperidol, chlorpromazine and metoclopramide inhibited striatal 3H-DOMP binding in a monophasic manner. In pituitary a single component could be detected for all tested antagonists including the DBD and Ki values for the latters were identical to those found for the low-affinity component in striatum.(ABSTRACT TRUNCATED AT 250 WORDS)

Citing Articles

Agonist high- and low-affinity states of dopamine D₂ receptors: methods of detection and clinical implications.

van Wieringen J, Booij J, Shalgunov V, Elsinga P, Michel M Naunyn Schmiedebergs Arch Pharmacol. 2012; 386(2):135-54.

PMID: 23224422 DOI: 10.1007/s00210-012-0817-0.

Effects of discriminant and non-discriminant dopamine antagonists on in vivo accumulation of 3H-N-propyl-norapomorphine in mouse striatum and tuberculum olfactorium.

LAFITTE A, Schwartz J, Protais P Naunyn Schmiedebergs Arch Pharmacol. 1985; 329(2):117-22.

PMID: 4040216 DOI: 10.1007/BF00501199.

Unexpected potentiation by discriminant benzamide derivatives of stereotyped behaviours elicited by dopamine agonists in mice.

Vasse M, Protais P, Costentin J, Schwartz J Naunyn Schmiedebergs Arch Pharmacol. 1985; 329(2):108-16.

PMID: 4040215 DOI: 10.1007/BF00501198.

3H-(-)DO 710 discriminates guanine nucleotide sensitive and insensitive dopamine binding sites.

Sokoloff P, Redouane K, Brann M, Martres M, Schwartz J Naunyn Schmiedebergs Arch Pharmacol. 1985; 329(3):236-43.

PMID: 4022135 DOI: 10.1007/BF00501874.

Autoradiographic localisation of 3H-apomorphine binding sites in rat brain.

Bouthenet M, Sales N, Schwartz J Naunyn Schmiedebergs Arch Pharmacol. 1985; 330(1):1-8.

PMID: 2995839 DOI: 10.1007/BF00586702.

References

Sibley D, Creese I . Interactions of ergot alkaloids with anterior pituitary D-2 dopamine receptors. Mol Pharmacol. 1983; 23(3):585-93. View

Heikkila R, Cabbat F . Ascorbate-induced lipid peroxidation and inhibition of [3H]spiroperidol binding in neostriatal membrane preparations. J Neurochem. 1983; 41(5):1384-92. DOI: 10.1111/j.1471-4159.1983.tb00836.x. View

Starke K, Spath L, Lang J, Adelung C . Further functional in vitro comparison of pre- and postsynaptic dopamine receptors in the rabbit caudate nucleus. Naunyn Schmiedebergs Arch Pharmacol. 1983; 323(4):298-306. DOI: 10.1007/BF00512467. View

Scatton B . Effect of dopamine agonists and neuroleptic agents on striatal acetylcholine transmission in the rat: evidence against dopamine receptor multiplicity. J Pharmacol Exp Ther. 1982; 220(1):197-202. View

Caron M, Beaulieu M, Raymond V, Gagne B, Drouin J, Lefkowitz R . Dopaminergic receptors in the anterior pituitary gland. Correlation of [3H]dihydroergocryptine binding with the dopaminergic control of prolactin release. J Biol Chem. 1978; 253(7):2244-53. View

Enjalbert A, Bockaert J . Pharmacological characterization of the D2 dopamine receptor negatively coupled with adenylate cyclase in rat anterior pituitary. Mol Pharmacol. 1983; 23(3):576-84. View

Protais P, Bonnet J, Costentin J . Pharmacological characterization of the receptors involved in the apomorphine-induced polyphasic modifications of locomotor activity in mice. Psychopharmacology (Berl). 1983; 81(2):126-34. DOI: 10.1007/BF00429006. View

Parker R, WAUD D . Pharmacological estimation of drug-receptor dissociation constants. Statistical evaluation. I. Agonists. J Pharmacol Exp Ther. 1971; 177(1):1-12. View

Legan S, Coon G, Karsch F . Role of estrogen as initiator of daily LH surges in the ovariectomized rat. Endocrinology. 1975; 96(1):50-6. DOI: 10.1210/endo-96-1-50. View

10.

Baudry M, Martres M, Schwartz J . 3H-Domperidone: a selective ligand for dopamine receptors. Naunyn Schmiedebergs Arch Pharmacol. 1979; 308(3):231-7. DOI: 10.1007/BF00501387. View

11.

Onali P, Schwartz J, Costa E . Dopaminergic modulation of adenylate cyclase stimulation by vasoactive intestinal peptide in anterior pituitary. Proc Natl Acad Sci U S A. 1981; 78(10):6531-4. PMC: 349074. DOI: 10.1073/pnas.78.10.6531. View

12.

Kebabian J, Calne D . Multiple receptors for dopamine. Nature. 1979; 277(5692):93-6. DOI: 10.1038/277093a0. View

13.

Zahniser N, Dubocovich M . Comparison of dopamine receptor sites labeled by [3H]-S-sulpiride and [3H]-spiperone in striatum. J Pharmacol Exp Ther. 1983; 227(3):592-9. View

14.

Molinoff P, Wolfe B, Weiland G . Quantitative analysis of drug-receptor interactions: II. Determination of the properties of receptor subtypes. Life Sci. 1981; 29(5):427-43. DOI: 10.1016/0024-3205(81)90208-3. View

15.

Cheng Y, Prusoff W . Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol. 1973; 22(23):3099-108. DOI: 10.1016/0006-2952(73)90196-2. View

16.

De Lean A, Kilpatrick B, Caron M . Dopamine receptor of the porcine anterior pituitary gland. Evidence for two affinity states discriminated by both agonists and antagonists. Mol Pharmacol. 1982; 22(2):290-7. View

17.

Jenner P, Marsden C . Substituted benzamide drugs as selective neuroleptic agents. Neuropharmacology. 1981; 20(12B):1285-93. View

18.

Jenner P, Theodorou A, Marsden C . Specific receptors for substituted benzamide drugs in brain. Adv Biochem Psychopharmacol. 1982; 35:109-41. View

19.

Stefanini E, Marchisio A, Devoto P, Vernaleone F, Collu R, Spano P . Sodium-dependent interaction of benzamides with dopamine receptors. Brain Res. 1980; 198(1):229-33. DOI: 10.1016/0006-8993(80)90360-1. View

20.

Protais P, Dubuc I, Costentin J . Pharmacological characteristics of dopamine receptors involved in the dual effect of dopamine agonists on yawning behaviour in rats. Eur J Pharmacol. 1983; 94(3-4):271-80. DOI: 10.1016/0014-2999(83)90416-8. View