Home LiteratureArticle Details
PMID: 2945992 Published · ppublish English Journal Article

5-HT1A-receptors mediate stimulation of adenylate cyclase in rat hippocampus.

Naunyn-Schmiedeberg's archives of pharmacology ·Vol. 333 ·No. 4 ·1986-08-00 ·Pages 335-41

Markstein R, Hoyer D, Engel G

Abstract

Serotonin (5-HT) stimulated adenylate cyclase activity in homogenates of rat hippocampus. This effect was pharmacologically characterised with a series of agonists and antagonists of various structural classes. These compounds where also tested in radioligand binding studies using selective ligands for the various subtypes of 5-HT1 and 5-HT2 receptors. 5-HT1A, 5-HT1B and 5-HT1C recognition sites were labelled with [3H]8-OH-DPAT([3H]8-hydroxy-2-(di-n-propylamino)-tetralin) in pig cortex membranes, [125I]CYP([125I]iodocyanopindolol) in rat cortex and [3H]mesulergine in pig choroid plexus membranes, respectively. The rank order of potency of 13 agonists stimulating adenylate cyclase activity in homogenates of rat hippocampus was in good agreement with the rank order of affinity of these agonists for the 5-HT1A binding site: N,N-dipropyl-5-carboxamidotryptamine (DP-5-CT) greater than 5-carboxamidotryptamine (5-CT) greater than 8-OH-DPAT greater than 5-HT greater than 5-methoxytryptamine (5-OCH3T) greater than d-LSD greater than 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole (RU 24969) greater than alpha-methylserotonin (alpha-CH3-5-HT) greater than dopamine greater than 2-methylserotonin (2-CH3-5-HT). The correlation between the respective potencies and affinities of these agonists was r = 0.934, P less than 0.001. There was no correlation between stimulation of adenylate cyclase activity by these agonists and their affinity for 5-HT1B, 5-HT1C or 5-HT2 binding sites. r = 0.381-0.108, P less than 0.20-0.73.(ABSTRACT TRUNCATED AT 250 WORDS)

MeSH Terms
8-Hydroxy-2-(di-n-propylamino)tetralin Adenylyl Cyclases/metabolism Animals Cerebral Cortex/metabolism Enzyme Activation Hippocampus/enzymology In Vitro Techniques Iodine Radioisotopes Iodocyanopindolol Male Pindolol/analogs & derivatives Rats Receptors, Serotonin/physiology Tetrahydronaphthalenes/metabolism
Chemicals
Iodine Radioisotopes Receptors, Serotonin Tetrahydronaphthalenes 8-Hydroxy-2-(di-n-propylamino)tetralin Iodocyanopindolol Pindolol Adenylyl Cyclases
Authors & Affiliations
3 authors, click to expand affiliations / ORCID
Markstein R
Hoyer D
Engel G
References (38)
38 references, click to expand
  1. A simple ultrasensitive method for the assay of cyclic AMP and cyclic GMP in tissues.
    Life Sci. 1976 Mar 1;18(5):529-41 PMID: 176557
  2. Multiple 3H-5-hydroxytryptamine binding sites in rat brain.
    J Physiol (Paris). 1981;77(2-3):369-72 PMID: 7288652
  3. Mesulergine and its 1,20-N,N-bidemethylated metabolite interact directly with D1- and D2-receptors.
    Eur J Pharmacol. 1983 Nov 11;95(1-2):101-7 PMID: 6230246
  4. Serotonin-sensitive adenylate cyclase and [3H]serotonin binding sites in the CNS of the rat--I.
    Biochem Pharmacol. 1980 Sep 15;29(18):2445-53 PMID: 7426051
  5. Serotonin receptor binding sites affected differentially by guanine nucleotides.
    Mol Pharmacol. 1979 Nov;16(3):700-8 PMID: 530255
  6. Two 5-HT receptors linked to adenylate cyclase in guinea pig hippocampus are discriminated by 5-carboxamidotryptamine and spiperone.
    Eur J Pharmacol. 1985 Mar 12;109 (3):427-9 PMID: 3987810
  7. Characterization of the 5-HT1B recognition site in rat brain: binding studies with (-)[125I]iodocyanopindolol.
    Eur J Pharmacol. 1985 Nov 26;118(1-2):1-12 PMID: 3002805
  8. Serotonin receptors in the human brain. II. Characterization and autoradiographic localization of 5-HT1C and 5-HT2 recognition sites.
    Brain Res. 1986 Jun 18;376(1):97-107 PMID: 2941113
  9. Identification of presynaptic serotonin autoreceptors using a new ligand: 3H-PAT.
    Nature. 1983 Sep 8-14;305(5930):140-2 PMID: 6225026
  10. Biochemical assessment of the central 5-HT agonist activity of RU 24969 (a piperidinyl indole).
    Eur J Pharmacol. 1980 Apr 11;63(1):65-72 PMID: 6155275
  11. Control of adenylate cyclase activity by G proteins.
    Adv Cyclic Nucleotide Protein Phosphorylation Res. 1985;19:103-11 PMID: 3159184
  12. Serotonin-elicited amplification of adenylate cyclase activity in hippocampal membranes from adult rat.
    J Neurochem. 1983 Jun;40(6):1671-9 PMID: 6854325
  13. [3H]8-hydroxy-2-(di-n-propylamino)tetralin binding to pre- and postsynaptic 5-hydroxytryptamine sites in various regions of the rat brain.
    J Neurochem. 1985 Jun;44(6):1685-96 PMID: 3157780
  14. Radioimmunoassay for the measurement of adenosine 3',5'-cyclic phosphate.
    Proc Natl Acad Sci U S A. 1969 Sep;64(1):367-73 PMID: 4189501
  15. Statistical quality control and routine data processing for radioimmunoassays and immunoradiometric assays.
    Clin Chem. 1974 Oct;20(10):1255-70 PMID: 4370388
  16. Discrimination of multiple [3H]5-hydroxytryptamine binding sites by the neuroleptic spiperone in rat brain.
    J Neurochem. 1981 Jan;36(1):220-6 PMID: 7463047
  17. 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 Dec 1;22(23):3099-108 PMID: 4202581
  18. [3H]Ketanserin (R 41 468), a selective 3H-ligand for serotonin2 receptor binding sites. Binding properties, brain distribution, and functional role.
    Mol Pharmacol. 1982 Mar;21(2):301-14 PMID: 7099138
  19. Identity of inhibitory presynaptic 5-hydroxytryptamine (5-HT) autoreceptors in the rat brain cortex with 5-HT1B binding sites.
    Naunyn Schmiedebergs Arch Pharmacol. 1986 Jan;332(1):1-7 PMID: 2936965
  20. Quantitative autoradiographic mapping of serotonin receptors in the rat brain. I. Serotonin-1 receptors.
    Brain Res. 1985 Nov 4;346(2):205-30 PMID: 4052776
  21. Mesulergine, a selective serotonin-2 ligand in the rat cortex, does not label these receptors in porcine and human cortex: evidence for species differences in brain serotonin-2 receptors.
    Eur J Pharmacol. 1984 Nov 27;106(3):531-8 PMID: 6519174
  22. The interaction of lisuride, an ergot derivative, with serotonergic and dopaminergic receptors in rabbit brain.
    J Pharmacol Exp Ther. 1981 Mar;216(3):526-31 PMID: 7205633
  23. Quantitative autoradiographic mapping of serotonin receptors in the rat brain. II. Serotonin-2 receptors.
    Brain Res. 1985 Nov 4;346(2):231-49 PMID: 4052777
  24. SCH 23390 - the first selective dopamine D-1 antagonist.
    Eur J Pharmacol. 1983 Jul 15;91(1):153-4 PMID: 6225651
  25. Effect of non-catecholic 2-aminotetralin derivatives on dopamine metabolism in the rat striatum.
    Naunyn Schmiedebergs Arch Pharmacol. 1980 Sep;313(3):213-9 PMID: 7432553
  26. An autoradiographic analysis of the differential ascending projections of the dorsal and median raphe nuclei in the rat.
    J Comp Neurol. 1978 Jun 1;179(3):641-67 PMID: 565370
  27. Serotonin receptors in the human brain. I. Characterization and autoradiographic localization of 5-HT1A recognition sites. Apparent absence of 5-HT1B recognition sites.
    Brain Res. 1986 Jun 18;376(1):85-96 PMID: 3719375
  28. The binding of serotonergic ligands to the porcine choroid plexus: characterization of a new type of serotonin recognition site.
    Eur J Pharmacol. 1984 Nov 27;106(3):539-46 PMID: 6519175
  29. Identification of serotonin M-receptor subtypes and their specific blockade by a new class of drugs.
    Nature. 1985 Jul 11-17;316(6024):126-31 PMID: 3839291
  30. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding.
    Anal Biochem. 1976 May 7;72:248-54 PMID: 942051
  31. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor.
    J Biol Chem. 1980 Aug 10;255(15):7108-17 PMID: 6248546
  32. Ca2+-guanine nucleotide interactions in brain membranes. I. Modulation of central 5-hydroxytryptamine receptors in the rat.
    J Neurochem. 1982 Jan;38(1):151-61 PMID: 7108524
  33. Molecular pharmacology of 5-HT1 and 5-HT2 recognition sites in rat and pig brain membranes: radioligand binding studies with [3H]5-HT, [3H]8-OH-DPAT, (-)[125I]iodocyanopindolol, [3H]mesulergine and [3H]ketanserin.
    Eur J Pharmacol. 1985 Nov 26;118(1-2):13-23 PMID: 2935410
  34. Two distinct central serotonin receptors with different physiological functions.
    Science. 1981 May 15;212(4496):827-9 PMID: 7221567
  35. beta-Adrenoceptor blocking agents recognize a subpopulation of serotonin receptors in brain.
    Brain Res. 1985 Sep 23;343(2):403-8 PMID: 2864978
  36. (+/-)[125Iodo] cyanopindolol, a new ligand for beta-adrenoceptors: identification and quantitation of subclasses of beta-adrenoceptors in guinea pig.
    Naunyn Schmiedebergs Arch Pharmacol. 1981;317(4):277-85 PMID: 6119625
  37. 8-Hydroxy-2-(di-n-propylamino)-tetralin discriminates between subtypes of the 5-HT1 recognition site.
    Eur J Pharmacol. 1983 May 20;90(1):151-3 PMID: 6223827
  38. Multiple serotonin receptors: differential binding of [3H]5-hydroxytryptamine, [3H]lysergic acid diethylamide and [3H]spiroperidol.
    Mol Pharmacol. 1979 Nov;16(3):687-99 PMID: 530254
Article Info
Journal
Naunyn-Schmiedeberg's archives of pharmacology
Abbr.
Naunyn Schmiedebergs Arch Pharmacol
ISSN
0028-1298
DOI
10.1007/BF00500006
Published
1986-08-00
Pages
335-41
Language
English
Region
Germany
NLM ID
0326264
Subset
IM
External Links
PubMed source DOI: 10.1007/BF00500006 View journal details
Analysis Services
Analysis Services

Contact

No. 2 Wenbo Road, Zhangqiu District, Jinan, Shandong

Qilu Normal University · Genelibs Bioinformatics Lab

750 Shunhua Rd, Jinan

2F, Bldg F, University Science Park

Tel: 0531-88819269

WeChat Official Account

Follow our WeChat subscription account for real-time updates and the latest in medical and biological research.


Business Email

E-mail: product@genelibs.com

Copyright © 2026.Genelibs Jinan Honghui Biotechnology Co., Ltd. 鲁ICP备20007159号-2