» Articles » PMID: 2300586

The 5HT2 Receptor Defines a Family of Structurally Distinct but Functionally Conserved Serotonin Receptors

Overview
Specialty Science
Date 1990 Feb 1
PMID 2300586
Citations 54
Authors
Affiliations
Soon will be listed here.
Abstract

Serotonin exerts its diverse physiological effects by interacting with multiple distinct receptor subtypes. We have isolated a rat brain 5HT2 serotonin receptor cDNA by virtue of its homology with the 5HT1c receptor. The 5HT2 receptor is a member of the family of receptors that are linked to guanine nucleotide-binding proteins and are predicted to span the lipid bilayer seven times. Overall sequence identity between the 5HT2 and 5HT1c receptors is 49%, but identity within the transmembrane domains is 80%. Expression of both the 5HT2 and 5HT1c receptors in transfected mouse fibroblasts activates phospholipase C signaling pathways and promotes cellular transformation. However, RNA blotting shows that these two receptor subtypes are differentially expressed in the central nervous system. In this manner, structurally and functionally homologous receptor subtypes may elicit distinct physiologic actions.

Citing Articles

Effects of (-)-MBP, a novel 5-HT agonist and 5-HT antagonist/inverse agonist on brain activity: A phMRI study on awake mice.

Sathe P, Ramdasi G, Giammatteo K, Beauzile H, Wang S, Zhang H Pharmacol Res Perspect. 2023; 11(5):e01144.

PMID: 37837184 PMC: 10576165. DOI: 10.1002/prp2.1144.


The Role of Serotonin in Breast Cancer Stem Cells.

Gwynne W, Shakeel M, Girgis-Gabardo A, Hassell J Molecules. 2021; 26(11).

PMID: 34073226 PMC: 8198186. DOI: 10.3390/molecules26113171.


International Union of Basic and Clinical Pharmacology. CX. Classification of Receptors for 5-hydroxytryptamine; Pharmacology and Function.

Barnes N, Ahern G, Becamel C, Bockaert J, Camilleri M, Chaumont-Dubel S Pharmacol Rev. 2020; 73(1):310-520.

PMID: 33370241 PMC: 7770494. DOI: 10.1124/pr.118.015552.


Antagonists of the serotonin receptor 5A target human breast tumor initiating cells.

Gwynne W, Shakeel M, Girgis-Gabardo A, Kim K, Ford E, Dvorkin-Gheva A BMC Cancer. 2020; 20(1):724.

PMID: 32758183 PMC: 7404930. DOI: 10.1186/s12885-020-07193-6.


Computational Methods for the Identification of Molecular Targets of Toxic Food Additives. Butylated Hydroxytoluene as a Case Study.

Tortosa V, Pietropaolo V, Brandi V, Macari G, Pasquadibisceglie A, Polticelli F Molecules. 2020; 25(9).

PMID: 32397407 PMC: 7248939. DOI: 10.3390/molecules25092229.


References
1.
Bonner T, Buckley N, Young A, Brann M . Identification of a family of muscarinic acetylcholine receptor genes. Science. 1987; 237(4814):527-32. DOI: 10.1126/science.3037705. View

2.
Arquint M, Roder J, Chia L, Down J, Wilkinson D, Bayley H . Molecular cloning and primary structure of myelin-associated glycoprotein. Proc Natl Acad Sci U S A. 1987; 84(2):600-4. PMC: 304258. DOI: 10.1073/pnas.84.2.600. View

3.
Kobilka B, Frielle T, Collins S, Kobilka T, Francke U, Lefkowitz R . An intronless gene encoding a potential member of the family of receptors coupled to guanine nucleotide regulatory proteins. Nature. 1987; 329(6134):75-9. DOI: 10.1038/329075a0. View

4.
Peralta E, Ashkenazi A, Winslow J, Smith D, Ramachandran J, Capon D . Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors. EMBO J. 1987; 6(13):3923-9. PMC: 553870. DOI: 10.1002/j.1460-2075.1987.tb02733.x. View

5.
Kirschmeier P, Housey G, Johnson M, Perkins A, Weinstein I . Construction and characterization of a retroviral vector demonstrating efficient expression of cloned cDNA sequences. DNA. 1988; 7(3):219-25. DOI: 10.1089/dna.1988.7.219. View