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SB-258719; Powerful 5-HT(7) Antagonist, benefits and negatives of 5-HT7 antagonism.

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Benefits of blocking 5-HT(7) Receptors?

-Relief of depression and some aldosterone secretion.
-Partial or complete Blockade of hypothermia induced by serotonin.
-Reduction of nervous system overstimulation.

Negatives/Downsides for blocking 5-HT(7) Receptors

-Questionable but possible reduction in analgesic efficiency.
-An increase in serotonin at other receptors and reduction in GnRH; a slightly decreased testosterone level.

is a drug developed by GlaxoSmithKline which acts as a selective 5-HT7 receptor partial inverse agonist,[1] and was the first such ligand identified for 5-HT7.[2] Its use in research has mainly been in demonstrating the potential use for 5-HT7 agonists as potential novel analgesics, due to the ability of SB-258719 to block the analgesic effects of a variety of 5-HT7 agonists across several different testing models.[3][4][5][6]

Endocrine. 1997 Oct;7(2):261-5.
Serotonin directly stimulates luteinizing hormone-releasing hormone release from GT1 cells via 5-HT7 receptors.
Héry M1, François-Bellan AM, Héry F, Deprez P, Becquet D.
Author information
1Laboratoire de Neuroendocrinologie Expérimentale, INSERM U297, Faculté de Médecine Nord, Institut Fédératif Jean Roche, Marseille, France.
Luteinizing hormone-releasing hormone (LHRH release, which serves as the primary drive to the hypothalamic-pituitary gonadal axis, is controlled by many neuromediators. Serotonin has been implicated in this regulation. However, it is unclear whether the central effect of serotonin on LHRH secretion is exerted directly on LHRH neurosecretory neurons or indirectly via multisynaptic pathways. The present studies were undertaken in order to examine whether LHRH secretion from immortalized LHRH cell lines is directly regulated by serotonin and, if so, to identify the receptor subtype involved. 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), a 5-HT1A/7 receptor agonist, stimulated LHRH release from GT1-1 cells. This effect was blocked by ritanserin, a 5-HT2/7 receptor antagonist, but not by SDZ-216-525, a 5-HT1A antagonist. Basal LHRH release was not affected by the 5-HT2 agonist DOI. Reverse transcription and polymerase chain reaction technique (RT-PCR) was used in order to identify 5-HT1A and 5-HT7 receptor mRNA in immortalized LHRH cell lines. GT1-1 cells express mRNA for the 5-HT7, but not the 5-HT1A receptor subtypes. These results demonstrate a direct stimulatory effect of serotonin on LHRH release via 5-HT7 receptor.
PMID: 9549053 [PubMed - indexed for MEDLINE]

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