HTR1F Membrane Protein Introduction

Introduction of HTR1F

5-hydroxytryptamine receptor 1F, also called serotonin receptor 1F, is one of the subtypes for serotonin receptor (5-HT receptor) which in human is encoded by HTR1F gene. It belongs to the G protein-coupled receptor (GPCR) family. HTR1F shares 61% sequence homology with the HTR1E receptor, which is the greatest among all the 5-HT receptors. HTR1Fs are found in spinal cord, mesentery, uterus, and brain, specifically in cortex, nucleus accumbens, striatum, amygdala, and hippocampus. And thus, HTR1F has supposed to be the subject of intense research as a target for anti-migraine drugs.

Function of HTR1F Membrane Protein

HTR1F or 5-HT1F acts as a receptor for the neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). 5-HT1F is suggested to be coupled to the inhibition of adenylyl cyclase. Activation of 5-HT1Fs in vivo is related to the inhibition of plasma extravasation in the dura, which is a component of neurogenic inflammation thought to be a possible cause of migraine. The activation of 5-HT1F receptors does not mediate constriction of human vasculature (unlike 5-HT1B/1D receptors), as this receptor is not present in blood vessels. Thus, 5-HT1F agonists would function without the unwanted cardiovascular side effects, which is a great advantage in the treatment of migraine. Furthermore, numerous preclinical studies have been indicated that the 5-HT1F mechanism seems to be primarily mediated by inhibition of pain signal transmission in the TNC (Tenascin C), in line with the central distribution of this receptor in the brainstem. Several 5-HT1F selective agonists have been developed with the hope that this mechanism could provide migraine headache relief by preventing pro-inflammatory neuropeptide release and interrupting pain signal transmission without vasoconstriction.

Fig.1 Signal transduction of 5-HT receptor subtypes. (Ohno, 2015)

Application of HTR1F Membrane Protein in Literature

1. Gibbs W. S., et al. 5-HT1F receptor regulates mitochondrial homeostasis and its loss potentiates acute kidney injury and impairs renal recovery. Am J Physiol Renal Physiol. 2018. PubMed ID: 29846105
   
   

   The results showed the 5-HT1F receptor was a component of physiological MB regulation in the kidney and its absence potentiates renal injury and impedes recovery.

2. Rubio-Beltrán E., et al. Is selective 5-HT1F receptor agonism an entity apart from that of the triptans in antimigraine therapy? Pharmacol Ther. 2018, 186:88-97. PubMed ID: 29352859
   
   

   This study found that lasmiditan possessed a high lipophilicity, which suggested a direct action on the central descending antinociceptive pathways. Furthermore, since 5-HT1F receptors were located on trigeminal fibers, they could modulate CGRP release.

3. Vila-Pueyo M., et al. Targeted 5-HT1F therapies for migraine. Neurotherapeutics. 2018, 15(2):291-303. PubMed ID: 29488143
   
   

   Authors of the study focused on the characterization of 5-HT1 receptor agonists and their effects as migraine therapies.

4. Scholpa N. E., et al. 5-HT1F receptor-mediated mitochondrial biogenesis for the treatment of Parkinson's disease. J Psychiatr Res. 2018, 175(2):348-358. PubMed ID: 29057453
   
   

   The findings indicated that the 5-HT1F receptor may be an effective therapeutic target for Parkinson's disease.

5. García-Pedraza J. Á., et al. Chronic 5-HT2 receptor blockade unmasks the role of 5-HT1F receptors in the inhibition of rat cardioaccelerator sympathetic outflow. Can J Physiol Pharmaco. 2018, 96(4):328-336. PubMed ID: 28886249
   
   

   These results demonstrated the novel mechanisms of MB (mitochondrial biogenesis), which provided the foundation for new chemicals that induced MB to treat acute and chronic organ injuries.

HTR1F Preparation Options

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Reference

1. Ohno Y., et al. (2015). New insight into the therapeutic role of the serotonergic system in Parkinson's disease. Progress in neurobiology. 134, pp.104-121.

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