5-HTR3E Membrane Protein Introduction

Introduction of 5-HTR3E

5-HTR3E is encoded by 5-HTR3E gene. It is one of 5-HTR3 receptor subunits. 5-HTR3 receptor is composed of five 5-HTR3A receptor subunits forming homomeric receptors or at least 5-HTR3A receptor subunit in combination with one or more of the 5-HTR3B, 5-HTR3C, 5-HTR3D and 5-HTR3E receptor subunits forming complex heteromers. Each subunit contains an extracellular N-terminal and C-terminal domain, a transmembrane domain comprised of four alpha helices (M1-M4), and a large cytoplasmic domain.

Function of 5-HTR3E Membrane Protein

5-HTR3E, a 5-HTR3 receptor subunit, plays a very important role in neurotransmission involved many physiological functions. 5-HTR3 receptor is widely expressed in the central and peripheral nervous systems. It is a ligand-gated ion channel which mediates Na⁺, K⁺, and Ca²⁺ permeability. Activated 5-HTR3 receptors by binding 5-HTR mediate neuronal excitation and depolarization through regulating inward current. It has been revealed that the stimulation of 5-HTR3 receptors could affect the cardiovascular function, expand blood vessel and disturb respiration. Moreover, the activated 5-HTR3 receptors in CNS lead to mental disorder, anxiety, cognitive disorder, the reward and withdrawal effect from drugs of abuse and eating disorders. Hence 5-HTR3 antagonists are promising therapeutic agents for psychosis, anxiety disorder, impaired cognitive and learning ability, as well as alcohol and certain drugs of abuse. 5-HTR3 receptor antagonists have been identified to reduce alcohol consumption. And 5-HTR3 receptor antagonists can also apply to decrease nausea and emesis in cancer patients accepting chemotherapy.

Fig.1 The mouse 5-HTR3 receptor as determined by X-ray crystallography.

Application of 5-HTR3E Membrane Protein in Literature

1. Yaakob N.S., et al. The C and E subunits of the serotonin 5-HT 3 receptor subtly modulate electrical properties of the receptor. Biomedicine & Pharmacotherapy. 2018, 97:1701-1709. PubMed ID: 29793334
   
   

   The study shows that the simple or complex heteromeric 5-HT3 receptors assembled by C and E subunits may change the action of 5-HT and clinically used antagonists, such as ondansetron and palonosetron.

2. Mori M., et al. 5-HT3, antagonists decrease discounting rate without affecting sensitivity to reward magnitude in the delay discounting task in mice. Psychopharmacology. 2018, 235(9):2619-2629. PubMed ID: 29955899
   
   

   The study identifies that 5-HT3 antagonism controls impulsive choice through reducing discounting rates without affecting sensitivity to reinforcer magnitude in mice.

3. Pottoo F.H., et al. Estrogen and serotonin: complexity of interactions and implications for epileptic seizures and epileptogenesis. Curr Neuropharmacol. 2018. PubMed ID: 29956631
   
   

   The review summarizes the 5-HT1A and 5-HT3 receptors can act as the potential targets for reducing seizure induced recurrent hypersynchronous neuronal activity and neurodegeneration.

4. Kou W., et al. Nephrotoxicity evaluation on cisplatin combined with 5-HT3 receptor antagonists: a retrospective study. Biomed Res Int. 2018, 1024324. PubMed ID: 29977907
   
   

   The study shows that the higher dosage cisplatin and 5-HT3 receptor antagonist ondansetron combined with cisplatin possibly enhance the incidence of nephrotoxicity. However, 5-HT3 receptor antagonist tropisetron have a relatively moderate effect on kidney function, which indicates tropisetron can be a preferable alternative in the process of cisplatin chemotherapy.

5. Perez-Palomar B., et al. Serotonin 5-HT3 receptor antagonism potentiates the antidepressant activity of citalopram. Neuropharmacology. 2018, 133:491-502. PubMed ID: 29477299
   
   

   The study shows that 5-HT3 receptor antagonism combined with selective serotonin reuptake inhibitor (SSRI) citalopram could increase antidepressant activity.

5-HTR3E Preparation Options

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