CHRM5 Membrane Protein Introduction

Introduction of CHRM5

CHRM5, encoded by CHRM5 gene, is a member of G protein-coupled receptors family which has seven distinctive transmembrane domains. It is one of five subtypes of muscarinic receptors, M1-M5, widely expressed on the numerous cell types in the central nervous system. It has been shown that muscarinic receptors are the promising treatment targets for a number of pathological conditions of the central nervous system.

Function of CHRM5 Membrane Protein

CHRM5 can couple to G_q protein and mediate many of the diverse actions of acetylcholine in the central nervous system (CNS), as well as throughout non-nervous tissues innervated by the parasympathetic nervous system. The activation of M5 receptor activates phospholipase C, leading to release of calcium from the endoplasmic reticulum via the regulation of inositol trisphosphate and to activate protein kinase C by the mediation of diacylglycerol. In rodents, CHRM5 is important for prolonged dopamine release which is associated with schizophrenia. And it has been revealed that polymorphisms in CHRM5 gene combined with the alpha7-nicotinic receptor (CHRNA7) gene may be linked to schizophrenia. Moreover, CHRM5 upregulates in human lymphocytes during immunological responses which suggest that it may be involved in immune response. Additionally, like other subtypes of muscarinic receptors, M5 receptor also can be regarded as a therapeutic target for treating neurodegenerative disorders.

Fig.1 The structure and signaling pathways of muscarinic and nicotinic acetylcholine receptors. (Jones, 2012)

Application of CHRM5 Membrane Protein in Literature

1. Berizzi A E., et al. Muscarinic M5 receptors modulate ethanol seeking in rats. Neuropsychopharmacology. 2018, 43(7): 1510-7. PubMed ID: 29483658
   
   

   The study reveals that ML375, a selective negative M5 muscarinic acetylcholine receptor allosteric modulator in rat, inhibits ethanol self-administration and decreases cue-induced reinstatement of ethanol seeking in ethanol-preferring (iP) rats. This suggests that M5 muscarinic acetylcholine receptor is a potential drug target for treating alcohol use disorders (AUDs).

2. Deckmann K., et al. Muscarinic receptors 2 and 5 regulate bitter response of urethral brush cells via negative feedback. Faseb Journal. 2018, 32(6): 2903-10. PubMed ID: 29401598
   
   

   It is reported that a cholinergic chemosensory cell in the urethral epithelium and urethral brush cell is identified and it activates a reflex detrusor under stimulation with bitter or bacterial substances. The study reveals that muscarinic receptors 2 and 5 can reduce bitter response of urethral brush cell through a negative autocrine feedback mechanism. Moreover, muscarinic receptors 5 dysfunctions may generate bladder overactivity.

3. Monica F., et al. Heat shock protein (Hsp) regulation by muscarinic acetylcholine receptor (mAChR) activation in the rat hippocampus. Journal of Cellular Physiology. 2018, 233(8): 6107-6116. PubMed ID: 29323700
   
   

   The study indicates that the activation of muscarinic acetylcholine receptor may be associated with the treatment of neurodegenerative disorders correlated with protein aggregation, such as Alzheimer disease.

4. Gunter B W., et al. Selective inhibition of M5 muscarinic acetylcholine receptors attenuates cocaine self-administration in rats. Addiction Biology. 2017, 136(Pt C): 362-373. PubMed ID: 29138080
   
   

   The research firstly indicates that the selective inhibition of muscarinic receptors 5, M5 NAM ML375, can reduce both the reinforcing effects and the relative strength of cocaine. This suggests that M5 NAMs may be considered as a potential therapeutic target for treatment cocaine use disorder (CUD).

5. Radu B M., et al. All muscarinic acetylcholine receptors (M1-M5) are expressed in murine brain microvascular endothelium. Scientific Reports. 2017, 7(1): 5083. PubMed ID: 28698560
   
   

   This article shows the expression of all muscarinic acetylcholine receptors (M1-M5) in mouse brain microvascular endothelium. M2, M3, and M5 expression are related to their respective protein levels, but no relationship between M1 and M4 expression and protein levels. Besides, acetylcholine with muscarinic receptors activates calcium transients in brain endothelium.

CHRM5 Preparation Options

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Reference

1. Jones C K, et al. (2012). Muscarinic and nicotinic acetylcholine receptor agonists and allosteric modulators for the treatment of schizophrenia. Neuropsychopharmacology. 37(1): 16.

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