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Neuroreceptors

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Neurochemistry in Clinical Practice

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Abstract

The neurobiology drug discovery landscape has transformed over the past decade or so by the discovery of allosteric modulators of receptor superfamilies. A wide range of physiological reactions are able to occur in response to a limited number of neurotransmitters. In this chapter, we will describe the general features of the receptors and the signaling pathways that are generated in response to neuroreceptor activation that allow for the explanation of this vast array of neurotransmitter responses. Primarily based upon structure, receptors in the nervous system can be classified into four groups: ligand-gated receptors, G-protein coupled receptors, enzyme-linked receptors, and nuclear receptors. We identify the neuroreceptors, their endogenous agonists, antagonists, sites of expression within the nervous system, and neuropharmacological clinical use. New molecular approaches and advances in our understanding of receptor biology combined with opportunities to repurpose existing drugs for new indications continue to highlight the exciting opportunities for modulating neuroreceptors for therapeutic purposes.

Corpora non agunt nisi fixate

Compounds do not act unless bound

—Paul Ehrlich, 1908 Nobel Prize in Medicine

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Abbreviations

12(R)-HPETE:

12R-hydroperoxyeicosatetraenoic acid

4-TM:

Four transmembrane-spanning α-helices

5-HT:

5-Hydroxytryptamine

7-TM:

Seven transmembrane-spanning α-helices

A1:

Adenosine A1 receptor

A2A:

Adenosine 2A receptor

A2B:

Adenosine 2B receptor

A3:

Adenosine 3 receptor

ACh:

Acetylcholine

AChBP:

Acetylcholine-binding protein

ACKR:

Atypical chemokine receptor

ACTH:

Adrenocorticotropic hormone

ADAR:

RNA-specific adenosine deaminase

ADGR:

Adhesion G protein-coupled receptor

ADP:

Adenosine diphosphate

AF-1:

Activation function-1

AM:

Adrenomedullin

AMP:

Adenosine monophosphate

AMPA:

α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid

AMY:

Amylin

AN:

Arcuate

ANF:

Atrial natriuretic factor

ANGPT:

Angiopoietin

ANP:

Atrial natriuretic peptide

AR:

Androgen receptor

ASIC:

Acid-sensing ion channel

AT2:

Angiotensin II receptor type 2

AXL:

AXL receptor tyrosine kinase

BAI:

Brain-specific angiogenesis inhibitor

BB:

Bombesin BB receptor

BDNF:

Brain-derived neurotrophic factor

BLT:

Leukotriene B4 receptor

C3a:

Complement peptide receptor C3a

CAH:

Carbonic anhydrase

CAK:

CDC-activating kinase

CAKAK:

CAK-activating kinase

CaMK:

Calcium/calmodulin-dependent protein kinase

cAMP:

Cyclic adenosine monophosphate

CAR:

Constitutive androstane receptor

CAS:

Ca2+-Sensing

CASK:

Calcium/calmodulin-dependent serin protein kinase

CaV:

Voltage-gated calcium channel

CB:

Cannabinoid receptor

CCK:

Cholecystokinin

CCL:

C-C chemokine ligand

CCR:

C-C chemokine receptor

CD:

Cluster of differentiation

CDK:

Cyclin-dependent kinase

CELSR:

Cadherin EGF LAG seven-pass G-type receptor

cGMP:

Cyclic guanosine monophosphate

CGRP:

Calcitonin gene-related peptide

CLR:

C-type lectin receptor

CNS:

Central nervous system

CO:

Colliculi

COL3A1:

Collagen type III alpha 1 chain

COUP-TF:

Chicken ovalbumin upstream promoter-transcription factor

CP:

Caudate Putamen

CRF:

Corticotropin-releasing factor receptor type

CSF1R:

Colony stimulating factor 1 receptor

CT:

Calcitonin

CTP:

Cytidine triphosphate

CX3CL:

C-X3-C chemokine ligand

CX3CR:

C-X3-C chemokine receptor

CXCL:

Chemokine (C-X-C motif) ligand

CXCR:

Chemokine (C-X-C) motif receptor

Cys:

Cysteine

D:

Dopamine receptor D

DAG:

Diacylglycerol

DAX-1:

Dosage-sensitive sex reversal adrenal hypoplasia congenital critical region on the X chromosome, gene1

DBD:

DNA binding domain

DDR:

Discoidin domain receptor

DP:

Prostaglandin D2 receptor

DRD:

Dopamine receptors

ECD:

Extracellular domain

EGF:

Epidermal growth factor

EGFR:

Epidermal growth factor receptor

EMR1:

EGF-like module-containing mucin-like hormone receptor-like 1 (also known as F4/80)

ENaC:

Epithelial sodium channel

EP:

Prostaglandin E2 receptor

Eph:

Erythropoietin-producing

Ephrin:

Eph receptor-interacting ligand

ErbB4:

Erb-B2 receptor tyrosine kinase 4

ERK:

Extracellular signal-regulated kinase

ERK:

Extracellular signal-regulated protein kinase

ERR:

Estrogen-related receptor

ESRRG:

Estrogen-related Receptor γ

ET:

Endothelin receptor type

F2L:

Formylpeptide receptor (FPR)-like (FPRL)-2 ligand

FGF:

Fibroblast growth factor

FGFR:

Fibroblast growth factor receptor

FLT3:

FMS-like tyrosine kinase 3

FLT3L:

FMS-like tyrosine kinase 3 ligand

FN:

Fibronectin

FN-III:

Fibronectin type III domain

FP:

Prostaglandin F receptor

FPR:

Formyl peptide receptor

FSH:

Follicle stimulating hormone receptor

FXR:

Farnesoid X receptor

FZD:

Frizzled

GABA:

Gamma-aminobutyric acid

GABAA:

Gamma-aminobutyric acid A receptor

GABAB:

Gamma-aminobutyric acid B receptor

GABP:

GA-binding protein

GAL:

Galanin

GAL:

Galanin receptor

GC:

Guanylate cyclase

GCNF:

Germ cell nuclear factor

GHRH:

Growth hormone–releasing hormone

GHRHR:

Growth hormone–releasing hormone receptor

GIP:

Glucose-dependent insulinotropic polypeptide

GIRK:

G protein-coupled inwardly-rectifying potassium channels

GLEPP:

Glomerular epithelial protein

GLP:

Glucagon-like peptide

Glu:

Glutamate

GluA:

Ca2+-permeable AMPA receptor

GluK:

Kainate receptor

GluN:

NMDA receptor

GluR:

Glutamate receptor

Gly:

Glycine

GlyR:

Glycine receptor

GlyT1:

Glycine transporter 1

GlyT2:

Glycine transporter 2

GnRH:

Gonadotropin-releasing hormone

GPBA:

G protein-coupled bile acid

GPCR:

G protein-coupled receptor

GPER:

G protein-coupled estrogen receptor

GR:

Glucocorticoid receptor

GRK:

G protein receptor kinase

GRP:

Gastrin-releasing peptide

GTP:

Guanosine triphosphate

Gα:

Gα Protein subunit

Gαgustducin:

Gα Protein, gustducin subunit (taste specificity)

Gαi:

Gα Protein, inhibitory subunit; adenylate cyclase inactivated, cAMP down

Gαo:

Gα Protein, other subunit

H:

Hippocampus

H:

Histamine receptor H

HAT:

Histone acetyltransferase

HB-EGF:

Heparin-binding EGF-like growth factor

HCA:

Hydroxycarboxylic acid receptor

HCF:

Heregulin

hCG:

Human chorionic gonadotropin

HDAC:

Histone deacetylase

HGF:

Hepatocyte growth factor

HIV:

Human immunodeficiency virus

HNF4:

Hepatic nuclear factor 4 receptor

HR:

Hormone receptor

HY:

Hypothalamus

IA2:

Islet tyrosine phosphatase

IGF:

Insulin-like growth factor

iGlu:

Ionotropic glutamate

iGluR:

Ionotropic glutamate receptor

INaC:

Intestine sodium channel receptor

IP:

Prostaglandin receptor

IP3:

Inositol 1,4,5- trisphosphate

IP3R:

Inositol 1,4,5-trisphosphate receptor

JNK:

c-Jun amino-terminal kinase

KIM:

Kinase interaction motif

Kit:

Tyrosine protein kinase

LAR:

Ligand-binding domain

LBP:

Ligand-binding pocket

LH:

Luteinizing hormone

LL-37:

Antimicrobial peptide belonging to the cathelicidin family

LMR:

Lemur kinase receptor subfamily

LPA:

Lysophosphatidic acid receptor

LRH-1:

Liver receptor homolog-1

LTB:

Leukotriene

LTK:

Leukocyte tyrosine kinase

LTX:

α-Latrotoxin

LXA4:

Lipoxin A4

LXR:

Liver X receptor

M:

Muscarinic acetylcholine receptor M

mAChR:

Muscarinic acetylcholine receptor

MAM:

Meprin-A5-μ domain

MAP2K:

Mitogen-activated protein kinase

MAPK:

Mitogen-activated protein kinase

MC:

Melanocortin

MCH:

Melanin-concentrating hormone receptor

MEK:

Mitogen-activated protein kinase

MER-TK:

Mer tyrosine kinase receptor

Mg:

Magnesium

mGlu:

Metabotropic glutamate

mGluR:

Metabotropic glutamate receptor

MR:

Mineralocorticoid receptor

MSH:

Melanocyte stimulating hormone

MT1:

Melatonin receptor type 1A

MuSK:

Muscle-associated receptor tyrosine kinase

Myt:

Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase

N/OFQ:

Nociceptin/orphanin Fq

nAChR:

Nicotinic acetylcholine receptors

NCOA1:

Nuclear receptor coactivator 1

NCoR:

Nuclear receptor corepressor

NF-κB:

Nuclear factor-κb

NGF:

Nerve growth factor

NK1:

Tachykinin receptor 1

NMDA:

N-methyl-d-aspartate

NMU1:

Neuromedin U receptor

NO:

Nitric oxide

NOP:

Nociception opioid peptide receptor

NOR:

Neuron-derived orphan receptor

NPBW:

Neuropeptide B/W receptor

NPFF:

Neuropeptide FF receptor

NPS:

Neuropeptide S

NPY:

Neuropeptide Y

NR0B:

Nuclear receptor subfamily 0 group B member

Nrg:

Neuregulin

NT:

Neurotrophin

NTD:

N-terminal domain

NTS:

Neurotensin receptor type

NURR1:

Nurr-related receptor factor 1

oGPCR:

Orphan G protein-coupled receptor

OPN1LW:

Opsin 1, long wave sensitive

OPN1MW:

Opsin 1, medium wave sensitive

OPN1SW:

Opsin 1, short wave sensitive

OX:

Orexin receptor type

P2X:

Adenosine triphosphate–gated cation channel P2X purinoceptor

P2Y:

G Protein-gated P2Y purinoceptor

PAC:

Pituitary adenylate cyclase

PAC1:

Pituitary adenylate cyclase–activating polypeptide-selective type I receptor

PACAP:

Pituitary adenylate cyclase–activating polypeptide

PAF:

Platelet-activating factor

PAM:

Positive allosteric modulator

PAR:

Protease-activated receptor

PDGF:

Platelet-derived growth factor

PDGFR:

Platelet-derived growth factor receptor

PGR:

Progesterone receptor

PHM:

Peptide histidine methionine

PHV:

Peptide histidine valine

PI3Kγ:

Phosphoinositide 3-kinase γ

PKA:

Protein kinase A

PKC:

Protein kinase C

PKG:

Protein kinase G

PKR1:

Prokineticin receptor 1

PKR2:

Prokineticin receptor 2

PLC-β:

Phospholipase C-β

PNR :

Photoreceptor cell-specific nuclear receptor

PP1:

Protein phosphatase 1

PPAR:

Peroxisome proliferator-activated receptor

PR:

Progesterone receptor

PrP:

Prion protein

PrRP:

Prolactin-releasing peptide

PTEN :

Phosphatase and tensin homolog deleted on chromosome 10

PTH:

Parathyroid hormone receptor

PTHrP:

Parathyroid hormone–related protein

PTK:

Protein tyrosine kinase

PTP:

Protein tyrosine phosphatase

PXR:

Pregnane X receptor

PYY:

Peptide YY

QRFP:

Neuropeptide 26RFa

RACK:

Receptors for activated C kinase

RAMP:

Receptor activity-modifying proteins

RAPGEF3:

Rap guanine nucleotide exchange factor 3

RAR:

Retinoic acid receptor

RARα:

Retinoic acid receptor

RDGS:

Peptides containing the sequence Arg-Gly-Asp-Ser

RET:

Ret proto-oncogene

REV-ERB:

Reverse-Erb receptor

REV-ERBα:

Reverse-Erb-Α

REV-ERBβ:

Reverse-Erb-Î’

rGC:

Receptor guanylyl cyclase

Rho:

Rho family of GTPases belong to the Ras superfamily of proteins

RhoA:

Ras homolog family member, a Rho family GTPase

RIP 140:

Receptor-interacting protein 140

ROR:

Retinoic acid–related orphan receptor

ROS:

Proto-oncogene that encodes an orphan receptor-type tyrosine kinase

RPTP:

Receptor-like protein tyrosine phosphatase

RSTK:

Receptor serine–threonine kinase

RXFP:

Relaxin family peptide

RXR:

Retinoid X receptor

RYK:

Transmembrane receptor tyrosine kinase

S1P:

Sphingosine-1-phosphate

SAP:

SLAM-associated protein

SAPK:

Stress-activated protein kinase

SCAM:

Substituted cysteine accessibility method

SCF:

Stem cell factor

SEA:

Stearoylethanolamide

SF-1:

Steroidogenic factor 1

SFK:

Src family of protein tyrosine kinases

SHH:

Sonic hedgehog

SHP:

Small heterodimer partner

SHP-2:

SH2 domain–containing protein tyrosine phosphatase-2

SK3:

Glycogen synthase kinase 3

SMO:

Smoothened

SMRT:

Silencing mediator of retinoic acid thyroid hormone receptors

SNARE:

Soluble-N-ethylmaleimide-sensitive-factor accessory-protein receptor

SRC:

Steroid receptor coactivator

SRIF:

Somatotropin release–inhibiting factor; also known as somatostatin

SST:

Somatostatin receptor

STEP:

Striatal-enriched phosphatase

STYK1:

Serine/threonine/tyrosine kinase 1

SUMO:

Small ubiquitin–related modifier

TAM:

Typo3, Axl, and Mer family of tyrosine kinase receptors

TAS1R:

Taste 1 Receptor

TGF:

Transforming growth factor

THRA:

Thyroid hormone receptor α

THRB:

Thyroid hormone receptor β

Tie:

Tyrosine kinase with immunoglobulin like and EGF-like domains

TKAR:

Tyrosine kinase–associated receptors

TLX:

The human orphan nuclear receptor tailless; also known as NR2E1

TNF:

Tumor necrosis factor

TP:

Thromboxane receptor

TR:

Thyroid hormone receptor

TRH:

Thyrotropin-releasing hormone

TrK:

Tropomyosin receptor kinase

TYRO3:

TAM family receptor tyrosine kinase

Ucn:

Urocortin

UDP:

Uridine diphosphate

UT:

Urotensin

UTP:

Uridine-5′-triphosphate

VDR:

Vitamin D receptor

VEGFR:

Vascular endothelial growth factor receptor

VIP:

Vasoactive intestinal peptide

VIPR:

Vasoactive intestinal peptide receptor

VPAC:

Vasoactive intestinal polypeptide receptor

Wnt:

Coined from the drosophila gene Wingless and the mouse oncogene Int-1.

WNT:

Superfamily of Wnt signaling proteins

Y:

Neuropeptide Y receptor

ZAC:

Zinc-activated channel receptor

Zn:

Zinc

α12A:

Adrenoreceptor type α2A

α12AB:

Adrenoreceptor type α2B

α12AC:

Adrenoreceptor type α2C

α1A:

Adrenoreceptor type α1A

α1B:

Adrenoreceptor type α1B

α1D:

Adrenoreceptor type α1D

β:

β-adrenergic receptor

βARK:

β-adrenergic receptor kinase

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Acknowledgments

The author acknowledges technical input by Benjamin Schoeder and Schengwei Wu. This work was supported by National Institutes of Health Grant R01 ES022966 (to S.C.M.).

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Authors and Affiliations

  1. Department of Surgery, University of Missouri School of Medicine, Columbia, MO, USA

    Susan C. McKarns

  2. Department of Molecular Microbiology and Immunology, University of Missouri School of Medicine, Columbia, MO, USA

    Susan C. McKarns

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  1. Susan C. McKarns
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Correspondence to Susan C. McKarns .

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Editors and Affiliations

  1. Department of Neurology, University of South Carolina School of Medicine, Prisma Health, Columbia, SC, USA

    Pradeep C. Bollu

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McKarns, S.C. (2022). Neuroreceptors. In: Bollu, P.C. (eds) Neurochemistry in Clinical Practice. Springer, Cham. https://doi.org/10.1007/978-3-031-07897-2_15

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  • DOI: https://doi.org/10.1007/978-3-031-07897-2_15

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  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-031-07896-5

  • Online ISBN: 978-3-031-07897-2

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