Cholecystokinin A receptor

PDB rendering based on 1d6g.

Available structures

Ortholog search: PDBe, RCSB

List of PDB id codes
1D6G, 1HZN, 1PB2

Identifiers

Symbols

CCKAR ; CCK-A; CCK1-R; CCK1R; CCKRA

External IDs

OMIM: 118444 MGI: 99478 HomoloGene: 37337 IUPHAR: 76 ChEMBL: 1901 GeneCards: CCKAR Gene

Gene ontology
Molecular function	• cholecystokinin receptor activity • peptide binding
Cellular component	• lysosome • endosome • endoplasmic reticulum • cytosol • plasma membrane • integral component of plasma membrane • terminal bouton
Biological process	• temperature homeostasis • gastric acid secretion • neuron migration • reduction of food intake in response to dietary excess • phospholipase C-activating G-protein coupled receptor signaling pathway • positive regulation of cytosolic calcium ion concentration • axonogenesis • response to nutrient • digestion • feeding behavior • response to radiation • response to heat • insulin secretion • pancreatic juice secretion • forebrain development • pancreas development • organ regeneration • actin cytoskeleton reorganization • response to lipopolysaccharide • cellular response to hormone stimulus • cholecystokinin signaling pathway • response to starvation • regulation of potassium ion transport • regulation of hormone secretion • response to glucocorticoid • regulation of calcium ion transport • positive regulation of somatostatin secretion • response to peptide
Sources: Amigo / QuickGO

RNA expression pattern

More reference expression data

Orthologs

Species

Human

Mouse

886

RefSeq (mRNA)

RefSeq (protein)

Location (UCSC)

Chr 4:
26.48 – 26.49 Mb

Chr 5:
53.7 – 53.71 Mb

PubMed search

Cholecystokinin A receptor, N-terminal domain

molecular complex of cholecystokinin-8 and n-terminus of the cholecystokinin a receptor by nmr spectroscopy

Identifiers

Symbol

CholecysA-Rec_N

Available protein structures:
Pfam	structures
PDB	RCSB PDB; PDBe; PDBj
PDBsum	structure summary

The Cholecystokinin A receptor is a human protein, also known as CCKAR or CCK₁, with CCK₁ now being the IUPHAR-recommended name.

Function

This gene encodes a G-protein coupled receptor that binds sulfated members of the cholecystokinin (CCK) family of peptide hormones. This receptor is a major physiologic mediator of pancreatic enzyme secretion and smooth muscle contraction of the gallbladder and stomach. In the central and peripheral nervous system this receptor regulates satiety and the release of beta-endorphin and dopamine.^[1]

The extracellular, N-terminal, domain of this protein adopts a tertiary structure consisting of a few helical turns and a disulfide-cross linked loop. It is required for interaction of the cholecystokinin A receptor with its corresponding hormonal ligand.^[2]

Selective Ligands

Agonists

Cholecystokinin
Gastrin
CCK-4
SR-146,131
A-71623 - modified tetrapeptide, potent and selective CCK_A agonist, IC₅₀ 3.7nM, 1200x selectivity over CCK_B, CAS# 130408-77-4

Antagonists

Proglumide
Lorglumide
Devazepide
Dexloxiglumide
Asperlicin
SR-27897
IQM-95333
JNJ-17156516

References

↑ "Entrez Gene: CCKAR cholecystokinin A receptor".
↑ Pellegrini M, Mierke DF (Nov 1999). "Molecular complex of cholecystokinin-8 and N-terminus of the cholecystokinin A receptor by NMR spectroscopy". Biochemistry 38 (45): 14775–83. doi:10.1021/bi991272l. PMID 10555959.

External links

"Cholecystokinin Receptors: CCK₁". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology.

Varga G, Bálint A, Burghardt B, D'Amato M (Apr 2004). "Involvement of endogenous CCK and CCK1 receptors in colonic motor function". British Journal of Pharmacology 141 (8): 1275–84. doi:10.1038/sj.bjp.0705769. PMC 1574909. PMID 15100163.
Wang J, Si YM, Liu ZL, Yu L (Jun 2003). "Cholecystokinin, cholecystokinin-A receptor and cholecystokinin-B receptor gene polymorphisms in Parkinson's disease". Pharmacogenetics 13 (6): 365–9. doi:10.1097/00008571-200306000-00008. PMID 12777967.
Miller LJ, Holicky EL, Ulrich CD, Wieben ED (Oct 1995). "Abnormal processing of the human cholecystokinin receptor gene in association with gallstones and obesity". Gastroenterology 109 (4): 1375–80. doi:10.1016/0016-5085(95)90601-0. PMID 7557108.
Huppi K, Siwarski D, Pisegna JR, Wank S (Feb 1995). "Chromosomal localization of the gastric and brain receptors for cholecystokinin (CCKAR and CCKBR) in human and mouse". Genomics 25 (3): 727–9. doi:10.1016/0888-7543(95)80018-H. PMID 7759110.
de Weerth A, Pisegna JR, Huppi K, Wank SA (Jul 1993). "Molecular cloning, functional expression and chromosomal localization of the human cholecystokinin type A receptor". Biochemical and Biophysical Research Communications 194 (2): 811–8. doi:10.1006/bbrc.1993.1894. PMID 8343165.
Ulrich CD, Ferber I, Holicky E, Hadac E, Buell G, Miller LJ (May 1993). "Molecular cloning and functional expression of the human gallbladder cholecystokinin A receptor". Biochemical and Biophysical Research Communications 193 (1): 204–11. doi:10.1006/bbrc.1993.1610. PMID 8503909.
Kennedy K, Gigoux V, Escrieut C, Maigret B, Martinez J, Moroder L, Fréhel D, Gully D, Vaysse N, Fourmy D (Jan 1997). "Identification of two amino acids of the human cholecystokinin-A receptor that interact with the N-terminal moiety of cholecystokinin". The Journal of Biological Chemistry 272 (5): 2920–6. doi:10.1074/jbc.272.5.2920. PMID 9006937.
Inoue H, Iannotti CA, Welling CM, Veile R, Donis-Keller H, Permutt MA (Jun 1997). "Human cholecystokinin type A receptor gene: cytogenetic localization, physical mapping, and identification of two missense variants in patients with obesity and non-insulin-dependent diabetes mellitus (NIDDM)". Genomics 42 (2): 331–5. doi:10.1006/geno.1997.4749. PMID 9192855.
Gigoux V, Escrieut C, Silvente-Poirot S, Maigret B, Gouilleux L, Fehrentz JA, Gully D, Moroder L, Vaysse N, Fourmy D (Jun 1998). "Met-195 of the cholecystokinin-A receptor interacts with the sulfated tyrosine of cholecystokinin and is crucial for receptor transition to high affinity state". The Journal of Biological Chemistry 273 (23): 14380–6. doi:10.1074/jbc.273.23.14380. PMID 9603948.
Funakoshi A, Fukamizu Y, Miyasaka K (2000). "Mechanism of cholecystokinin-A- receptor antagonist on human pancreatic exocrine secretion. Localization of CCK-A receptor in the human duodenum". Digestion. 60 Suppl 1: 75–80. doi:10.1159/000051459. PMID 10026437.
Gigoux V, Escrieut C, Fehrentz JA, Poirot S, Maigret B, Moroder L, Gully D, Martinez J, Vaysse N, Fourmy D (Jul 1999). "Arginine 336 and asparagine 333 of the human cholecystokinin-A receptor binding site interact with the penultimate aspartic acid and the C-terminal amide of cholecystokinin". The Journal of Biological Chemistry 274 (29): 20457–64. doi:10.1074/jbc.274.29.20457. PMID 10400673.
Gigoux V, Maigret B, Escrieut C, Silvente-Poirot S, Bouisson M, Fehrentz JA, Moroder L, Gully D, Martinez J, Vaysse N, Fourmy AD (Nov 1999). "Arginine 197 of the cholecystokinin-A receptor binding site interacts with the sulfate of the peptide agonist cholecystokinin". Protein Science 8 (11): 2347–54. doi:10.1110/ps.8.11.2347. PMC 2144185. PMID 10595537.
Funakoshi A, Miyasaka K, Matsumoto H, Yamamori S, Takiguchi S, Kataoka K, Takata Y, Matsusue K, Kono A, Shimokata H (Jan 2000). "Gene structure of human cholecystokinin (CCK) type-A receptor: body fat content is related to CCK type-A receptor gene promoter polymorphism". FEBS Letters 466 (2-3): 264–6. doi:10.1016/S0014-5793(00)01080-2. PMID 10682840.
Tachikawa H, Harada S, Kawanishi Y, Okubo T, Shiraishi H (Apr 2000). "Novel polymorphisms of the human cholecystokinin A receptor gene: an association analysis with schizophrenia". American Journal of Medical Genetics 96 (2): 141–5. doi:10.1002/(SICI)1096-8628(20000403)96:2<141::AID-AJMG3>3.0.CO;2-R. PMID 10893485.
Giragossian C, Mierke DF (Apr 2001). "Intermolecular interactions between cholecystokinin-8 and the third extracellular loop of the cholecystokinin A receptor". Biochemistry 40 (13): 3804–9. doi:10.1021/bi002659n. PMID 11300760.
Schmitz F, Schrader H, Otte J, Schmitz H, Stüber E, Herzig K, Schmidt WE (Sep 2001). "Identification of CCK-B/gastrin receptor splice variants in human peripheral blood mononuclear cells". Regulatory Peptides 101 (1-3): 25–33. doi:10.1016/S0167-0115(01)00281-6. PMID 11495676.
Tachikawa H, Harada S, Kawanishi Y, Okubo T, Suzuki T (Sep 2001). "Linked polymorphisms (-333G>T and -286A>G) in the promoter region of the CCK-A receptor gene may be associated with schizophrenia". Psychiatry Research 103 (2-3): 147–55. doi:10.1016/S0165-1781(01)00276-1. PMID 11549403.
Schmitz F, Göke MN, Otte JM, Schrader H, Reimann B, Kruse ML, Siegel EG, Peters J, Herzig KH, Fölsch UR, Schmidt WE (Dec 2001). "Cellular expression of CCK-A and CCK-B/gastrin receptors in human gastric mucosa". Regulatory Peptides 102 (2-3): 101–10. doi:10.1016/S0167-0115(01)00307-X. PMID 11730982.
Okubo T, Harada S, Higuchi S, Matsushita S (Aug 2002). "Investigation of quantitative trait loci in the CCKAR gene with susceptibility to alcoholism". Alcoholism, Clinical and Experimental Research 26 (8 Suppl): 2S–5S. doi:10.1097/01.ALC.0000026826.96191.FB. PMID 12198366.
Takata Y, Takeda S, Kawanami T, Takiguchi S, Yoshida Y, Miyasaka K, Funakoshi A (2003). "Promoter analysis of human cholecystokinin type-A receptor gene". Journal of Gastroenterology 37 (10): 815–20. doi:10.1007/s005350200135. PMID 12424565.

This article incorporates text from the United States National Library of Medicine, which is in the public domain.

PDB gallery

1d6g: MOLECULAR COMPLEX OF CHOLECYSTOKININ-8 AND N-TERMINUS OF THE CHOLECYSTOKININ A RECEPTOR BY NMR SPECTROSCOPY

Cell surface receptor: G protein-coupled receptors

Class A: Rhodopsin like

Neurotransmitter

Adrenergic	α1 (A B D) α2 (A B C) β1 β2 β3

Purinergic	Adenosine (A1 A2A A2B A3) P2Y (1 2 4 5 6 8 9 10 11 12 13 14)

Serotonin	(all but 5-HT3) 5-HT1 (A B D E F) 5-HT2 (A B C) 5-HT (4 5A 6 7)

Other	Acetylcholine (M1 M2 M3 M4 M5) Dopamine (D1 D2 D3 D4 D5) Histamine (H1 H2 H3 H4) Melatonin (1A 1B 1C) TAAR (1 2 3 5 6 8 9)

Metabolites and
signaling molecules

Eicosanoid	CysLT (1 2) LTB4 (1 2) FPRL1 OXE Prostaglandin (DP (1 2), EP (1 2 3 4), FP) Prostacyclin Thromboxane

Other	Bile acid Cannabinoid (CB1 CB2, GPR (18 55 119)) EBI2 Estrogen Free fatty acid (1 2 3 4) Lactate Lysophosphatidic acid (1 2 3 4 5 6) Lysophospholipid (1 2 3 4 5 6 7 8) Niacin (1 2) Oxoglutarate PAF Sphingosine-1-phosphate (1 2 3 4 5) Succinate

Peptide

Neuropeptide	B/W (1 2) FF (1 2) S Y (1 2 4 5) Neuromedin (B U (1 2)) Neurotensin (1 2)

Other	Anaphylatoxin (C3a C5a) Angiotensin (1 2) Apelin Bombesin (BRS3 GRPR NMBR) Bradykinin (B1 B2) Chemokine Cholecystokinin (A B) Endothelin (A B) Formyl peptide (1 2 3) FSH Galanin (1 2 3) GHB receptor Gonadotropin-releasing hormone (1 2) Ghrelin Kisspeptin Luteinizing hormone/choriogonadotropin MAS (1 1L D E F G X1 X2 X3 X4) Melanocortin (1 2 3 4 5) MCHR (1 2) Motilin Opioid (Delta Kappa Mu Nociceptin & Zeta, but not Sigma) Orexin (1 2) Oxytocin Prokineticin (1 2) Prolactin-releasing peptide Relaxin (1 2 3 4) Somatostatin (1 2 3 4 5) Tachykinin (1 2 3) Thyrotropin Thyrotropin-releasing hormone Urotensin-II Vasopressin (1A 1B 2)

Miscellaneous

Orphan	GPR (1 3 4 6 12 15 17 18 19 20 21 22 23 25 26 27 31 32 33 34 35 37 39 42 44 45 50 52 55 61 62 63 65 68 75 77 78 81 82 83 84 85 87 88 92 101 103 109A 109B 119 120 132 135 137B 139 141 142 146 148 149 150 151 152 153 160 161 162 171 173 174 176 177 182 183)

Other	Adrenomedullin Olfactory Opsin (3 4 5 1LW 1MW 1SW RGR RRH) Protease-activated (1 2 3 4) SREB (1 2 3)

Class B: Secretin like

Adhesion	ADGRG (1 2 3 4 5 6 7)

Orphan	GPR (56 64 97 98 110 111 112 113 114 115 116 123 124 125 126 128 133 143 144 155 157)

Other	Brain-specific angiogenesis inhibitor (1 2 3) Cadherin (1 2 3) Calcitonin CALCRL CD97 Corticotropin-releasing hormone (1 2) EMR (1 2 3) Glucagon (GR GIPR GLP1R GLP2R) Growth hormone releasing hormone PACAPR1 GPR Latrophilin (1 2 3 ELTD1) Methuselah-like proteins Parathyroid hormone (1 2) Secretin Vasoactive intestinal peptide (1 2)

Class C: Metabotropic glutamate / pheromone

Taste	TAS1R (1 2 3) TAS2R (1 3 4 5 7 8 9 10 13 14 16 19 20 30 31 38 39 40 41 42 43 45 46 50 60)

Other	Calcium-sensing receptor GABA B (1 2) Glutamate receptor (Metabotropic glutamate (1 2 3 4 5 6 7 8)) GPRC6A GPR (156 158 179) RAIG (1 2 3 4)

Class F: Frizzled / Smoothened

Frizzled	Frizzled (1 2 3 4 5 6 7 8 9 10)

Smoothened	Smoothened

Neuropeptide receptors

G protein-coupled receptor

Hormone receptors

Hypothalamic	CRH FSH LHRH TRH Somatostatin

Pituitary	Vasopressin 1A 1B 2 Oxytocin LHCG TSH

Other	Atrial natriuretic factor NPR3 Calcitonin Cholecystokinin A B VIP

Opioid receptors

Other neuropeptide receptors

Type I cytokine receptor

GH
Prolactin

Enzyme-linked receptor

Atrial natriuretic factor
- NPR1
- NPR2

Other

Sigma
- 1
- 2

Peptide receptor modulators

Adiponectin

AdipoR₁	Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon (–)-Arctigenin Arctiin Gramine Matairesinol Antagonists: Peptide: ADP-400

AdipoR₂	Agonists: Peptide: Adiponectin ADP-355 ADP-399; Non-peptide: AdipoRon Deoxyschizandrin Parthenolide Syringing Taxifoliol Antagonists: Peptide: ADP-400

Angiotensin

Agonists: Angiotensin II
Angiotensin III
Angiotensin IV
Saralasin

Antagonists: Abitesartan
Azilsartan
Azilsartan medoxomil
Candesartan
Elisartan
Embusartan
Eprosartan
EXP-3174
Fimasartan
Forasartan
Irbesartan
Losartan
Milfasartan
Olmesartan
Olmesartan medoxomil
PD123319
Pomisartan
Pratosartan
Ripisartan
Saprisartan
Sparsentan
Tasosartan
Telmisartan
Valsartan
Zolasartan

Bradykinin

Agonists: Bradykinin
Kallidin

Antagonists: FR-173657
Icatibant
LF22-0542

CGRP

Agonists: Amylin
CGRP
Pramlintide

Antagonists: BI 44370 TA
BMS-927711
CGRP (8-37)
MK-3207
Olcegepant
Rimegepant
SB-268262
Telcagepant
Ubrogepant

Cholecystokinin

CCK_A	Agonists: Cholecystokinin CCK-4 Antagonists: Amiglumide Asperlicin Devazepide Dexloxiglumide Lintitript Lorglumide Loxiglumide Pranazepide Proglumide Tarazepide Tomoglumide

CCK_B	Agonists: Cholecystokinin CCK-4 Gastrin Antagonists: CI-988 (PD-134,308) Itriglumide L-365,360 Netazepide Proglumide Spiroglumide

Unsorted	Antagonists: Nastorazepide

CRH

CRF₁	Agonists: Cortagine Corticorelin Corticotropin releasing hormone Sauvagine Stressin I Urocortin Antagonists: Antalarmin Astressin-B CP-154,526 Emicerfont Hypericin LWH-234 NBI-27914 Pexacerfont R-121,919 TS-041 Verucerfont

CRF₂	Agonists: Corticorelin Corticotropin releasing hormone Sauvagine Urocortin Antagonists: Astressin-B

Endothelin

Agonists: Endothelin 1
Endothelin 2
Endothelin 3
IRL-1620

Antagonists: A-192,621
ACT-132577
Ambrisentan
Atrasentan
Avosentan
Bosentan
BQ-123
BQ-788
Clazosentan
Darusentan
Edonentan
Enrasentan
Fandosentan
Feloprentan
Macitentan
Nebentan
Sitaxentan
Sparsentan
Tezosentan
Zibotentan

Galanin

GAL₁	Agonists: Galanin Galanin (1-15) Galanin-like peptide Galmic Galnon Antagonists: C7 Dithiepine-1,1,4,4-tetroxide Galantide (M15) M32 M35 M40 SCH-202596

GAL₂	Agonists: Galanin Galanin (1-15) Galanin (2-11) Galanin-like peptide Galmic Galnon J18 Antagonists: C7 Galantide (M15) M32 M35 M40 M871

GAL₃	Agonists: Galanin Galanin (1-15) Galmic Galnon Antagonists: C7 Galantide (M15) GalR3ant HT-2157 M32 M35 M40 SNAP-37889 SNAP-398299

Ghrelin/GHS

Agonists: Peptide: Alexamorelin
Cortistatin-14
Examorelin (hexarelin)
Ghrelin (lenomorelin)
GHRP-1
GHRP-3
GHRP-4
GHRP-5
GHRP-6
Ipamorelin
Pralmorelin (GHRP-2)
Relamorelin
Tabimorelin
Ulimorelin; Non-peptide: Adenosine
Anamorelin
Capromorelin
CP-464709
Ibutamoren (MK-677)
L-692,585
Macimorelin
SM-130,686; Unsorted: LY-426410
LY-444711

Antagonists: A-778,193
Cortistatin-8
(D-Lys^3)-GHRP-6
JMV2959
YIL-781

Agonists: Bovine somatotropin
Efpegsomatropin
Human placental lactogen
MOD-4023
Somapacitan
Somatotropin (growth hormone)
Somatrem
Somavaratan

Antagonists: G120K-hGH
Pegvisomant

GHRH

Agonists: Peptide: CJC-1295
Dumorelin
GHRH (somatorelin)
Modified GRF (1-29)
Rismorelin
Sermorelin
Tesamorelin

Antagonists: MZ-5-156

GLP

GLP-1	Agonists: Albiglutide Dulaglutide Efpeglenatide Exenatide GLP-1 Langlenatide Liraglutide Lixisenatide Oxyntomodulin Semaglutide Taspoglutide

GLP-2	Agonists: Elsiglutide GLP-2 Teduglutide

Glucagon

Agonists: Glucagon

Antagonists: L-168,049
LGD-6972

GnRH

Antagonists: Peptide: Abarelix
Acyline
Cetrorelix
Degarelix
Detirelix
Ganirelix
Iturelix
Ozarelix
Prazarelix
Ramorelix
Teverelix (antarelix); Non-peptide: ASP-1707
Elagolix
KLH-2109
Relugolix
Sufugolix

Gonadotropin

LH/CG	Agonists: Human chorionic gonadotropin Luteinizing hormone

FSH	Agonists: Follicle-stimulating hormone

Insulin

Antagonists: BMS-754807
S661
S961

Interleukin

IL-1	Agonists: Interleukin-1 α β Antagonists: IL-1RA (anakinra) Antibodies: Canakinumab

IL-6	Agonists: Interleukin-6 Antibodies: Clazakizumab Elsilimomab Olokizumab Sarilumab Siltuximab Sirukumab Tocilizumab

Kisspeptin

Agonists: Kisspeptin
Kisspeptin-10

Antagonists: Kisspeptin-234

Leptin

Agonists: Leptin

MCH

MCH₁	Agonists: Melanin concentrating hormone Antagonists: ATC-0065 ATC-0175 GW-803,430 NGD-4715 SNAP-7941 SNAP-94847

MCH₂	Agonists: Melanin concentrating hormone

Melanocortin

MC₁	Agonists: α-MSH β-MSH γ-MSH ACTH (corticotropin) Afamelanotide BMS-470,539 Bremelanotide HS-014 HS-024 Melanotan II Modimelanotide PL-8177 SHU-8914 SHU-9005 SHU-9119 SNAP-7941 Antagonists: ASIP

MC₂	Agonists: ACTH (corticotropin) Alsactide Codactide Giractide Norleusactide (pentacosactride) Seractide Tetracosactide (tetracosactrin, cosyntropin) Tosactide (octacosactrin) Tricosactide Tridecactide

MC₃	Agonists: α-MSH β-MSH γ-MSH ACTH (corticotropin) Afamelanotide Bremelanotide Melanotan II Modimelanotide PG-931 Antagonists: AGRP ASIP HS-014 ML-00253764 PG-106 SHU-8914 SHU-9005 SHU-9119

MC₄	Agonists: α-MSH β-MSH γ-MSH ACTH (corticotropin) Afamelanotide AZD2820 BIM-22493 Bremelanotide LY-2112688 Melanotan II MK-0493 Modimelanotide PF-00446687 PG-931 PL-6983 Ro 27-3225 Setmelanotide THIQ Antagonists: AGRP ASIP HS-014 HS-024 HS-131 JKC-363 MCL-0020 MCL-0042 MCL-0129 ML-00253764 MPB-10 SHU-8914 SHU-9005 SHU-9119 Unknown: Semax

MC₅	Agonists: α-MSH β-MSH γ-MSH ACTH (corticotropin) Afamelanotide Bremelanotide HS-014 HS-024 Melanotan II Modimelanotide SHU-8914 SHU-9005 SHU-9119 Antagonists: ASIP ML-00253764 Unknown: Semax

Unsorted	Agonists: Alsactide Codactide Giractide Norleusactide (pentacosactride) Seractide Tetracosactide (tetracosactrin, cosyntropin) Tosactide (octacosactrin) Tricosactide Tridecactide

Neuropeptide FF

Agonists: Neuropeptide AF
Neuropeptide FF
Neuropeptide SF (RFRP-1)
Neuropeptide VF (RFRP-3)

Antagonists: BIBP-3226
RF9

Neuropeptide S

Agonists: Neuropeptide S

Antagonists: ML-154
SHA-68

Neuropeptide Y

Y₁	Agonists: Neuropeptide Y Peptide YY Antagonists: BIBO-3304 BIBP-3226 BVD-10 GR-231,118 PD-160,170

Y₂	Agonists: 2-Thiouridine 5'-triphosphate Neuropeptide Y Neuropeptide Y (13-36) Peptide YY Peptide YY (3-36) Antagonists: BIIE-0246 JNJ-5207787 SF-11

Y₄	Agonists: GR-231,118 Neuropeptide Y Pancreatic polypeptide Peptide YY Antagonists: UR-AK49

Y₅	Agonists: BWX-46 Neuropeptide Y Peptide YY Antagonists: CGP-71683 FMS-586 L-152,804 Lu AA-33810 MK-0557 NTNCB Velneperit (S-2367)

Neurotensin

NTS₁	Agonists: Neurotensin Neuromedin N Antagonists: Meclinertant SR-142,948

NTS₂	Agonists: Neurotensin Antagonists: Levocabastine SR-142,948

Neurotrophin

See here instead.

Opioid

See here instead.

Orexin

OX₁	Agonists: Orexin-A Orexin-B Antagonists: ACT-335827 ACT-462206 Almorexant Filorexant Lemborexant SB-334,867 SB-408,124 SB-649,868 Suvorexant TCS-1102

OX₂	Agonists: Orexin-A Orexin-B SB-668,875 Antagonists: ACT-335827 ACT-462206 Almorexant EMPA Filorexant JNJ-10397049 MIN-202 (JNJ-42847922) Lemborexant MK-1064 SB-649,868 Suvorexant TCS-1102 TCS-OX2-29

Oxytocin

Agonists: Peptide: Aspartocin
Carbetocin
Cargutocin
Demoxytocin
Lipo-oxytocin-1
Merotocin
Nacartocin
Oxytocin
TGOT
Vasotocin (argiprestocin); Non-peptide: TC OT 39
WAY-267,464

Antagonists: Peptide: Atosiban
Tocinoic acid; Non-peptide: Barusiban
Epelsiban
Erlosiban
IX-01
L-368,899
L-371,257
L-372,662
Retosiban
SSR-126,768
WAY-162,720

Prolactin

Antagonists: Δ1–9-G129R-hPRL
Δ1–14-G129R-hPRL
G120K-hGH
G129R-hPRL

PTH

Agonists: Abaloparatide
PTH
PTHrP
Semparatide
Teriparatide

Somatomedin

IGF-1	Agonists: des(1-3)IGF-1 IGF-1 (somatomedin C) (mecasermin, mecasermin rinfabate) IGF-1 LR3 IGF-2 (somatomedin A) Insulin Antagonists: BMS-754807 Antibodies: AVE1642 Cixutumumab Dalotuzumab Figitumumab Ganitumab NVP-ADW742 NVP-AEW541 Robatumumab OSl-906 R1507

IGF-2	Agonists: IGF-2 (somatomedin A)

Somatostatin

Agonists: BIM-23052
CH-275
Cortistatin-14
Depreotide
Ilatreotide
L-803,087
L-817,818
Lanreotide
NNC 26-9100
Octreotide
Pasireotide
Pentetreotide
RC-160
Seglitide
Somatostatin (GHIH)
Somatostatin (1-28)
SRIF-14
SRIF-28
TT-232
Vapreotide

Antagonists: BIM-23056
Cyclosomatostatin
CYN-154806

Tachykinin

NK₁	Agonists: Substance P Antagonists: Aprepitant Befetupitant Burapitant Casopitant CI-1021 CP-96,345 CP-99,994 CP-122,721 Dapitant Ezlopitant Figopitant FK-888 Fosaprepitant Fosnetupitant GR-203,040 GW-597,599 HSP-117 L-733,060 L-741,671 L-743,310 L-758,298 Lanepitant LY-306,740 Maropitant Netupitant NKP-608 Nolpitantium besilate Orvepitant Rolapitant RP-67,580 SDZ NKT 343 Serlopitant Telmapitant Tradipitant Vestipitant Vofopitant

NK₂	Agonists: Neurokinin A Antagonists: GR-159,897 Ibodutant Nepadutant Saredutant

NK₃	Agonists: Neurokinin B Antagonists: Osanetant Talnetant

TRH

Agonists: Azetirelin
Fertirelin
Montirelin
Orotirelin
Posatirelin
Protirelin
Rovatirelin
Taltirelin
TRH/TRF

TSH

Agonists: TSH (thyrotropin)

Vasopressin

V_1A	Agonists: Felypressin Lypressin Ornipressin Selepressin Terlipressin Vasopressin (argipressin) Vasotocin (argiprestocin) Antagonists: Atosiban Conivaptan FR-218944 JNJ-17079166 JNJ-17308616 LY-307174 PF-184563 Relcovaptan RG7314 SRX246 SRX251 TC OT 39 WAY-267,464 YM-218 YM-471 YM-35471

V_1B	Agonists: Desmopressin Felypressin Lypressin Ornipressin Terlipressin Vasopressin (argipressin) Vasotocin (argiprestocin) Antagonists: ABT-436 Nelivaptan ORG-52186

V₂	Agonists: Desmopressin Felypressin Lypressin Ornipressin TC OT 39 Terlipressin Vasopressin (argipressin) Vasotocin (argiprestocin) Antagonists: Conivaptan JNJ-17079166 Lixivaptan Mozavaptan RWJ-351647 Satavaptan Tolvaptan YM-471 YM-35471

Unsorted	Antagonists: Ribuvaptan RWJ-339489 VMAX-367 VMAX-372 VMAX-382 YM-222546

VIP

VIPR₁	Agonists: Peptide: LBT-3393 VIP

VIPR₂	Agonists: Peptide: LBT-3627 VIP

Unsorted

Isunakinra
Trofinetide

This article incorporates text from the public domain Pfam and InterPro IPR015276

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