Hypocretin (orexin) receptor 2

Available structures

Ortholog search: PDBe, RCSB

List of PDB id codes
4S0V

Identifiers

Symbols

HCRTR2 ; OX2R

External IDs

OMIM: 602393 MGI: 2680765 HomoloGene: 1168 IUPHAR: 322 ChEMBL: 4792 GeneCards: HCRTR2 Gene

Gene ontology
Molecular function	• neuropeptide receptor activity • orexin receptor activity • peptide hormone binding • peptide binding
Cellular component	• plasma membrane • integral component of plasma membrane
Biological process	• phospholipase C-activating G-protein coupled receptor signaling pathway • neuropeptide signaling pathway • synaptic transmission • feeding behavior • circadian sleep/wake cycle process • cellular response to hormone stimulus • regulation of circadian sleep/wake cycle, sleep • response to peptide
Sources: Amigo / QuickGO

RNA expression pattern

More reference expression data

Orthologs

Species

Human

Mouse

RefSeq (mRNA)

RefSeq (protein)

Location (UCSC)

Chr 6:
55.11 – 55.28 Mb

Chr 9:
76.23 – 76.32 Mb

PubMed search

Orexin receptor type 2

Identifiers

Symbol

Orexin_rec2

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

Orexin receptor type 2 (Ox2R or OX₂), also known as hypocretin receptor type 2, is a protein that in humans is encoded by the HCRTR2 gene.^[1]

Function

OX₂ is a G-protein coupled receptor expressed exclusively in the brain. It has 64% identity with OX₁. OX₂ binds both orexin A and orexin B neuropeptides. OX₂ is involved in the central feedback mechanism that regulates feeding behaviour.^[1]

Ligands

Agonists

Orexin-A
Orexin-B
SB-668,875

Antagonists

Almorexant - Dual OX₁ and OX₂ antagonist
EMPA - Selective OX₂ antagonist
Filorexant - Dual OX₁ and OX₂ antagonist
JNJ-10397049 (600x selective for OX₂ over OX₁)^[2]
Lemborexant - Dual OX₁ and OX₂ antagonist
MIN-202 - Selective OX₂ antagonist
MK-1064 - Selective OX₂ antagonist^[3]
MK-8133 - Selective OX₂ antagonist^[4]
SB-649,868 - Dual OX₁ and OX₂ antagonist
Suvorexant - Dual OX₁ and OX₂ antagonist
TCS-OX2-29 - Selective OX₂ antagonist
(3,4-dimethoxyphenoxy)alkylamino acetamides^[5]
Compound 1m - Selective OX₂ antagonist ^[6]

References

1 2 "Entrez Gene: HCRTR2 hypocretin (orexin) receptor 2".
↑ McAtee LC, Sutton SW, Rudolph DA, Li X, Aluisio LE, Phuong VK, Dvorak CA, Lovenberg TW, Carruthers NI, Jones TK (Aug 2004). "Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists". Bioorganic & Medicinal Chemistry Letters 14 (16): 4225–9. doi:10.1016/j.bmcl.2004.06.032. PMID 15261275.
↑ Roecker AJ, Mercer SP, Schreier JD, Cox CD, Fraley ME, Steen JT, Lemaire W, Bruno JG, Harrell CM, Garson SL, Gotter AL, Fox SV, Stevens J, Tannenbaum PL, Prueksaritanont T, Cabalu TD, Cui D, Stellabott J, Hartman GD, Young SD, Winrow CJ, Renger JJ, Coleman PJ (Feb 2014). "Discovery of 5-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia". ChemMedChem 9 (2): 311–22. doi:10.1002/cmdc.201300447. PMID 24376006.
↑ Kuduk SD, Skudlarek JW, DiMarco CN, Bruno JG, Pausch MH, O'Brien JA, Cabalu TD, Stevens J, Brunner J, Tannenbaum PL, Garson SL, Savitz AT, Harrell CM, Gotter AL, Winrow CJ, Renger JJ, Coleman PJ (Jun 2015). "Identification of MK-8133: An orexin-2 selective receptor antagonist with favorable development properties". Bioorganic & Medicinal Chemistry Letters 25 (12): 2488–92. doi:10.1016/j.bmcl.2015.04.066. PMID 25981685.
↑ Cole AG, Stroke IL, Qin LY, Hussain Z, Simhadri S, Brescia MR, Waksmunski FS, Strohl B, Tellew JE, Williams JP, Saunders J, Appell KC, Henderson I, Webb ML (Oct 2008). "Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists". Bioorganic & Medicinal Chemistry Letters 18 (20): 5420–3. doi:10.1016/j.bmcl.2008.09.038. PMID 18815029.
↑ Fujimoto T, Kunitomo J, Tomata Y, Nishiyama K, Nakashima M, Hirozane M, Yoshikubo S, Hirai K, Marui S (Nov 2011). "Discovery of potent, selective, orally active benzoxazepine-based Orexin-2 receptor antagonists". Bioorganic & Medicinal Chemistry Letters 21 (21): 6414–6. doi:10.1016/j.bmcl.2011.08.093. PMID 21917455.

Flier JS, Maratos-Flier E (Feb 1998). "Obesity and the hypothalamus: novel peptides for new pathways". Cell 92 (4): 437–40. doi:10.1016/S0092-8674(00)80937-X. PMID 9491885.
Willie JT, Chemelli RM, Sinton CM, Yanagisawa M (2001). "To eat or to sleep? Orexin in the regulation of feeding and wakefulness". Annual Review of Neuroscience 24: 429–58. doi:10.1146/annurev.neuro.24.1.429. PMID 11283317.
Hungs M, Mignot E (May 2001). "Hypocretin/orexin, sleep and narcolepsy". BioEssays 23 (5): 397–408. doi:10.1002/bies.1058. PMID 11340621.
de Lecea L, Kilduff TS, Peyron C, Gao X, Foye PE, Danielson PE, Fukuhara C, Battenberg EL, Gautvik VT, Bartlett FS, Frankel WN, van den Pol AN, Bloom FE, Gautvik KM, Sutcliffe JG (Jan 1998). "The hypocretins: hypothalamus-specific peptides with neuroexcitatory activity". Proceedings of the National Academy of Sciences of the United States of America 95 (1): 322–7. doi:10.1073/pnas.95.1.322. PMC 18213. PMID 9419374.
Sakurai T, Amemiya A, Ishii M, Matsuzaki I, Chemelli RM, Tanaka H, Williams SC, Richardson JA, Kozlowski GP, Wilson S, Arch JR, Buckingham RE, Haynes AC, Carr SA, Annan RS, McNulty DE, Liu WS, Terrett JA, Elshourbagy NA, Bergsma DJ, Yanagisawa M (Feb 1998). "Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior" (PDF). Cell 92 (4): 573–85. doi:10.1016/S0092-8674(00)80949-6. PMID 9491897.
Sakurai T, Amemiya A, Ishii M, Matsuzaki I, Chemelli RM, Tanaka H, Williams SC, Richarson JA, Kozlowski GP, Wilson S, Arch JR, Buckingham RE, Haynes AC, Carr SA, Annan RS, McNulty DE, Liu WS, Terrett JA, Elshourbagy NA, Bergsma DJ, Yanagisawa M (Mar 1998). "Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior". Cell 92 (5): 1 page following 696. doi:10.1016/S0092-8674(02)09256-5. PMID 9527442.
Peyron C, Faraco J, Rogers W, Ripley B, Overeem S, Charnay Y, Nevsimalova S, Aldrich M, Reynolds D, Albin R, Li R, Hungs M, Pedrazzoli M, Padigaru M, Kucherlapati M, Fan J, Maki R, Lammers GJ, Bouras C, Kucherlapati R, Nishino S, Mignot E (Sep 2000). "A mutation in a case of early onset narcolepsy and a generalized absence of hypocretin peptides in human narcoleptic brains". Nature Medicine 6 (9): 991–7. doi:10.1038/79690. PMID 10973318.
Wright GJ, Puklavec MJ, Willis AC, Hoek RM, Sedgwick JD, Brown MH, Barclay AN (Aug 2000). "Lymphoid/neuronal cell surface OX2 glycoprotein recognizes a novel receptor on macrophages implicated in the control of their function". Immunity 13 (2): 233–42. doi:10.1016/S1074-7613(00)00023-6. PMID 10981966.
Hartley JL, Temple GF, Brasch MA (Nov 2000). "DNA cloning using in vitro site-specific recombination". Genome Research 10 (11): 1788–95. doi:10.1101/gr.143000. PMC 310948. PMID 11076863.
Mazzocchi G, Malendowicz LK, Gottardo L, Aragona F, Nussdorfer GG (Feb 2001). "Orexin A stimulates cortisol secretion from human adrenocortical cells through activation of the adenylate cyclase-dependent signaling cascade". The Journal of Clinical Endocrinology and Metabolism 86 (2): 778–82. doi:10.1210/jc.86.2.778. PMID 11158046.
Blanco M, López M, García-Caballero T, Gallego R, Vázquez-Boquete A, Morel G, Señarís R, Casanueva F, Diéguez C, Beiras A (Apr 2001). "Cellular localization of orexin receptors in human pituitary". The Journal of Clinical Endocrinology and Metabolism 86 (4): 1616–9. doi:10.1210/jc.86.4.1616. PMID 11297593.
Blanco M, López M, GarcIa-Caballero T, Gallego R, Morel G, SeñarIs R, Casanueva F, Diéguez C, Beiras A (Jul 2001). "Cellular localization of orexin receptors in human pituitary". The Journal of Clinical Endocrinology and Metabolism 86 (7): 1616–9. doi:10.1210/jc.86.7.3444. PMID 11443222.
Karteris E, Randeva HS, Grammatopoulos DK, Jaffe RB, Hillhouse EW (Sep 2001). "Expression and coupling characteristics of the CRH and orexin type 2 receptors in human fetal adrenals". The Journal of Clinical Endocrinology and Metabolism 86 (9): 4512–9. doi:10.1210/jc.86.9.4512. PMID 11549701.
Randeva HS, Karteris E, Grammatopoulos D, Hillhouse EW (Oct 2001). "Expression of orexin-A and functional orexin type 2 receptors in the human adult adrenals: implications for adrenal function and energy homeostasis". The Journal of Clinical Endocrinology and Metabolism 86 (10): 4808–13. doi:10.1210/jc.86.10.4808. PMID 11600545.
Olafsdóttir BR, Rye DB, Scammell TE, Matheson JK, Stefánsson K, Gulcher JR (Nov 2001). "Polymorphisms in hypocretin/orexin pathway genes and narcolepsy". Neurology 57 (10): 1896–9. doi:10.1212/wnl.57.10.1896. PMID 11723285.
Blanco M, García-Caballero T, Fraga M, Gallego R, Cuevas J, Forteza J, Beiras A, Diéguez C (Mar 2002). "Cellular localization of orexin receptors in human adrenal gland, adrenocortical adenomas and pheochromocytomas". Regulatory Peptides 104 (1-3): 161–5. doi:10.1016/S0167-0115(01)00359-7. PMID 11830291.
Strausberg RL, Feingold EA, Grouse LH, Derge JG, Klausner RD, Collins FS, Wagner L, Shenmen CM, Schuler GD, Altschul SF, Zeeberg B, Buetow KH, Schaefer CF, Bhat NK, Hopkins RF, Jordan H, Moore T, Max SI, Wang J, Hsieh F, Diatchenko L, Marusina K, Farmer AA, Rubin GM, Hong L, Stapleton M, Soares MB, Bonaldo MF, Casavant TL, Scheetz TE, Brownstein MJ, Usdin TB, Toshiyuki S, Carninci P, Prange C, Raha SS, Loquellano NA, Peters GJ, Abramson RD, Mullahy SJ, Bosak SA, McEwan PJ, McKernan KJ, Malek JA, Gunaratne PH, Richards S, Worley KC, Hale S, Garcia AM, Gay LJ, Hulyk SW, Villalon DK, Muzny DM, Sodergren EJ, Lu X, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madan A, Young AC, Shevchenko Y, Bouffard GG, Blakesley RW, Touchman JW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Krzywinski MI, Skalska U, Smailus DE, Schnerch A, Schein JE, Jones SJ, Marra MA (Dec 2002). "Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences". Proceedings of the National Academy of Sciences of the United States of America 99 (26): 16899–903. doi:10.1073/pnas.242603899. PMC 139241. PMID 12477932.

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

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

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

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