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The first list below includes endogenous neuroactive extracellular signal transducers with known receptors. The list is composed of neurotransmitters, neuromodulators, neuropeptides, neurosteroids, and neuroactive hormones. The list does not include growth factors, cytokines, and intracellular second messengers; note that I have classified insulin as a growth factor. In all but a few cases (in which available information is lacking or misleading), the substances listed are known to or very likely to affect neurons in the human brain. For the most part, I have neglected to include non-receptor binding sites such as enzymes and voltage-gated ion channels. Ligand groups marked with an asterisk (*) have been grouped together due to the difficulty of matching each ligand with its specific receptors; the receptors listed for such groups are not necessarily affected by each of the ligands listed. Do not assume that the list is comprehensive; many endogenous ligands and receptors have not yet been identified or characterized. You are strongly encouraged to report any errors or suggestions. -- Shawn Thomas
Please note that "G5" represents a link to a PDF file from Neuropsychopharmacology: The Fifth Generation of Progress; "G4" represents a link to an HTML file from Psychopharmacology - The Fourth Generation of Progress (published by the American College of Neuropsychopharmacology).
Overview of Irish Neuroscience: (Updated
1/12/06) Endogenous
Ligands Receptors
Reviews OMIM GRP:
18q21;
NMB: 15q22-qter;
GRPR: Xp22.3-p21.2;
NMBR: 6q21-qter;
BRS3: Xq26-q28 Glutamate,
quinolinate, glutathione (GSH) [see the link provided for a description of GSH's
complex activity at NMDA receptors], gamma-L-Glutamylglutamate (LGG) [also a possible
agonist at AMPA/kainate receptors], l-homocysteate, L-serine-O-sulfate, l-cysteine
sulfate, l-cysteic acid, succinate [Glycine
and NMDA] [D-serine]
[Dynorphin A(1-13)] [Kynurenate]
Gonadotropin-releasing hormone I receptors [GNRHR] (aka luteinizing hormone-releasing
hormone receptors [LHRHR])
alpha-Melanocyte-stimulating hormone (alpha-MSH), desacetyl-alpha-melanocyte-stimulating
hormone (desacetyl-alpha-MSH), beta-melanocyte-stimulating hormone (beta-MSH) [NMU1
and NMU2 receptors] [Neuromedin s is a novel anorexigenic hormone.] [Neuropeptide S promotes both arousal and anxiolytic-like effects]
[G5]
[Receptor binding affinities] [MU3]
[MU
splice variants] [Endogenous
morphine] [Kappa1a,
kappa1b receptors] [Kappa2a,
kappa2b receptors] [Delta
opioid receptor] [Delta
opioid receptor subtypes] [Epsilon
opioid receptor] [beta-casomorphin
and opioid receptors] [beta-casomorphin
and lactacting women] [VV-hemorphin-7/LVV-hemorphin-7]
[VV-hemorphin-7]
[Hemorphins
in rat tissues] [MERF,
MERGL, BAM-12P in the human brain] [Metorphamide,
peptide E, and BAM 18P in the rat brain] [Endomorphin-1
and endomorphin-2 in the mouse brain] [Dynorphin
peptides and neoendorphins in the human brain] [Synenkephalin
in the rat brain] [Cytochrophin-4]
[Cytochrophin-4
and epsilon receptors] [G4]
*ATP, UTP, ADP, UDP, ATPgammaS, UTPgammaS, 2Cl-ADP, 2MeSATP, 2MeSADP, ADPbetaS,
ADPbetaF, alphabeta-meATP, betagamma-meATP, BzATP, Ap3A, Ap4A, Ap5A, Ap6A, etc. [P2X/P2Y]
[Molecular
Physiology of P2X Receptors] [P2X]
[P2Y12] [P2Y13]
[G5] [G4]
[P2D]
[P3];
[P4,
Diadenosine polyphosphate receptors] Pancreastatin
precursor gene: 14q32 PTH:
11p15.3-p15.1;
PTH1: 3p22-p21.1;
PTH2: 2q33 Thrombin:
11p11-q12;
granzyme A: 5q11-q12;
cathepsin G: 14q11.2 Somatostatin:
3q28;
cortistatin: 1p36;
SST1: 14q13;
SST2: 17q24;
SST3: 22q13.1;
SST4: 20p11.2;
SST5: 16p13.3 S1P1:
???; S1P2:
???; S1P3:
9q22.1-q22.2;
S1P4: 19p13.3;
S1P5: Chr.19;
GPR3: 1p36.1-p34.3;
GPR6: 6q21-q22.1;
GPR12: 13q12;
GPR63: 6q16.1-q16.3 Neuroactive signaling molecules:
gases Endogenous
Ligands Receptors
Reviews OMIM Endogenous neuroactive extracellular
signal transducers with putative or unknown binding sites Endogenous
Ligands Receptors
Reviews OMIM Endogenous substances that may
or may not be defined as neuroactive extracellular signal transducers: Endogenous
Ligands Receptors
Reviews OMIM [Apolipoprotein
IV and rat hypothalamus] [Apolipoprotein
IV binding] [PE-11]
[GAWK/CCB]
[SR-17/HQ-34]
[Chromogranin B derived
peptides] [CgB
derived peptides]
Irish Neuroscience - Virtual Museum
Irish Pioneers - Ten Neuroscientists
Irish Citizenship - Eligibility FAQ
Irish Times - Motor Neuron Breakthrough
Acetylcholine
Acetylcholine receptors [muscarinic: M1, M2, M3, M4, M5; nicotinic] [Muscarinic]
[Nicotinic]
[G5] [G4:
Muscarinic] [G4:
Nicotinic]
M1:
11q13;
M2: 7q35-q36;
M3: 1q41-q44;
M4: 11p12-p11.2;
M5: 15q26 Catestatin
[an endogenous noncompetitive antagonist] Acetylcholine
receptors [nicotinic] [Catestatin]
Adenosine Adenosine
receptors [A1, A2A, A2B, A3] [Adenosine
receptors] [Purine
and pyrimidine receptors] [G5]
A1:
1q32.1;
A2A: 22q11.2;
A2B: 10q25.3-q26.3;
A3: 1p21-p13 Inosine
[an adenosine metabolite] Adenosine
A1, A3 receptors [Inosine]
[Adenosine
receptors] A1:
1q32.1;
A3: 1p21-p13
Epinephrine [aka adrenaline], norepinephrine [aka noradrenaline]
Adrenoceptors:
[alpha-1A, alpha-1B, alpha-1D, alpha-2A, alpha-2B, alpha-2C, beta-1, beta-2, beta-3], D4 receptors
[G5]
[G4] ["Epinephrine and norepinephrine act as potent agonists at the recombinant human dopamine D4 receptor."]
alpha-1A:
8p21;
alpha-1B: 5q33;
alpha-1D: 20p13;
alpha-2A: 10q24-q26;
alpha-2B: Chr.2;
alpha-2C: 4p16.1;
beta-1: 10q24-q26;
beta-2: 5q32-q34;
beta-3: 8p12-p11.2 Lipoxin
A4 (LXA4) ALX
receptors (aka LXA4 receptors) [Leukotriene
and lipoxin receptors] [LXA4
and sleep] ALX
receptor: Chr.19
Angiotensin II (Ang II), angiotensin III (Ang III) Angiotensin
receptors [AT1A, AT1B, AT2] [Angiotensin
II] AT1A/AT1B:
3q21-q25;
AT2: Xq22-q23 Apelin APJ
receptors [APJ] [Apelin]
[Apelin]
Apelin:
Xq25-q26.3;
APJ: 11q12
KiSS-1
AXOR12
receptors (aka GPR54 receptors) [AXOR12]
[Kisspeptins]
[Metastin
exhibits potent LH releasing activity]
Diazepam-binding
inhibitor (DBI), octadecaneuropeptide (ODN), COOH-terminal octapeptide fragment
of ODN, triakontatetraneuropeptide [all are inverse agonists at benzodiazepine
receptors; triakontatetraneuropeptide may not be active at central-type benzodiazepine
receptors] Benzodiazepine
binding sites [central and peripheral] [COOH-terminal
octapeptide, ODN] [DBI]
[Peripheral
benzodiazepine receptors] [Triakontatetraneuropeptide] Peripheral
benzodiazepine receptor: 22q13.31 Porphyrins Benzodiazepine
receptors [peripheral] [Peripheral
benzodiazepine receptors] Peripheral
benzodiazepine receptor: 22q13.31
Gastrin-releasing peptide (GRP), neuromedin B (NMB), neuromedin C (NMC)
Bombesin-like peptide receptors: gastrin-releasing peptide receptor [GRPR], neuromedin
B receptor [NMBR], bombesin-like receptor 3 [BRS3] [NMBR]
Anaphylatoxin
C3a
C3a anaphylatoxin receptors [C3aR] [Neuronal
anaphylatoxin receptors] C3a:
19p13.3-p13.2;
C3aR: ??? Anaphylatoxin
C5a C5a
anaphylatoxin receptors [C5aR] [Neuronal
anaphylatoxin receptors] C5aR:
Chr.19
*Calcitonin, alpha-CGRP, beta-CGRP, amylin [aka islet amyloid polypeptide (IAPP)],
adrenomedullin (please view the first link provided for a description of the complex
relationships between these ligands and their receptors)
Calcitonin, amylin, CGRP, and adrenomedullin receptors [CL, CTR] [Calcitonin,
amylin, CGRP, adrenomedullin] [Adrenomedullin] Calcitonin,
alpha-CGRP: 11p15.2-p15.1;
beta-CGRP: 11p15.2-p15.1;
amylin: 12p12.3-p12.1;
adrenomedullin: 11p15.4;
CL: 2q31-q32;
CTR: 7q21.3
Anandamide [aka arachidonoylethanolamide], 2-arachidonoylglycerol, 2-arachidonylglyceryl
ether [aka noladin ether], virodhamine, N-Arachidonoyldopamine (NADA)
Cannabinoid receptors [CB1, CB2] (note that CB2 receptors are not found in the
brain) [Cannabinoid
Receptors] [Virodhamine]
[NADA] [G5]
CB1:
6q14-q15;
CB2: Chr.1
Cholecystokinin (CCK)-4, CCK-5, CCK-7, CCK-7 sulfate, CCK-8, CCK-8 sulfate, CCK-12,
CCK-22, CCK-33, CCK-39, CCK-58, gastrin Cholecystokinin
receptors [CCK1 (CCK-A), CCK2 (CCK-B)] [Cholecystokinin]
[G4] CCK:
3pter-p21;
Gastrin: 17q21;
CCK1: 4p15.2-p15.1;
CCK2: 11p15.5-p15.4
Corticotropin-releasing factor (CRF) [aka corticotropin-releasing hormone (CRH)],
urocortin [aka urotensin I]
Corticotropin-releasing factor receptors [CRF1, CRF2] [CRF]
[G5] [G4]
CRF:
8q13;
Urocortin: Chr.2;
CRF1: 17q12-q22;
CRF2: 7p21-p15 Stresscopin
(SCP) [aka urocortin III], stresscopin-related peptide (SRP) [aka urocortin II
or urocortin-related peptide (URP)] CRF2
receptors [Stresscopin]
[SCP/SRP] SCP:
???; SRP:
3p21.3;
CRF2: 7p21-p15 Cysteinyl
leukotrienes: LTC4, LTD4, LTE4 Cysteinyl-leukotriene
receptors [CYSLT1, CYSLT2] [Leukotriene
Receptors] CYSLT1:
Xq13-q21;
CYSLT2: 13q14
Dopamine
Dopamine receptors [D1, D2, D3, D4, D5] [Dopamine]
[Dopamine/Neurotensin]
[G5]
D1:
5q35.1;
D2: 11q23;
D3: 3q13.3;
D4: 11p15.5;
D5: 4p16.1-p15.3
Endothelin-1 (ET-1) , ET-2, ET-3
Endothelin receptors [ETA, ETB] [Endothelin] ET-1:
6p24-p23;
ET-2: 1p34;
ET-3: 20q13.2-q13.3;
ETA: Chr.4;
ETB: 13q22 Follicle-stimulating
hormone (FSH) [aka follitropin] Follicle-stimulating
hormone receptors [FSHR] [FSH]
[Gonadotropins]
FSH:
11p13;
FSHR: 2p21-p16
GABA [aka gamma-aminobutyric acid]
GABA
receptors [GABA-A, GABA-B]
[GABA-A]
[GABA-B]
[G5]
GABAB1:
???; GABAB2:
9q22.1
Galanin, galanin-like peptide (GALP) Galanin
receptors [GALR1, GALR2, GALR3] [G4]
[Human GALP
is located on chromosome 19] Galanin:
11q13.3-q13.5;
GALR1: 18q23;
GALR2: 17q25.3;
GALR3: 22q12.2-q13.1 Gastric
inhibitory polypeptide (GIP) [aka glucose-dependent insulinotropic peptide] Gastric
inhibitory polypeptide receptors [GIPR] [Glucagon
receptor family]
[PACAP/Glucagon
superfamily]GIP:
17q21.3-q22;
GIPR: 19q13.3 gamma-Hydroxybutyrate
(GHB), 4-Hydroxy-trans-2-nonenoic acid GHB
receptors [GHB]
[4-Hydroxy-trans-2-nonenoic
acid]
Glucagon Glucagon
receptors [GCGR] [Glucagon
receptor family] [PACAP/Glucagon
superfamily] Glucagon:
2q36-q37;
GCGR: 17q25 Glucagon-like
peptide-1 (GLP-1) GLP-1
receptors [GLP1R] [Glucagon-like
peptides] [Glucagon
receptor family] [PACAP/Glucagon
superfamily] GLP1:
2q36-q37;
GLP1R: 6p21 Glucagon-like
peptide-2 (GLP-2) GLP-2
receptors [GLP2R]
[Glucagon-like
peptides] [Glucagon
receptor family] [PACAP/Glucagon
superfamily] GLP2:
2q36-q37;
GLP2R: 17p13.3 Cortisol Glucocorticoid
receptors [GR], mineralocorticoid receptors [MR] [Cortisol
(on site link)] GR:
5q31;
MR: 4q31.1
Glutamate
Glutamate
AMPA receptors [ionotropic receptors composed of subunits including GluR1, GluR2,
GluR3, GluR4]
[General]
[G5]
GluR1:
5q33;
GluR2: 4q32-q33;
GluR3: Xq25-q26;
GluR4: 11q22-q23 Glutamate
Glutamate
kainate receptors [ionotropic receptors composed of subunits including GluR5,
GluR6, GluR7, KA-1, KA-2]
[Kainate]
[G5]
GluR5:
21q22;
GluR6: 6q21;
GluR7: 1p34-p33;
KA-1: 11q22.3;
KA-2: 19q13.2 Glutamate
NMDA receptors [ionotropic receptors composed of subunits including NR1, NR2A,
NR2B, NR2C, NR2D, NR3A, NMDARA1] (eight splice variants of the NR1 subunit exist:
NR1-1a, NR1-2a, NR1-3a, NR1-4a, NR1-1b, NR1-2b, NR1-3b, NR1-4b) [NMDA]
[G5] [Quinolinate]
[Glutathione]
[gamma-L-Glutamylglutamate]
[NR1
splice variants] [l-homocysteate]
[L-serine-O-sulfate]
[Succinate]
NR1:
9q34.3;
NR2A: 16p13;
NR2B: 12p12;
NR2C: 17q25;
NR2D: 19q13.1-qter;
NR3A: ???;
NR3B: 19p13.3;
NMDARA1: 8q24.3 Spermine,
spermidine [neuromodulators at the receptors and channnels listed] Glutamate
AMPA, kainate, NMDA receptors; inward rectifying K+ channels [Spermine
and Spermidine]
Glutamate, L-aspartate, L-homocysteine sulfinic acid, L-homocysteic acid,
L-cysteine sulfinic acid, L-cysteic acid, etc. [note that the sulphur-containing
excitatory amino acids (the latter four ligands) are not equally effective agonists
at all mGluRs]
Metabotropic glutamate receptors [Group I: mGluR1, mGluR5; Group II: mGluR2, mGluR3;
Group III: mGluR4, mGluR6, mGluR7, mGluR8] [G5]
[Sulphur-containing
excitatory amino acids]
mGluR1:
6q24;
mGluR2: 3p21.2-p21.1;
mGluR3: 7q21.1-q21.2;
mGluR4: 6p21.3;
mGluR5: ???;
mGluR6: 5q35;
mGluR7: 3p26.1-p25.2;
mGluR8: 7q31.3-q32.1 N-Acetylaspartylglutamate
(NAAG) mGluR3,
NMDA receptors [N-Acetylaspartylglutamate]
[NAAG
is a very low potency agonist at NMDA receptors] [NAAG
lacks activity at NMDA receptors on cerebellar granule neurons] [NAAG
showed a 12-fold preference for mGluR3 over mGluR2 receptors expressed in CHO
cells] mGluR3:
7q21.1-q21.2
Glycine, beta-alanine, taurine
Glycine GlyR receptors [ionotropic receptors composed of subunits including alpha-1,
alpha-2, beta] [Glycine] GlyR
alpha-1 subunit: 5q32;
GlyR alpha-2 subunit: Xp22.1-p21.2;
GlyR beta subunit: 4q31.3 Glycine,
D-serine, dynorphin A(1-13), kynurenate [an endogenous antagonist at both the
GlycineB binding site and the alpha7 nicotinic acetylcholine receptor] GlycineB
binding site on NMDA receptors (located on the NR1 subunit)
Growth hormone-releasing hormone (GHRH) [aka growth hormone-releasing factor (GRF)
or somatocrinin] GHRH
receptors [GHRHR] [Glucagon
receptor family]
[PACAP/Glucagon
superfamily]
Gonadotropin-releasing hormone I (GNRH I) [aka luteinizing hormone-releasing hormone
(LHRH) or prolactin release-inhibiting factor (PIF)]
[GNRH] [G4]
GNRH
I : 8p21-p11.2;
GNRHR: 4q21.2 Gonadotropin-releasing
hormone II (GNRH II) GNRH
II receptors, GNRH I receptors [GNRHR] [GNRH
II] [GNRH II]
[GNRH
II and GNRHR] GNRH2:
20p13 Sphingosylphosphorylcholine
(SPC)
GPR12
[GPR12]
GPR12: 13q12
Neuropeptide
B (NPB), neuropeptide W (NPW) GPR7
and GPR8 receptors [Neuropeptide
B/Neuropeptide W] [GPR7/GPR8]
[NPW and
neuroendocrine regulation] GPR7:
10q11.2-q21.1;
GPR8: 20q13.3 Growth
hormone (GH) Growth
hormone receptors [GHR] [GH
and NPY neurons] [GH
as a neuronal rescue factor] GH:
17q22-q24;
GHR: 5p13-p12 Ghrelin Growth
hormone secretagogue receptor [GHSR] [Ghrelin]
[Ghrelin]
Ghrelin:
3p26-p25;
GHSR: ???
Histamine
Histamine receptors [H1, H2, H3, H4] [Histamine]
[G5] [G4]
H1:
3p21-p14;
H2: ???;
H3: ???;
H4: 18q11.2
5-Hydroxytryptamine (5-HT) [aka serotonin]
5-Hydroxytryptamine (5-HT) receptors [5-HT1A, 5-HT1B, 5-HT1D, 5-HT1E, 5-HT1F,
5-HT2A, 5-HT2B, 5-HT2C, 5-HT3A/B, 5-HT4A/B/C/D, 5-HT5A, 5-HT6, 5-HT7A/B/C/D] (letters
not separated by commas indicate splice variants) [G5]
5-HT1A:
5q11.2-q13;
5-HT1B: 6q13;
5-HT1D: 1p36.3-p34.3;
5-HT1E: 6q14-q15;
5-HT1F: 3p12;
5-HT2A: 13q14-q21;
5-HT2B: 2q36.3-q37.1;
5-HT2C: Xq24;
5-HT3A: 11q23.1-q23.2;
5-HT3B: 11q23.1;
5-HT4: 5q31-q33;
5-HT5A: 7q36.1;
5-HT6: 1p36-p35;
5-HT7: 10q21-q24 5-HT-moduline
[an endogenous antagonist] 5-HT1B
receptors [5-HT-moduline]
[NESP55 (Precursor
Peptide)] NESP55:
20q13.2 Agmatine
[also an endogenous antagonist at glutamate NMDA receptors] Imidazoline
receptors [I(1), I(2)], alpha-2D-adrenoceptors [Agmatine]
[Agmatine
and NMDA receptors] [Agmatine
and alpha-2D-adrenoceptors] I1/I2:
???
Kinins:
bradykinin (BK), kallidin [aka Lys-BK], Met-Lys-BK, des-Arg9-BK, Lys-des-Arg9-BK,
T-kinin [aka Ile-Ser-BK], etc.
Kinin receptors [B1, B2]
[B1
Receptors] [Kinin
Receptors] [Neuronal
Kinin Receptors] [Bradykinin is also an agonist at GPR100 receptors]
B1
receptor: 14q32.1-q32.2;
B2 receptor: 14q32.1-q32.2 Kyotorphin Kyotorphin
receptors [Kyotorphin]
[The
kyotorphin receptor] Leptin Leptin
receptors [LEPR] Leptin:
7q31.3;
LEPR: 1p31 Leukotriene
B4 [aka dihydroxy-leukotriene] Leukotriene
B4 receptors [BLT1, BLT2], vanilloid receptors [VR1] [Leukotriene
Receptors] [VR1] BLT1:
14q11.2-q12;
BLT2: 14q11.2-q12 Relaxin
1 LGR7
and LGR8 receptors [Relaxin
1 and LGR7, LGR8] [Relaxin
1]
Relaxin
1: 9pter-q12;
LGR7: 4q32;
LGR8: 13q13.1
Relaxin
3
GPCR135
receptors, GPCR142 (GPR100) receptors, LGR7 receptors
Relaxin
3: 19p13.3;
LGR7: 4q32
Luteinizing
hormone (LH) [aka lutropin], choriogonadotropin (CG) [aka chorionic gonadotropin] Luteinizing
hormone/choriogonadotropin receptors [LHR] [Lutropin/Choriogonadotropin]
[Gonadotropins] LH:
19q13.32;
CG: 19q13.32;
LHR: 2p21 Lysophosphatidic
acid (LPA) Lysophosphatidic
acid (LPA) receptors [LPA1, LPA2, LPA3, LPA4 (aka GPR23)] [Lysophospholipid
Receptors] [LPA
and the brain] [LPA4] LPA1:
???; LPA2:
19p12;
LPA3: ???;
LPA4: Xq13-q21.1 Angiotensin-(1-7)
Mas proto-oncogene
[Angiotensin-(1-7)
and Mas] [Mas Knockout
Mice] [G-protein-coupled receptor Mas is a physiological antagonist of the angiotensin II type 1 receptor.]
Mas:
6q25.3-q26
Melanin-concentrating
hormone (MCH) Melanin-concentrating
hormone receptors [MCH1R, MCH2R] [MCH] MCH:
12q23-q24;
MCH1R: 22q13.3;
MCH2R: 6q16.2-q21 Melanocortin
(MC) receptors [MC1, MC2, MC3, MC4, MC5] [desacetyl-alpha-MSH] MSH
peptides: 2p23.3;
MC1: 16q24.3;
MC2: 18p11.2;
MC3: 20q13.2;
MC4: 18q22;
MC5: 18p11.2
Neuropeptide EI (NEI), neuropeptide GE (NGE) Melanocortin
MC1 receptors [NEI/NGE
and MC1-R] NEI/NGE:
12q23-q24;
MC1: 16q24.3 Adrenocorticotrophin
(ACTH) Melanocortin
MC2 receptors [aka adrenocorticotropin (ACTH) receptors] ACTH:
2p23.3;
MC2: 18p11.2 HP-4
(aka corticostatin) [an endogenous competitive antagonist at ACTH receptors and
an agonist at L-type calcium channnels] Melanocortin
MC2 receptors [aka adrenocorticotropin (ACTH) receptors] [HP-4]
[Corticostatin
and ACTH] HP-4:
Chr.8;
MC2: 18p11.2
gamma-melanocyte-stimulating
hormone (gamma-MSH) Melanocortin
MC3 receptors [gamma-MSH] gamma-MSH:
2p23.3;
MC3: 20q13.2
Agouti gene-related protein (AGRP) [an endogenous inverse agonist] Melanocortin
MC3, MC4 receptors [AGRP
inverse agonism] [AGRP
also exhibits weak activity at MC2, MC5] AGRP:
16q22;
MC3: 20q13.2;
MC4: 18q22
Melatonin (MLT) [aka N-acetyl-5-methoxytryptamine]
Melatonin receptors [MT1 (aka Mel1a), MT2 (aka Mel1b)] [Melatonin]
[MT3 is the quinone
reductase 2] MT1:
4q35.1;
MT2: 11q21-q22 Motilin Motilin
receptors [MTLR1]
[Motilin
and anxiety] [Motilin]
Motilin:
6p21.3;
MTLR1: 13q14-q21 Atrial
natriuretic peptide (ANP), brain natriuretic peptide (BNP) Natriuretic
peptide receptors [NPR-A, NPR-C] (BNP is a low affinity agonist at NPR-A receptors) [Natriuretic
Peptides] [Natriuretic
peptide receptor guanylyl cyclases] [Evidence
for a novel NPR] ANP:
1p36.2;
BNP: 1p36.2;
NPR-A: 1q21-q22;
NPR-C: 5p14-p12
Type
C-natriuretic peptide (CNP) Natriuretic
peptide receptors [NPR-B, NPR-C] [Natriuretic
Peptides] [Natriuretic
peptide receptor guanylyl cyclases] CNP:
2q24-qter;
NPR-B: 9p21-p12;
NPR-C: 5p14-p12
Neuromedin
U, neuropeptide S
Neuromedin
U (NMU) receptors [NMU1, NMU2]
NMU:
???; NMU1:
???; NMU2:
???
Neuropeptide Y (NPY), peptide YY (PYY), pancreatic polypeptide (PP) Neuropeptide
Y receptors [Y1, Y2, Y4, Y5] [NPY/PP]
[G4] NPY:
7p15.1;
PYY: 17q21;
PPY: 17q12-q21;
Y1: 4q31.3-q32;
Y2: 4q31;
Y4: 10q11.2-q21.2;
Y5: 4q31-q32
Neurotensin, neuromedin N
Neurotensin
receptors [NTS1, NTS2, NTS3 (aka sortilin)]
[Dopamine/Neurotensin]
[G4] Neurotensin:
12q21;
NT1: 20q13;
NT2: ???;
NT3: 1p21.3-p13.1 Xenin
Neurotensin
NTS1 receptors, unknown binding site
[Xenin]
[Xenin
and NT-1] [Unknown
binding site] NT1:
20q13 Neuropeptide
FF (NPFF) [also an agonist at OT7T022 receptors], neuropeptide AF (NPAF), neuropeptide
SF (NPSF), NPVF-derived peptides NPFF
receptors [NPFF1, NPFF2] [NPFF-like
peptides] [NPFF1,
NPFF2] [NPFF
and OT7T022] NPFF/NPAF:
???; NPFF1:
10q21;
NPFF2: 4q13.2-q13.3
*beta-endorphin, Leu-enkephalin, Met-enkephalin, Met-enkephalin-Arg-Gly-Leu (MERGL),
Met-Enkephalin-Arg-Phe (MERF), morphine, peptide E, peptide F, endomorphin-1,
endomorphin-2, metorphamide, neo-dynorphin, dynorphin-(1-17), dynorphin A-(1-8),
dynorphin B, alpha-neoendorphin, beta-neoendorphin, BAM-12P, BAM-18P, synenkephalin,
beta-casomorphin, VV-hemorphin-7, LVV-hemorphin-7, LVV-hemorphin-6, VV-hemorphin-5,
VV-hemorphin-4, cytochrophin-4, etc.
Opioid
receptors [mu1, mu2, mu3, kappa1a, kappa1b, kappa2a, kappa2b [putative],
delta1, delta2, epsilon receptors] (mu1, mu2, and mu3 receptors are splice variants
of the mu opioid receptor gene; genetic information on kappa and delta receptor
subtypes is not yet available.)
Proenkephalin:
8q23-q24;
prodynorphin: 20pter-p12.2;
POMC: 2p23.3;
mu: 6q24-q25;
kappa: 8q11.2;
delta: 1p36.1-p34.3 Orexin
A, orexin B [aka hypocretins] Orexin
receptors [OX1R, OX2R] (note that OX1R is moderately selective for orexin A) [Orexins] Orexin
A, orexin B: 17q21;
OX1R: ???;
OX2R: ??? RFamide-related
peptide-1 (RFRP-1), RFamide-related peptide-3 (RFRP-3), neuropeptide FF (NPFF) OT7T022
receptors [OT7T022]
[RFRP-1]
[RFRP
immunoreactivity] [NPFF
and OT7T022] Nociceptin/orphanin
FQ (N/OFQ) ORL1
receptors [aka NOP1 receptors] [Orphanin
FQ/Nociceptin] N/OFQ:
8p21;
ORL1: ??? Oxyntomodulin Oxyntomodulin
receptors [putative], glucagon receptors [GCGR], GLP-1 receptors [GLP1R] [Oxyntomodulin]
[Glucagon
receptor family] GCGR:
17q25;
GLP1R: 6p21 Oxytocin
(OT) Oxytocin
receptors [OTR] [Oxytocin] Oxytocin:
20p13;
OTR: 3p26.2 P2X
receptors [ionotropic receptors composed of subunits including P2X1, P2X2, P2X3,
P2X4, P2X5, P2X6, P2X7]; P2Y receptors [P2Y1, P2Y2 (aka P2U), P2Y4, P2Y6, P2Y11,
P2Y12, P2Y13]; P2D receptors [putative]; P3 receptors; P4 receptors [putative];
P2T (found on platelets); P2Z (found on mast cells and lyphocytes) P2X1:
17p13.3;
P2X2: ???;
P2X3: 11q12;
P2X4: 12q24.32;
P2X5: ???;
P2X7: 12q24;
P2Y1: 3q25;
P2Y2: 11q13.5;
P2Y4: Xq13;
P2Y6: 11q13.5;
P2Y11: 19p13 Pituitary
adenylate cyclase activating peptide (PACAP) PAC
receptors [PAC1], VPAC receptors [VPAC1, VPAC2] [PACAP]
[VIP/PACAP]
[PACAP/Glucagon
superfamily] PACAP:
18p11;
PAC1: 7p14;
VPAC1: 3p22;
VPAC2: 7q36.3 Pancreastatin Pancreastatin
receptors [Pancreastatin]
[Pancreastatin
receptor] [Effects
of pancreastatin on the rat brain] Parathyroid
hormone (PTH) Parathyroid
hormone 1 receptors [PTH1], parathyroid hormone 2 receptors [PTH2] [PTH] Parathyroid
hormone-related protein (PTHrP) Parathyroid
hormone 1 receptors [PTH1] [PTHrP
and AVP secretion] PTHrP:
12p12.1-p11.2;
PTH1: 3p22-p21.1
Tuberoinfundibular
peptide of 39 residues (TIP39) [TIP39 is an antagonist at PTH1 receptors] Parathyroid
hormone 1 receptors [PTH1], parathyroid hormone 2 receptors [PTH2] [TIP39]
[TIP39
expression in the rat CNS] PTH1:
3p22-p21.1;
PTH2: 2q33 Prostaglandin
PGD2 PGD2
receptors (aka DP receptors) [Prostanoids]
[Prostanoid receptors] PGD2
receptor: ??? Prostaglandin
PGE2 PGE2
receptors [EP1, EP2, EP3, EP4] [Prostanoids]
[Prostanoid receptors] EP1:
19p13.1;
EP2: 14q22;
EP3: 1p31.2;
EP4: 5p13.1 Prostaglandin
PGF2-alpha PGF2-alpha
receptors (aka FP receptors) [Prostanoids]
[Prostanoid receptors] FP
receptor: 1p31.1 Prostaglandin
PGI2 [aka prostacyclin] PGI2
receptors (aka IP receptors) [Prostanoids]
[Prostanoid receptors] IP
receptor: 19q13.3 Peptide
histidine isoleucine (PHI), peptide histidine methionine (PHM), peptide histidine
valine (PHV) PHI/PHV
receptors [putative], VPAC receptors [VPAC1, VPAC2] (PHI and PHM bind only weakly
at VPAC receptors) [PACAP/Glucagon
superfamily] [PHM
in the human brain] [PHI,
PHV in the mouse brain] [PHI/PHV
receptor in the goldfish] PHI/PHM/PHV:
6q26-q27;
VPAC1: 3p22;
VPAC2: 7q36.3
Platelet-activating
factor (PAF) [PAF may also inhibit GABA-A receptor activity] Platelet-activating
factor receptors [PTAFR] [PAF
and LTP in the dentate gyrus] [PAF
and GABA-A receptors] PTAFR:
1p35-p34.3
Prokineticin 2, prokineticin 1
Prokineticin PK2 receptors
[Molecular cloning and characterization of prokineticin receptors.] [Regulation of prokineticin 2 expression by light and the circadian clock.]
PK2: 20p12.3; prokineticin 2: 3p21.1
Prolactin Prolactin
receptors [PRLR] [Prolactin]
[Prolactin]
Prolactin:
6p22.2-p21.3;
PRLR: 5p13-p12 Prolactin-releasing
peptide (PrRP) [aka prolactin-releasing hormone (PRH)] (two isoforms exist: PrRP31
and PrRP20) Prolactin-releasing
peptide (PrRP) receptors (aka UHR1/GPR10 receptors), NPFF2 receptors [PrRP
and its receptor] [PrRP
and NPFF2 receptors] [PrRP
isoforms] PrRP:
???; GPR10:
10q25.3-q26;
NPFF2: 4q13.2-q13.3
*Endogenous
proteinase-activated receptor regulators: thrombin, trypsin, tryptase, cathepsin
G, granzyme A, streptokinase-plasminogen, etc. [see the review for a larger list] Proteinase-activated
receptors [PAR1, PAR2, PAR3, PAR4]
Secretin Secretin
receptors [SR] [Glucagon
receptor family]
[PACAP/Glucagon
superfamily]Secretin:
11p15.5;
secretin receptor: 2q14.1
Somatostatin-14 (S-14), somatostatin-28 (S-28), cortistatin (CST-14) Somatostatin
receptors [SST1, SST2, SST3, SST4, SST5] [G4]
Sphingosine-1-phosphate
(S1P), dihydro-sphingosine 1-phosphate (DHS1P)
Sphingosine-1-phosphate
(S1P) receptors [S1P1, S1P2, S1P3, S1P4, S1P5], GPR3, GPR6, GPR12, GPR63
[Lysophospholipid
Receptors] [Sphingosine-1-phosphate]
[GPR3,
GPR6, GPR12] [GPR63]
*Steroids:
estradiol, aldosterone, dihydrotestosterone (DHT), testosterone, dehydroepiandrosterone
(DHEA),
dehydroepiandrosterone sulfate (DHEA-S), androstenedione, 5-pregnen-3
alpha-ol-20-one sulphate (pregnenolone sulfate); progesterone; 3a-hydroxy-4-pregnen-20-one
(3alphaHP); 5 alpha-pregnan-3 alpha-ol-20-one [aka allopregnanolone]; 3alpha,5alpha-tetrahydroprogesterone
(3alpha,5alpha THP); 5alpha-pregnane-3,20-dione (5alpha-DHP) [aka 5alphaP]; 3alpha,5alpha-tetrahydrodeoxycorticosterone
(3alpha,5alpha-THDOC); 5beta-tetrahydrodeoxycorticosterone (5beta-THDOC); 5-alpha-dihydro-11-deoxycorticosterone
(5alpha-DHDOC); etc. [Please note that this list is not comprehensive;
it will likely be updated at some point in time.]Steroid
receptors and modulatory sites [Steroid
Hormones]
*Substance P (SP), neurokinin A (NKA) [aka substance K or neuromedin L],
neurokinin B (NKB) [aka neuromedin K], neuropeptide K, neuropeptide gamma
Tachykinin receptors [NK1, NK2, NK3] [Tachykinin
Peptide Family] [G5]
[Putative
NK4 receptor] [NK4]
[NK4
reappraisal]
SP,
NKA: 7q21-q22;
NKB: 12q13-q21;
NK1: Chr.2;
NK2: 10q11-q21;
NK3: ??? Thromboxane
A2 (TxA2) Thromboxane
A2 receptors [TP] [Prostanoids]
[Prostanoid receptors] TP:
19p13.3 Triiodothyronine
(T3), Thyroxine (T4) Thyroid
hormone receptors [TRalpha isoforms, TRbeta isoforms] [Thyroid
hormones] [Two novel
TRbeta isoforms] TRalpha:
17q11.2;
TRbeta: 3p24.3
Thyrotropin-releasing hormone (TRH)
Thyrotropin-releasing hormone receptors [TRH-R1, TRH-R2]
[TRH-R1, TRH-R2]
[TRH-R2
expression in the rat CNS] TRH:
3q13.3-q21;
TRH-R1: 8q23
Thyroid-stimulating
hormone (TSH) [aka thyrotropin] Thyroid-stimulating
hormone receptors [TSHR] [TSH]
[TSHR] TSH:
1p13;
TSHR: 14q31 Trace
amines: p-tyramine, beta-phenethylamine, tryptamine, octopamine Trace
amine receptors [TAR1] [Trace
amines] [TAR1]
Urotensin II-related peptide, Urotensin
II
Urotensin
II receptor [UT] (aka GPR14)
[Urotensin
II] [Urotensin II-related peptide, the endogenous ligand for the urotensin II receptor in the rat brain.]
Urotensin
II: 1p36;
UT: 17q25.3
N-Arachidonoyldopamine
(NADA), N-Oleoyldopamine (OLDA), anandamide [aka arachidonoylethanolamide], palmitoylethanolamide
and N-acyl ethanolamines [endogenous enhancers of anandamide- mediated
VR1 activation], 12- and 15-(S)-hydroperoxyeicosatetraenoic acids, 5- and 15-(S)-hydroxyeicosatetraenoic
acids, leukotriene B4 Vanilloid
VR1 receptors (aka TRPV1 or capsaicin receptors) [Vanilloid
receptors] [NADA/OLDA]
[Anandamide]
[N-acyl
ethanolamines] [Lipoxygenase
Products] VR1:
17p13
Arginine
Vasopressin (AVP) [aka antidiuretic hormone (ADH)]
Vasopressin receptors [V1A, V1B, V2] [G4] AVP:
20p13;
V1A: 12q14-q15;
V1B: 1q32;
V2: Xq28
Vasoactive intentinal peptide (VIP)
VPAC receptors [VPAC1, VPAC2]
[VIP/PACAP]
[PACAP/Glucagon
superfamily] [G4] VIP:
6q26-q27;
VPAC1: 3p22;
VPAC2: 7q36.3
Nitric oxide (NO)
soluble guanylate cyclase (sGC), NO receptors [putative NOA, NOB receptors] [Nitric
Oxide] [sGC]
[NOA, NOB]
[G4] [NO
as a signalling molecule in the nervous system]
Carbon monoxide (CO) soluble
guanylate cyclase (sGC) [CO]
[G4]
Cocaine-
and amphetamine-regulated transcript (CART), CART- derived peptides CART
receptors [putative] [CART
regulates mu opioid and serotonin 5-HT2A receptors] [CART
and central dopamine neurons] ??? TRH-potentiating
peptide [aka Ps4 or Prepro-TRH-(160-169)] TRH-potentiating
peptide (Ps4) receptors [putative] [Ps4]
[Ps4 binding
in the rat pituitary] [Ps4]
[pro-TRH-Derived
Peptides] 3q13.3-q21 Secretoneurin Secretoneurin
receptors [putative] [Secretoneurin]
[Secretoneurin
and cerebellar granule cells] Stanniocalcin
1 (STC1) [also an inhibitor of L-type calcium channels] Stanniocalcin
1 receptors [putative] [Stanniocalcin
1 receptors] [Stanniocalcin]
[STC1
and L-type calcium channels] 8p21-p11.2 beta-Lipotropin,
gamma-lipotropin Unknown
binding sites [beta-lipotropin
may act at MC2 receptors (ACTH receptors] [beta-lipotropin
and MC2 receptors in murine adipose tissues] 2p23.3 Corticotropin-like
intermediate lobe peptide (CLIP) Unknown
binding sites [CLIP
in the rat dorsal raphe nucleus] 2p23.3 Delta
sleep-inducing peptide (DSIP) Unknown
binding sites ["DSIP
is influenced by the initiation of sleep"] Enterostatin Unknown
binding sites [Enterostatin]
[Enterostatin
receptors] Glicentin Unknown
binding sites [Glicentin] Lipoxin
B4 (LXB4) Unknown
binding sites [Leukotriene
and Lipoxin Receptors] [LXB4
and Sleep] Nocistatin Unknown
binding sites [Nocistatin]
[Nocistatin]
8p21 Prepro-TRH-(178-199)
[aka Ps5] Unknown
binding sites [pro-TRH-Derived
Peptides] 3q13.3-q21 Tyr-MIF-1,
Tyr-W-MIF-1, Tyr-K-MIF-1, MIF-1 [some of these peptides may modulate mu opioid
and/or GABA-A receptors] Unknown
binding sites [Tyr-MIF-1
family peptides] WE-14 WE-14
receptors [putative] [WE-14]
[WE-14
expression]
Medium
and long chain fatty acids: docosahexaenoic acid (DHA), palmitate, oleate, stearate,
linoleate, linolenate, etc. [See links for larger lists of ligands. Note that
not all of the fatty acids listed are likely to act as extracellular signal transducers
in the brain; DHA represents the most likely fatty acid to act extracellularly
in the brain.] GPR40
receptors [GPR40]
[GPR40]
GPR40:
19q13.1 UDP-glucose,
UDP-galactose, UDP-glucuronic acid, UDP-N-acetylglucosamine P2Y14
receptors [KIAA0001
ligands] [KIAA0001
renamed P2Y14] [UDP-glucose
as an extracellular signaling molecule] Agouti
signaling protein (ASP) [an endogenous antagonist] Melanocortin
MC1, MC4 receptors [ASP
and MC1, MC4] ASP:
20q11.2 beta-Lactotensin Neurotensin
NT2 receptors [beta-Lactotensin
and NT2 receptors] [NT2
receptors in the rat brain] [Neurotensin
exhibits antagonist activity at NT2 receptors in CHO cells]
Peroxisome
proliferators Peroxisome
proliferator activated receptors [PPARs] Proctolin Proctolin
receptors [putative] [Proctolin
in the human brain stem]
Prokineticin 2beta, prokineticin 1, prokineticin 2
Prokineticin PK1 receptors
[Molecular cloning and characterization of prokineticin receptors.] [Identification and Pharmacological Characterization of Prokineticin 2{beta} as a Selective Ligand for Prokineticin Receptor 1.]
2p13.1
Peptide
P518 SP9155
(aka AQ27 and GPR103) receptors [Peptide
P518 and SP9155] Apolipoprotein
AIV Unknown
binding sites 11q23 C-peptide Unknown
binding sites [C-peptide
binding] 11p15.5 Carnosine Unknown
binding sites, ryanodine receptors [Carnosine
and ryanodine receptors] Chromogranin
A (CgA) derived peptides: vasostatin I, vasostatin II, parastatin, chromostatin,
beta-granin, etc. Unknown
binding sites [Chromogranin
A] 14q32 Chromogranin
B (CgB) derived peptides: PE-11, WE-15, GAWK, CCB, SR-17, HQ-34, etc. Unknown
binding sites 20pter-p12 GAIPIRRH Unknown
binding sites [GAIPIRRH] 20q13.2 Miniglucagon
(glucagon 19-29) Unknown
binding sites [Miniglucagon] Prepro-TRH
derived peptides: Prepro-TRH-(53-74), Prepro-TRH-(178-185), Prepro-TRH-(186-199),
Prepro-TRH-(83-106), Prepro-TRH-(208-255) Unknown
binding sites [pro-TRH-Derived
Peptides] 3q13.3-q21 RFamide-related
peptide-2 (RFRP-2) Unknown
binding sites [RFRP-2] Stanniocalcin
2 (STC2) Unknown
binding sites [Stanniocalcin
2] ??? TRH-like
peptides: pGlu-Glu-Pro-NH(2) (EEP), pGlu-Val-Pro-NH(2) (Val(2)-TRH), Leu(2)-TRH,
Phe(2)-TRH, Tyr(2)-TRH, TRH-Gly [the immediate precursor of TRH] Unknown
binding sites [TRH-like
peptides] [TRH-like
peptides and cocaine] TRH
metabolites: Cyclo(His-Pro), TRH-OH Unknown
binding sites [Cyclo(His-Pro)]
[TRH-OH] 3q13.3-q21