Enzyme (modulators )
ChAT AChE BChE
Inhibitors: Affinine
Affinisine
Conodurine
Cymserine
Ladostigil
Profenamine (ethopropazine)
Rivastigmine
Tacrine
Many of the other AChE inhibitors listed above
Transporter (modulators )
CHT
Inhibitors: Hemicholinium-3 (hemicholine)
Triethylcholine
VAChT
Release (modulators )
Inhibitors
SNAP-25 inactivators: Botulinum toxin (A , , )
VAMP inactivators: Botulinum toxin (, , , )
Enhancers
LPHN agonists: α-Latrotoxin
See also: Receptor/signaling modulators • Muscarinic acetylcholine receptor modulators • Nicotinic acetylcholine receptor modulators
ER
Agonists
Steroidal: 2-Hydroxyestradiol
2-Hydroxyestrone
3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol
3α-Androstanediol
3α-Hydroxytibolone
3β-Hydroxytibolone
3β-Androstanediol
4-Androstenediol
4-Androstenedione
4-Fluoroestradiol
4-Hydroxyestradiol
4-Hydroxyestrone
4-Methoxyestradiol
4-Methoxyestrone
5-Androstenediol
7-Oxo-DHEA
7α-Hydroxy-DHEA
7α-Methylestradiol
7β-Hydroxyepiandrosterone
8,9-Dehydroestradiol
8,9-Dehydroestrone
8β-VE2
10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED)
11β-Chloromethylestradiol
11β-Methoxyestradiol
15α-Hydroxyestradiol
16-Ketoestradiol
16-Ketoestrone
16α-Fluoroestradiol
16α-Hydroxy-DHEA
16α-Hydroxyestrone
16α-Iodoestradiol
16α-LE2
16β-Hydroxyestrone
16β,17α-Epiestriol (16β-hydroxy-17α-estradiol)
17α-Estradiol (alfatradiol )
17α-Dihydroequilenin
17α-Dihydroequilin
17α-Epiestriol (16α-hydroxy-17α-estradiol)
17α-Ethynyl-3α-androstanediol
17α-Ethynyl-3β-androstanediol
17β-Dihydroequilenin
17β-Dihydroequilin
17β-Methyl-17α-dihydroequilenin
Abiraterone
Abiraterone acetate
Alestramustine
Almestrone
Anabolic steroids (e.g., testosterone and esters , methyltestosterone , metandienone (methandrostenolone) , nandrolone and esters , many others; via estrogenic metabolites)
Atrimustine
Bolandiol
Bolandiol dipropionate
Butolame
Clomestrone
Cloxestradiol
Conjugated estriol
Conjugated estrogens
Cyclodiol
Cyclotriol
DHEA
DHEA-S
ent -Estradiol
Epiestriol (16β-epiestriol, 16β-hydroxy-17β-estradiol)
Epimestrol
Equilenin
Equilin
ERA-63 (ORG-37663)
Esterified estrogens
Estetrol
Estradiol
Estradiol esters
Lipoidal estradiol
Polyestradiol phosphate
Estramustine
Estramustine phosphate
Estrapronicate
Estrazinol
Estriol
Estriol esters
Polyestriol phosphate
Estrofurate
Estrogenic substances
Estromustine
Estrone
Estrone esters
Estrone methyl ether
Estropipate
Etamestrol (eptamestrol)
Ethinylandrostenediol
Ethinylestradiol
Ethinylestradiol 3-benzoate
Ethinylestradiol sulfonate
Ethinylestriol
Ethylestradiol
Etynodiol
Etynodiol diacetate
Hexolame
Hippulin
Hydroxyestrone diacetate
Lynestrenol
Lynestrenol phenylpropionate
Mestranol
Methylestradiol
Moxestrol
Mytatrienediol
Nilestriol
Norethisterone
Noretynodrel
Orestrate
Pentolame
Prodiame
Prolame
Promestriene
RU-16117
Quinestradol
Quinestrol
Tibolone
Nonsteroidal: (R,R)-THC
(S,S)-THC
2,8-DHHHC
β-LGND2 (GTx-878)
Allenestrol
Allenolic acid
Benzestrol
Bifluranol
Bisdehydrodoisynolic acid
Butestrol
Carbestrol
D-15414
DCW234
Diarylpropionitrile
Dienestrol
Diethylstilbestrol
Diethylstilbestrol esters
Dimestrol (dianisylhexene)
Dimethylstilbestrol
Doisynoestrol (fenocycline)
Doisynolic acid
Efavirenz
ERB-196 (WAY-202196)
Erteberel (SERBA-1, LY-500307)
Estrobin (DBE)
Fenestrel
FERb 033
Fosfestrol (diethylstilbestrol diphosphate)
Furostilbestrol (diethylstilbestrol difuroate)
GTx-758
Hexestrol
ICI-85966 (Stilbostat)
M2613
meso -Butestrol
meso -Hexestrol
Mestilbol
Methallenestril
Methestrol
Methestrol dipropionate
Paroxypropione
Pentafluranol
Phenestrol
Prinaberel (ERB-041, WAY-202041)
Propylpyrazoletriol
Quadrosilan
SC-4289
SERBA-2
SKF-82,958
Terfluranol
Triphenylbromoethylene
Triphenylchloroethylene
Triphenyliodoethylene
Triphenylmethylethylene (triphenylpropene)
WAY-166818
WAY-200070
WAY-204688 (SIM-688)
WAY-214156
Unknown/unsorted: ERB-26
ERA-45
ERB-79
ZK-283197
Xenoestrogens: Anise -related (e.g., anethole , anol , dianethole , dianol , photoanethole )
Chalconoids (e.g., isoliquiritigenin , phloretin , phlorizin (phloridzin) , wedelolactone )
Coumestans (e.g., coumestrol , psoralidin )
Flavonoids (incl. 7,8-DHF , 8-prenylnaringenin , apigenin , baicalein , baicalin , biochanin A , calycosin , catechin , daidzein , daidzin , ECG , EGCG , epicatechin , equol , formononetin , glabrene , glabridin , genistein , genistin , glycitein , kaempferol , liquiritigenin , mirificin , myricetin , naringenin , , pinocembrin , prunetin , puerarin , quercetin , tectoridin , tectorigenin )
Lavender oil
Lignans (e.g., enterodiol , enterolactone , nyasol (cis -hinokiresinol) )
Metalloestrogens (e.g., cadmium )
Pesticides (e.g., alternariol , dieldrin , endosulfan , fenarimol , HPTE , methiocarb , methoxychlor , triclocarban , triclosan )
Phytosteroids (e.g., digitoxin (digitalis ), diosgenin , guggulsterone )
Phytosterols (e.g., β-sitosterol , campesterol , stigmasterol )
Resorcylic acid lactones (e.g., zearalanone , α-zearalenol , β-zearalenol , zearalenone , zeranol (α-zearalanol) , taleranol (teranol, β-zearalanol) )
Steroid -like (e.g., deoxymiroestrol , miroestrol )
Stilbenoids (e.g., resveratrol , rhaponticin )
Synthetic xenoestrogens (e.g., alkylphenols , bisphenols (e.g., BPA , BPF , BPS ), DDT , parabens , PBBs , PHBA , phthalates , PCBs )
Others (e.g., agnuside , )
Mixed (SERMs )
4'-Hydroxynorendoxifen
27-Hydroxycholesterol
Acefluranol
Acolbifene
Afimoxifene
Anordiol
Anordrin
Arzoxifene
Bazedoxifene
Brilanestrant
Broparestrol
Chlorotrianisene
Clomifene
Clomifenoxide
Cyclofenil
Desmethylchlorotrianisene
Droloxifene
Elacestrant
Enclomifene
Endoxifen
Etacstil (GW-5638, DPC-974)
Ethamoxytriphetol (MER-25)
Femarelle
Fispemifene
ICI-55548
Idoxifene
Lasofoxifene
Levormeloxifene
LN-1643
LN-2299
Menerba
Miproxifene
Miproxifene phosphate
Nafoxidine
Nitromifene
NNC 45-0095
Ormeloxifene
Ospemifene
Panomifene
Pipendoxifene
Raloxifene
Rimostil (P-081)
Spironolactone
Tamoxifen
TAS-108 (SR-16234)
Toremifene
Trioxifene
Zindoxifene
Zuclomifene
Antagonists
(R,R)-THC
7β-Hydroxy-DHEA
Cytestrol acetate
Epitiostanol
Fulvestrant (ICI-182780)
Glyceollins (I , , III , )
ICI-164384
Mepitiostane
Methylepitiostanol
Methylpiperidinopyrazole
MIBE
Phenytoin
PHTPP
Prochloraz
TAS-108 (SR-16234)
ZB716
Coregulator-binding modulators: ERX-11
Noncompetitive inhibitors: Trilostane
GPER
Agonists
2-Methoxyestradiol
7β-Hydroxyepiandrosterone
Afimoxifene (4-hydroxytamoxifen)
Aldosterone
Atrazine
Bisphenol A
Daidzein
DDT (p,p'-DDT , )
Diarylpropionitrile
Equol
Estradiol
Ethinylestradiol
Fulvestrant (ICI-182780)
Genistein
Hydroxytyrosol
Kepone
Niacin
Niacinamide
Nonylphenol
Oleuropein
PCBs ()
Propylpyrazoletriol
Quercetin
Raloxifene
Resveratrol
Tamoxifen
Tectoridin
Antagonists Unknown
Diethylstilbestrol
Zearalenone
See also
Receptor/signaling modulators
Estrogens and antiestrogens
Androgen receptor modulators
Progesterone receptor modulators
List of estrogens
Calcium
Potassium
Sodium
VGSCs
Blockers
Antiarrhythmics (class I): Ajmaline
Aprindine
Disopyramide
Dronedarone
Encainide
Flecainide
Lidocaine
Lorajmine
Lorcainide
Mexiletine
Moricizine
Pilsicainide
Prajmaline
Procainamide
Propafenone
Quinidine
Sparteine
Tocainide
Anticonvulsants:
Carbamazepine
Cenobamate
Chlorphenacemide
Eslicarbazepine acetate
Ethotoin
Fosphenytoin
Lacosamide
Licarbazepine
Mephenytoin
Oxcarbazepine
Oxitriptyline
Phenacemide
Pheneturide
Phenytoin
Rufinamide
Topiramate
Sodium valproate
Valnoctamide
Valproate pivoxil
Valproate semisodium
Valproic acid
Valpromide
Zonisamide
Analgesics:
DSP-2230
Funapide
PF-05089771
Ralfinamide
Raxatrigine
Toxins: Conotoxins
Neosaxitoxin
Saxitoxin
Tetrodotoxin
Zetekitoxin AB
Others: Buprenorphine
Evenamide
Menthol (mint )
Safinamide
Tricyclic antidepressants
Activators
ENaC
Blockers
Amiloride
Benzamil
Triamterene
Activators
ASICs
Blockers
Amiloride
Aspirin
Ibuprofen
Chloride
CaCCs
Blockers
Crofelemer
DIDS
Ethacrynic acid
Flufenamic acid
Fluoxetine
Furosemide
Glibenclamide
Mefloquine
Mibefradil
Niflumic acid
Activators
CFTR
Unsorted
Blockers
Bumetanide
Flufenamic acid
Meclofenamic acid
Mefenamic acid
Mepacrine
Niflumic acid
Tolfenamic acid
Trifluoperazine
Others
See also: Receptor/signaling modulators • Transient receptor potential channel modulators
AMPAR
Antagonists:
Becampanel
Caroverine
CNQX
Dasolampanel
DNQX
Fanapanel (MPQX)
Kaitocephalin
Kynurenic acid
Kynurenine
Licostinel (ACEA-1021)
NBQX
Selurampanel
Tezampanel
Theanine
Topiramate
Zonampanel ; Negative allosteric modulators: Barbiturates (e.g., pentobarbital , sodium thiopental )
Cyclopropane
Enflurane
Ethanol (alcohol)
Evans blue
GYKI-52466
Halothane
Irampanel
Isoflurane
Perampanel
Pregnenolone sulfate
Sevoflurane
Talampanel ; Unknown/unsorted antagonists: Minocycline
KAR
Agonists: Main site agonists:
5-Iodowillardiine
AMPA
Domoic acid
Glutamate
Ibotenic acid
Kainic acid
Proline
Quisqualic acid
; Positive allosteric modulators: Cyclothiazide
Diazoxide
Enflurane
Halothane
Isoflurane
Antagonists:
CNQX
Dasolampanel
DNQX
Kaitocephalin
Kynurenic acid
Licostinel (ACEA-1021)
NBQX
NS102
Selurampanel
Tezampanel
Theanine
Topiramate
UBP-302 ; Negative allosteric modulators: Barbiturates (e.g., pentobarbital , sodium thiopental )
Enflurane
Ethanol (alcohol)
Evans blue
Pregnenolone sulfate
NMDAR
See also: Receptor/signaling modulators
Metabotropic glutamate receptor modulators
Glutamate metabolism/transport modulators
MOR DOR KOR NOP
Agonists:
Buprenorphine
Cebranopadol
Dihydroetorphine
Etorphine
Levomethorphan
Levorphanol
MCOPPB
NNC 63-0532
Nociceptin (orphanin FQ)
Norbuprenorphine
Racemethorphan
Racemorphan
Ro64-6198
SR-16435
Unsorted
β-Casomorphins
Amidorphin
Cytochrophin-4
Gliadorphin (gluteomorphin)
Gluten exorphins
Hemorphins
Kava constituents
NEM
Neoendorphins
Nepetalactone (catnip )
Rubiscolins
Others
Enkephalinase inhibitors : Amastatin
Candoxatril
D -Phenylalanine
Ecadotril (sinorphan)
Kelatorphan
Racecadotril (acetorphan)
RB-101
RB-120
RB-3007
Selank
Semax
Spinorphin
Thiorphan
Tynorphin
Ubenimex (bestatin)
Propeptides: β-Lipotropin (proendorphin)
Prodynorphin
Proenkephalin
Proopiomelanocortin (POMC)
Others: Kyotorphin (met-enkephalin releaser/degradation stabilizer)