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GPCR Compounds

Inhibitors and modulators to a wide range of GPCR targets.

Finding Your Compound: browse through the target categories below or use the Search Box above. Still can't find what you're looking for - contact us directly at sales@mayflowerbio.com and we'll work to source it for you through our extensive supplier network.

GPCR Categories

5-Hydroxytryptamine Receptors

Acetylcholine Receptors

Adenosine Receptors

Adrenoceptors

Angiotensin Receptors

Apelin Receptor

Bombesin Receptors

Bradykinin Receptors

Calcitonin Receptors

Cannabinoid Receptors

Cholecystokinin Receptors

Corticotropin-releasing Factor Receptors

Dopamine Receptors

Endothelin Receptors

Formylpeptide Receptors

Free Fatty Acid Receptors

Frizzled Class GPCRs

Ghrelin Receptor

Glucagon Receptors

Histamine Receptors

Hydroxycarboxylic Acid Receptors

Leukotriene Receptors

Melanin-concentrating Hormone Receptors

Melanocortin Receptors

Metabotropic Glutamate Receptors

Motilin Receptor

Neuropeptide Receptors

Opioid Receptors

Orexin Receptors

Orphan Receptors

P2Y Receptors

Parathyroid Hormone Receptors

Prolactin-releasing peptide Receptor

Prostanoid Receptors

Proteinase-activated Receptors

Somatostatin Receptors

Tachykinin Receptors

Thyrotropin-releasing Hormone Receptors

Trace Amine Receptor

Urotensin Receptor

Vasopressin and Oxytocin Receptors

VIP and PACAP Receptors

 


5-Hydroxytryptamine Receptors

(+)-Ketanserin Tartrate (5-HT2A and TRPV1 antagonist, potential α1-adrenergic antagonist)

Acepromazine Maleate (D1/2 and 5-HT1A/2A antagonist)

Agomelatine (MT1/2 agonist, 5-HT2C antagonist)

Amisulpride (5-HT7 and D2/3 antagonist)

Amitriptyline Hydrochloride (FIASMA, σ1, RyR2, TrkA/B agonist, 5-HT2/6/7, M1-5 mAChR, histamine H1/4, α1-adr. antagonist, SERT, NET inhibitor, Kv1.1/7.2/7.3 K+, L-type Ca2+ channel blocker)

Amoxapine (5-HT2/3/6/7, D2/3/4, histamine H1, α1-adrenergic antagonist, SERT and NET inhibitor, hERG K+ channel blocker)

Aniracetam (AMPA positive allosteric modulator, D2, 5-HT2A, nAChR agonist)

Aripiprazole (D2 and 5-HT1A partial agonist, 5-HT2C/6/7 antagonist, SERT inhibitor)

Buspirone Hydrochloride (α1-adrenergic and 5-HT1A partial agonist, D2/3/4 antagonist)

Chlorpromazine Hydrochloride (FIASMA; D1/2/3/4, 5-HT1/2, M1/2 mAChR, α1/2-adrenergic antagonist)

Clomipramine Hydrochloride (FIASMA, mAChR, 5-HT2/3/6/7, α1/2-adrenergic antagonist, SERT and NET inhibitor, hERG K+ and L-type Ca2+ channel blocker)

Clozapine (M4 mAChR agonist, 5-HT1A partial agonist, M1/2/3/5 mAChR, D2 antagonist, Kv1.1 K+ channel blocker)

Dimebon Dihydrochloride (AMPK activator, L-type Ca2+ channel and NMDA, histamine H1/2, α-adrenergic, 5-HT2C/5A/6 receptor antagonist)

Doxepin Hydrochloride (FIASMA, 5-HT1/2, M1-5 mAChR, α1-adrenergic, histamine H1/2 antagonist, SERT, NET, H+/K+ ATPase inhibitor)

Flibanserin (5-HT1A agonist, 5-HT2A antagonist)

Fluoxetine Hydrochloride (FIASMA, SERT inhibitor, 5-HT and σ1 antagonist)

Haloperidol (σ2 agonist, α1-adrenergic, D2, 5-HT2A, σ1 antagonist)

Hydroxyzine Dihydrochloride (FIASMA, histamine H1 inverse agonist, 5-HT2A, D1/2, α1-adrenergic antagonist)

Iloperidone (D2 and 5-HT2A antagonist, potential hERG K+ channel blocker)

Ketanserin (5-HT2A antagonist, potential α1-adrenergic antagonist)

Maprotiline Hydrochloride (FIASMA, histamine H1, 5-HT2, mAChR, α1-adrenergic antagonist, L-type Ca2+ channel blocker, NET inhibitor)

Mirtazapine (5-HT1 agonist, 5-HT2/3 and α2-adrenergic antagonist, histamine H1 inverse agonist)

Nefazodone Hydrochloride (5-HT2 antagonist, SERT and NET inhibitor, hERG K+ channel blocker)

Olanzapine (AMPK activator, D1-4, 5-HT1A/2/3/6/7, M1-5 mAChR, α1/2-adrenergic antagonist)

Paliperidone (D2 and 5-HT2A antagonist)

Pizotyline Malate (5-HT1A partial agonist, 5-HT2C antagonist)

Puerarin (GABA-A potentiator, 5-HT2C antagonist)

Quetiapine Fumarate (5-HT1A and σ1/2 agonist, 5-HT2A/2C/6/7, D1-4, histamine H1/2, M1 mAChR, α1A/1B/2C-adrenergic antagonist)

Risperidone (5-HT7 and NMDA agonist, D-amino acid oxidase inhibitor, 5-HT2A and D2 antagonist)

Sumatriptan Succinate (5-HT1B/1D agonist, TRPV1 antagonist)

Synephrine (adrenergic, TAAR-1, 5-HT agonist)

Tetrahydroberberine (5-HT1A agonist, D2 antagonist, ATP-sensitive K+ channel blocker)

Thioridazine Hydrochloride (FIASMA, D1-5, histamine H1/2, M1-5 mAChR, 5-HT1/2/5/6/7, α1/2-adrenergic antagonist, NET inhibitor, hERG K+ channel inhibitor)

Trazodone Hydrochloride (5-HT1A partial agonist, 5-HT2, histamine, α1/2-adrenergic antagonist, SERT inhibitor, voltage-gated K+ channel blocker)

Urapidil (5-HT1A agonist, α1-adrenergic antagonist)

Urapidil Hydrochloride (5-HT1A agonist, α1-adrenergic antagonist)

Vilazodone (5-HT1A partial agonist, SERT inhibitor)

Vortioxetine (5-HT1A agonist, 5-HT1B partial agonist, 5-HT3A/7 antagonist, SERT inhibitor, potential β1-adrenergic agonist)

Zolmitriptan (5-HT1B/1D agonist)

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Acetylcholine Receptors

13-Desmethyl Spirolide C (nAChR and mAChR antagonist)

Amitriptyline Hydrochloride (FIASMA, σ1, RyR2, TrkA/B agonist, 5-HT2/6/7, M1-5 mAChR, histamine H1/4, α1-adr. antagonist, SERT, NET inhibitor, Kv1.1/7.2/7.3 K+, L-type Ca2+ channel blocker)

Anisodamine (α1-adrenergic and mAChR antagonist)

Atropine (mAChR antagonist)

Atropine Sulfate Monohydrate (mAChR antagonist)

Brompheniramine Maleate (histamine H1 and mAChR antagonist, potential SERT and MAO-B inhibitor)

Chlorpromazine Hydrochloride (FIASMA; D1/2/3/4, 5-HT1/2, M1/2 mAChR, α1/2-adrenergic antagonist)

Cisatracurium Besylate (nAChR and M2 mAChR antagonist)

Clomipramine Hydrochloride (FIASMA, mAChR, 5-HT2/3/6/7, α1/2-adrenergic antagonist, SERT and NET inhibitor, hERG K+ and L-type Ca2+ channel blocker)

Clozapine (M4 mAChR agonist, 5-HT1A partial agonist, M1/2/3/5 mAChR, D2 antagonist, Kv1.1 K+ channel blocker)

Darifenacin Hydrobromide (M3 mAChR antagonist)

Diphenhydramine Hydrochloride (Voltage-gated Na+ channel blocker, mAChR antagonist, histamine H1 inverse agonist)

Doxepin Hydrochloride (FIASMA, 5-HT1/2, M1-5 mAChR, α1-adrenergic, histamine H1/2 antagonist, SERT, NET, H+/K+ ATPase inhibitor)

Galantamine Hydrobromide (AChE inhibitor, α7 nAChR agonist, mAChR agonist)

Maprotiline Hydrochloride (FIASMA, histamine H1, 5-HT2, mAChR, α1-adrenergic antagonist, L-type Ca2+ channel blocker, NET inhibitor)

Olanzapine (AMPK activator, D1-4, 5-HT1A/2/3/6/7, M1-5 mAChR, α1/2-adrenergic antagonist)

Oxybutynin Hydrochloride (mAChR antagonist)

Paroxetine Hydrochloride Hemihydrate (FIASMA, SERT and NET inhibitor, mAChR antagonist)

Peiminine (M2 mAChR antagonist, potential TRPV1 and TRPA1 antagonist)

Quetiapine Fumarate (5-HT1A and σ1/2 agonist, 5-HT2A/2C/6/7, D1-4, histamine H1/2, M1 mAChR, α1A/1B/2C-adrenergic antagonist)

Rocuronium Bromide (nAChR and M2/3 mAChR antagonist)

Scopolamine Hydrobromide Trihydrate (M1 mAChR antagonist)

Scopolamine N-butylbromide (M1 mAChR antagonist)

Thioridazine Hydrochloride (FIASMA, D1-5, histamine H1/2, M1-5 mAChR, 5-HT1/2/5/6/7, α1/2-adrenergic antagonist, NET inhibitor, hERG K+ channel inhibitor)

Tropicamide (mAChR antaonist)

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Adenosine Receptors

Aminophylline Anhydrous (Adenosine antagonist, PDE inhibitor)

Aminophylline Dihydrate (adenosine antagonist, PDE inhibitor)

Caffeine (adenosine agonist, PDE inhibitor)

Chloroadenosine (DNA chain terminator, adenosine agonist)

Clofarabine (DNA chain terminator, ribonucleotide reductase and DNA polymerase inhibitor, A1/2/3 adenosine modulator)

Fludarabine (DNA chain terminator, ribonucleotide reductase, DNA ligase, DNA primase inhibitor, A1 adenosine antagonist)

Fludarabine Phosphate (DNA chain terminator, ribonucleotide reductase, DNA ligase, DNA primase inhibitor, A1 adenosine antagonist)

Gabapentin (GABA potentiator, adenosine A1 agonist, voltage-gated α2δ Ca2+ channel blocker, NMDA modulator)

Istradefylline (Adenosine A2A antagonist)

Pentoxifylline (adenosine A2 antagonist, PDE inhibitor)

Regadenoson (Adenosine A2A agonist)

Theophylline (PDE inhibitor, A1/2 adenosine antagonist)

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Adrenoceptors

(−)-Epinephrine (α/β-adrenergic agonist)

(+)-Ketanserin Tartrate (5-HT2A and TRPV1 antagonist, potential α1-adrenergic antagonist)

Alfuzosin Hydrochloride (α1-adrenergic antagonist)

Amiodarone Hydrochloride (Voltage-gated Na+, Ca2+, K+ channel blocker, α/β-adrenergic antagonist, FIASMA)

Amitraz (α-adrenergic agonist, MAO inhibitor)

Amitriptyline Hydrochloride (FIASMA, σ1, RyR2, TrkA/B agonist, 5-HT2/6/7, M1-5 mAChR, histamine H1/4, α1-adr. antagonist, SERT, NET inhibitor, Kv1.1/7.2/7.3 K+, L-type Ca2+ channel blocker)

Anisodamine (α1-adrenergic and mAChR antagonist)

Arformoterol Tartrate (β2-adrenergic and TAS2R agonist)

Atenolol (β1-adrenergic antagonist)

Azaperone (α-adrenergic, D2, histamine antagonist)

Bambuterol Hydrochloride (β2-adrenergic agonist, BChE inhibitor)

Buspirone Hydrochloride (α1-adrenergic and 5-HT1A partial agonist, D2/3/4 antagonist)

Carvedilol (FIASMA; α1- and β1/2-adrenergic antagonist)

Carvedilol Phosphate Hemihydrate (FIASMA; α1- and β1/2-adrenergic antagonist)

Chlorpromazine Hydrochloride (FIASMA; D1/2/3/4, 5-HT1/2, M1/2 mAChR, α1/2-adrenergic antagonist)

Clenbuterol Hydrochloride (β2-adrenergic agonist)

Clomipramine Hydrochloride (FIASMA, mAChR, 5-HT2/3/6/7, α1/2-adrenergic antagonist, SERT and NET inhibitor, hERG K+ and L-type Ca2+ channel blocker)

Clonidine Hydrochloride (Imidazoline and α2-adrenergic agonist, Nav1.7 Na+ channel blocker)

Dapiprazole Hydrochloride (α1-Adrenergic antagonist)

Dimebon Dihydrochloride (AMPK activator, L-type Ca2+ channel and NMDA, histamine H1/2, α-adrenergic, 5-HT2C/5A/6 receptor antagonist)

Dobutamine Hydrochloride (β1-adrenergic agonist, β2- and α1-adrenergic antagonist)

Doxazosin Mesylate (α1-adrenergic antagonist)

Doxepin Hydrochloride (FIASMA, 5-HT1/2, M1-5 mAChR, α1-adrenergic, histamine H1/2 antagonist, SERT, NET, H+/K+ ATPase inhibitor)

Efaroxan Hydrochloride (α2-adrenergic and imidazoline-1 antagonist, ATP-sensitive K+ channel blocker)

Fenoldopam Mesylate (D1 partial agonist, potential α1-adrenergic antagonist)

Fluticasone Propionate (β2-adrenergic agonist)

Formoterol Fumarate Dihydrate (β2-adrenergic agonist)

Haloperidol (σ2 agonist, α1-adrenergic, D2, 5-HT2A, σ1 antagonist)

Hydroxyzine Dihydrochloride (FIASMA, histamine H1 inverse agonist, 5-HT2A, D1/2, α1-adrenergic antagonist)

Isoproterenol Hydrochloride (β-adrenergic agonist)

Ketanserin (5-HT2A antagonist, potential α1-adrenergic antagonist)

Lofexidine Hydrochloride (α2-adrenergic agonist)

Luteolin (DAT and NET potentiator, HSP90, IGF-1R, PDE inhibitor, potential α2-adrenergic antagonist)

Maprotiline Hydrochloride (FIASMA, histamine H1, 5-HT2, mAChR, α1-adrenergic antagonist, L-type Ca2+ channel blocker, NET inhibitor)

Methyldopa Sesquihydrate (DOPA decarboxylase inhibitor, indirect α2-adrenergic agonist)

Metoprolol Tartrate (β1-adrenergic antagonist)

Mirtazapine (5-HT1 agonist, 5-HT2/3 and α2-adrenergic antagonist, histamine H1 inverse agonist)

Naftopidil (α1-adrenergic antagonist)

Naphazoline Hydrochloride (α1-adrenergic agonist)

Naphazoline Nitrate (α1-adrenergic agonist)

Norepinephrine Bitartrate Monohydrate (α/β-adrenergic agonist)

Octopamine Hydrochloride (potential α/β-adrenergic agonist)

Olanzapine (AMPK activator, D1-4, 5-HT1A/2/3/6/7, M1-5 mAChR, α1/2-adrenergic antagonist)

Oxymetazoline Hydrochloride (α1-adrenergic agonist, α2-adrenergic partial agonist)

Phentolamine Hydrochloride (ATP-sensitive K+ channel activator, α-adrenergic antagonist)

Phentolamine Methanesulfonate (ATP-sensitive K+ channel activator, α-adrenergic antagonist)

Procaterol Hydrochloride (β2-adrenergic agonist)

Propafenone Hydrochloride (β-adrenergic antagonist, Kv1.4 and K2P2 K+ channel blocker)

Propranolol Hydrochloride (β1/2-adrenergic antagonist)

Quetiapine Fumarate (5-HT1A and σ1/2 agonist, 5-HT2A/2C/6/7, D1-4, histamine H1/2, M1 mAChR, α1A/1B/2C-adrenergic antagonist)

Ractopamine Hydrochloride (β1/2-adrenergic agonist)

Ritodrine Hydrochloride (β2-adrenergic agonist, SK/BK and ATP-sensitive K+ channel activator)

Salbutamol Free Base (β2-adrenergic agonist)

Salbutamol Sulfate (β2-adrenergic agonist)

Salmeterol (β2-adrenergic agonist)

Sertraline Hydrochloride (FIASMA, SERT and DAT inhibitor, α1-adrenergic antagonist, potential σ1 antagonist)

Silodosin (α1A-adrenergic antagonist)

Sotalol Hydrochloride (β-adrenergic antagonist, voltage-gated Na+ and K+ channel blocker)

Synephrine (adrenergic, TAAR-1, 5-HT agonist)

Tamsulosin Hydrochloride (α1-adrenergic antagonist)

Terazosin Hydrochloride Dihydrate (α1-adrenergic antagonist)

Terbutaline (β2-adrenergic agonist, potential ENaC activator)

Thioridazine Hydrochloride (FIASMA, D1-5, histamine H1/2, M1-5 mAChR, 5-HT1/2/5/6/7, α1/2-adrenergic antagonist, NET inhibitor, hERG K+ channel inhibitor)

Timolol Maleate (β-adrenergic antagonist)

Trazodone Hydrochloride (5-HT1A partial agonist, 5-HT2, histamine, α1/2-adrenergic antagonist, SERT inhibitor, voltage-gated K+ channel blocker)

Tulobuterol Hydrochloride (β2-adrenergic agonist)

Urapidil (5-HT1A agonist, α1-adrenergic antagonist)

Urapidil Hydrochloride (5-HT1A agonist, α1-adrenergic antagonist)

Vortioxetine (5-HT1A agonist, 5-HT1B partial agonist, 5-HT3A/7 antagonist, SERT inhibitor, potential β1-adrenergic agonist)

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Angiotensin Receptors

[Ile7]-Angiotensin III (AT1 agonist)

[Sar1 Ile8]-Angiotensin II (AT1 agonist, Na+/H+ transporter activator)

[Sar1]-Angiotensin II (AT1 agonist, Na+/H+ transporter activator)

[Val5]-Angiotensin II, human (AT1 agonist, Na+/H+ transporter activator)

Angiotensin II (1-4), human (AT1 agonist, Na+/H+ transporter activator)

Angiotensin II (3-8), human (AT1 agonist, Na+/H+ transporter activator)

Angiotensin II (4-8), human (AT1 agonist, Na+/H+ transporter activator)

Angiotensin II, human (AT1 agonist, Na+/H+ transporter activator)

Angiotensin III, human (AT1 agonist)

Candesartan (AT1 inhibitor)

Candesartan Celexetil Ester (AT1 inhibitor)

Irbesartan (PPARγ agonist, AT1 inhibitor)

Losartan Potassium (AT1 antagonist)

Olmesartan Medoxomil (AT1 inhibitor)

Telmisartan (AT-II antagonist, PPARγ/δ modulator)

Valsartan (AT1 inhibitor)

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Apelin Receptor

Apelin-13, human/cow (APJ agonist)

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Bombesin Receptors

[Tyr4]-Bombesin (bombesin and GRP agonist, hERG K+ channel blocker)

Bombesin (bombesin and GRP agonist, hERG K+ channel blocker)

Neuromedin B, pig (BB1 agonist)

Neuromedin C (18-27), pig (BB2 agonist)

Neuromedin U, rat (neuromedin agonist)

Phyllolitorin (GRP (BB1) and neuromedin B (BB2) agonist)

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Bradykinin Receptors

[Des-Arg9]-Bradykinin (B1/2 agonist)

[Des-Pro2]-Bradykinin (B1/2 agonist)

[DPhe7]-Bradykinin (B1/2 agonist)

[Hyp3]-Bradykinin (B1/2 agonist)

[Tyr8]-Bradykinin (B1/2 agonist)

Bradykinin (1-3) (B1/2 agonist)

Bradykinin (1-5) (B1/2 agonist)

Bradykinin (1-6) (B1/2 agonist)

Bradykinin (1-7) (B1/2 agonist)

Bradykinin (2-9) (B1/2 agonist)

Bradykinin Triacetate (B1/2 agonist)

Bradykinin Potentiator B (bradykinin inhibiting peptidase and ACE inhibitor)

Bradykinin Potentiator C (bradykinin inhibiting peptidase and ACE inhibitor)

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Calcitonin Receptors

Adrenomedullin (13-52), human (CLR-RAMP2/3 agonist)

Adrenomedullin (1-52), human (CLR-RAMP2/3 agonist)

Adrenomedullin (22-52), human (CLR-RAMP2/3 agonist)

Amylin (8-37), human (calcitonin-RAMP agonist)

Amylin (8-37), rat (calcitonin-RAMP agonist)

Amylin, cat (calcitonin-RAMP agonist)

Amylin, human (calcitonin-RAMP agonist)

Amylin, rat (calcitonin-RAMP agonist)

Calcitonin Gene Related Peptide (8-37), human (RAMP1 and CGRP agonist)

Calcitonin Gene Related Peptide (8-37), rat (RAMP1 and CGRP agonist)

Calcitonin Gene Related Peptide II, human (RAMP1 and CGRP agonist)

Calcitonin Gene Related Peptide II, rat (RAMP1 and CGRP agonist)

Calcitonin Gene Related Peptide, rat (RAMP1 and CGRP agonist)

α-Calcitonin Gene Related Peptide, chicken (RAMP1 and CGRP agonist)

α-Calcitonin Gene Related Peptide, human (RAMP1 and CGRP agonist)

β-Calcitonin Gene Related Peptide, human (RAMP1 and CGRP agonist)

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Cannabinoid Receptors

(−)-Epicatechin gallate (CB1 agonist)

(−)-Epigallocatechin (CB1 agonist)

Arvanil (CB1 agonist, TRPV1 agonist)

Valdecoxib (CB1 agonist, COX-2 inhibitor)

Yangonin (CB1 agonist, GABA-A potentiator)

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Cholecystokinin Receptors

Gastrin I, human (CCK2 agonist, indirect H+/K+ TPase activator)

Gastrin, chicken (CCK2 agonist, indirect H+/K+ ATPase activator)

Gastrin-1, rat (CCK2 agonist, indirect H+/K+ ATPase activator)

Lorglumide Sodium (CCK antagonist)

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Corticotropin-releasing Factor Receptors

Corticosterone (mineralocorticoid and glucocorticoid agonist)

Corticotropin Releasing Factor, cow (CRF agonist)

Corticotropin Releasing Factor, human/rat (CRF agonist)

Corticotropin Releasing Factor, sheep (CRF agonist)

Eplerenone (Mineralocorticoid antagonist)

Stresscopin, human (CRFR2 agonist)

Stresscopin-Related Peptide, human (CRFR2 agonist)

Urocortin II, human (CRF2 agonist)

Urocortin II, mouse (CRF2 agonist)

Urocortin III, human (CRF2 agonist)

Urocortin III, mouse (CRF2 agonist)

Urocortin, human (CRF1/2 agonist)

Urocortin, rat (CRF1/2 agonist)

Urotensin I (CRF1/2 agonist)

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Dopamine Receptors

Acepromazine Maleate (D1/2 and 5-HT1A/2A antagonist)

Amisulpride (5-HT7 and D2/3 antagonist)

Aniracetam (AMPA positive allosteric modulator, D2, 5-HT2A, nAChR agonist)

Aripiprazole (D2 and 5-HT1A partial agonist, 5-HT2C/6/7 antagonist, SERT inhibitor)

Azaperone (α-adrenergic, D2, histamine antagonist)

Buspirone Hydrochloride (α1-adrenergic and 5-HT1A partial agonist, D2/3/4 antagonist)

Chlorpromazine Hydrochloride (FIASMA; D1/2/3/4, 5-HT1/2, M1/2 mAChR, α1/2-adrenergic antagonist)

Cinnarizine (FIASMA, L-type Ca2+ channel blocker, D2 antagonist)

Clozapine (M4 mAChR agonist, 5-HT1A partial agonist, M1/2/3/5 mAChR, D2 antagonist, Kv1.1 K+ channel blocker)

Dopamine Hydrochloride (D1-5 agonist)

Fenoldopam Mesylate (D1 partial agonist, potential α1-adrenergic antagonist)

Fluphenazine Hydrochloride (FIASMA, D2 antagonist, hERG K+ channel blocker)

Haloperidol (σ2 agonist, α1-adrenergic, D2, 5-HT2A, σ1 antagonist)

Hydroxyzine Dihydrochloride (FIASMA, histamine H1 inverse agonist, 5-HT2A, D1/2, α1-adrenergic antagonist)

Iloperidone (D2 and 5-HT2A antagonist, potential hERG K+ channel blocker)

Itopride Hydrochloride (AChE inhibitor, D2 antagonist)

Melanostatin, frog (D2 modulator)

Melitracen Hydrochloride (potential D1/2 antagonist)

Memantine Hydrochloride (D2 agonist, NMDA, 5-HT3, α7 nAChR antagonist)

Olanzapine (AMPK activator, D1-4, 5-HT1A/2/3/6/7, M1-5 mAChR, α1/2-adrenergic antagonist)

Paliperidone (D2 and 5-HT2A antagonist)

Pramipexole Dihydrochloride (D2/3 agonist)

Quetiapine Fumarate (5-HT1A and σ1/2 agonist, 5-HT2A/2C/6/7, D1-4, histamine H1/2, M1 mAChR, α1A/1B/2C-adrenergic antagonist)

Risperidone (5-HT7 and NMDA agonist, D-amino acid oxidase inhibitor, 5-HT2A and D2 antagonist)

Ropinirole Hydrochloride (D2/3 agonist)

S-(−)-Sulpiride (GHB agonist, D2/3 antagonist)

R,S-(±)-Sulpiride (GHB agonist, D2/3 antagonist)

Tetrahydroberberine (5-HT1A agonist, D2 antagonist, ATP-sensitive K+ channel blocker)

D-Tetrahydropalmatine (D1 antagonist, organic cation transporter 1 inhibitor)

D,L-Tetrahydropalmatine (D1/2 antagonist, potential L-type Ca2+ and K+ channel blocker)

L-Tetrahydropalmatine (D1/2 antagonist)

Thioridazine Hydrochloride (FIASMA, D1-5, histamine H1/2, M1-5 mAChR, 5-HT1/2/5/6/7, α1/2-adrenergic antagonist, NET inhibitor, hERG K+ channel inhibitor)

Trifluoperazine Dihydrochloride (D1/2 and α1-adrenergic antagonist, calmodulin and CDPK4 inhibitor, Nav1.4 and Nav1.7 Na+ channel blocker)

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Endothelin Receptors

Big Endothelin-1 (1-38), human (ET-A/B/C agonist)

Endothelin-1, human (ET-A/B agonist)

Endothelin-2, human (ET-A/B agonist)

Endothelin-3, human (ET-B agonist)

Kendomycin (ET antagonist, proteasome inhibitor)

Macitentan (ET-A/B antagonist)

Sarafotoxin 6c (ET-B agonist, ATP-sensitive K+ channel activator)

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Formylpeptide Receptors

Boc-FLFLF (FRP1 antagonist)

Humanin, human (FPRL1/2 agonist)

N-formyl-Met-Ala-Ser (FPR1 agonist)

N-formyl-Met-Leu-Phe (FPR1 agonist)

N-formyl-Met-Leu-Phe-Lys (FPR1 agonist)

N-formyl-Nle-Leu-Phe-Nle-Tyr-Lys (FPR1 agonist)

Spinorphin, cow (P2X3 and N-formylpeptide antagonist, ACE, enkephalinase, aminopeptidase IV, neutral endopeptidase, DPP3 inhibitor)

WKYMVM-NH2 (FPRL1 agonist)

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Free Fatty Acid Receptors

Phytanic Acid (RXR and PPAR agonist, potential GPR40 agonist)

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Frizzled Class GPCRs

Cyclopamine (Smo inhibitor)

GDC-0449 (Smo inhibitor)

Itraconazole (14-α demethylase inhibitor, Smo modulator)

NVP-LDE225 Diphosphate (Smo inhibitor)

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Ghrelin Receptor

Cortistatin-14 (somatostatin and ghrelin agonist)

Ghrelin, human (ghrelin agonist)

Ghrelin, rat (ghrelin agonist)

Growth Hormone Releasing Hexapeptide (ghrelin agonist)

Growth Hormone Releasing Peptide 2 (ghrelin agonist)

Hexarelin (ghrelin agonist)

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Glucagon Receptors

Gastric Inhibitory Peptide, human (GIP-R agonist)

Secretin, human (SCTR agonist)

Secretin, pig (SCTR agonist)

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Histamine Receptors

Amitriptyline Hydrochloride (FIASMA, σ1, RyR2, TrkA/B agonist, 5-HT2/6/7, M1-5 mAChR, histamine H1/4, α1-adr. antagonist, SERT, NET inhibitor, Kv1.1/7.2/7.3 K+, L-type Ca2+ channel blocker)

Amoxapine (5-HT2/3/6/7, D2/3/4, histamine H1, α1-adrenergic antagonist, SERT and NET inhibitor, hERG K+ channel blocker)

Azaperone (α-adrenergic, D2, histamine antagonist)

Azelastine Hydrochloride (TRPV1 agonist, histamine H1 antagonist)

Brompheniramine Maleate (histamine H1 and mAChR antagonist, potential SERT and MAO-B inhibitor)

Cetirizine Dihydrochloride (Histamine H1 antagonist)

Chlorpheniramine Maleate (histamine H1 antagonist, SERT and NET inhibitor)

Cimetidine (Histamine H2 and AR antagonist, catalase inhibitor)

Desloratadine (FIASMA, histamine H1 antagonist)

Dimebon Dihydrochloride (AMPK activator, L-type Ca2+ channel and NMDA, histamine H1/2, α-adrenergic, 5-HT2C/5A/6 receptor antagonist)

Diphenhydramine Hydrochloride (Voltage-gated Na+ channel blocker, mAChR antagonist, histamine H1 inverse agonist)

Doxepin Hydrochloride (FIASMA, 5-HT1/2, M1-5 mAChR, α1-adrenergic, histamine H1/2 antagonist, SERT, NET, H+/K+ ATPase inhibitor)

Ebastine (Histamine H1 antagonist)

Famotidine (Histamine H2 antagonist, GSK-3β inhibitor)

Fexofenadine Hydrochloride (Histamine H1 antagonist)

Hydroxyzine Dihydrochloride (FIASMA, histamine H1 inverse agonist, 5-HT2A, D1/2, α1-adrenergic antagonist)

Ketotifen Fumarate (H1 histamine and LT antagonist, PDE inhibitor)

Levocetirizine Dihydrochloride (histamine H1 antagonist)

Loratadine (Histamine H1 antagonist, FIASMA)

Maprotiline Hydrochloride (FIASMA, histamine H1, 5-HT2, mAChR, α1-adrenergic antagonist, L-type Ca2+ channel blocker, NET inhibitor)

Mirtazapine (5-HT1 agonist, 5-HT2/3 and α2-adrenergic antagonist, histamine H1 inverse agonist)

Nizatidine (Histamine H2 inverse agonist)

Olopatadine Hydrochloride (histamine H1/2/3 antagonist)

Quetiapine Fumarate (5-HT1A and σ1/2 agonist, 5-HT2A/2C/6/7, D1-4, histamine H1/2, M1 mAChR, α1A/1B/2C-adrenergic antagonist)

Ranitidine Hydrochloride (Histamine H2 inverse agonist)

Roxatidine Acetate Hydrochloride (Histamine H2 antagonist)

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Hydroxycarboxylic Acid Receptors

Niacin (GPR109A agonist, hepatic diacylglycerol acyltransferase-2 inhibitor)

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Leukotriene Receptors

Ibudilast (PDE3/5 inhibitor, LTD4 antagonist)

Lupinine (AChE and BChE inhibitor, potential CD69 activator)

Montelukast Sodium (CysLT1 antagonist)

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Melanin-concentrating Hormone Receptors

Melanin Concentrating Hormone, human/mouse/rat (MCHR agonist)

Melanin Concentrating Hormone, salmon (MCHR agonist)

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Melanocortin Receptors

Adrenocorticotropic Hormone (1-4) (MC2 agonist)

Adrenocorticotropic Hormone (4-10), human (MC2 agonist)

Adrenocorticotropic Hormone (1-10), human (MC2 agonist)

Adrenocorticotropic Hormone (1-13), human (MC2 agonist)

Adrenocorticotropic Hormone (1-14) (MC2 agonist)

Adrenocorticotropic Hormone (1-16), human (MC2 agonist)

Adrenocorticotropic Hormone (1-17), human (MC2 agonist)

Adrenocorticotropic Hormone (1-24), human (MC2 agonist)

Adrenocorticotropic Hormone (1-39), human (MC2 agonist)

Adrenocorticotropic Hormone (1-39), rat (MC2 agonist)

Adrenocorticotropic Hormone (18-39), human (MC2 agonist)

Agomelatine (MT1/2 agonist, 5-HT2C antagonist)

Melatonin (MT agonist)

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Metabotropic Glutamate Receptors

Nefiracetam (NMDA and mGluR5 agonist, N-type and L-type Ca2+ channel activator, α4β2 nAChR potentiator)

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Motilin Receptor

Motilin, dog (motilin agonist)

Motilin, pig (motilin agonist)

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Neuropeptide Receptors

Neuropeptide Y (13-36), human (Y1-5 agonist)

Neuropeptide Y (3-36), human (Y1-5 agonist)

Neuropeptide Y, human/rat (Y1-5 agonist)

Pancreatic Polypeptide, chicken (Y4 agonist)

Pancreatic Polypeptide, human (Y4 agonist)

Pancreatic Polypeptide, rat (Y4 agonist)

Peptide YY (3-36), human (Y1/2 agonist)

Peptide YY, human (Y1/2 agonist)

Peptide YY, pig (Y1/2 agonist)

RF-NH2 (potential GPR147 agonist, potential acid-sensing ion channel activator)

RFRP-1, human (GPR147 activator)

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Opioid Receptors

Acetyl-α-Endorphin (μOr agonist)

Adrenorphin (μOR and κOR agonist)

BAM-12P (κOR agonist)

BAM-22P (κOR and μOR agonist)

CTAP (μOR agonist)

DAMGO (μOR agonist)

Deltorphin I (δOR agonist)

Dermenkephalin (δOR-2 agonist)

Dermorphin (δOR agonist)

Dermorphin Analog (δOR and μOR agonist)

Dextromethorphan Hydrobromide Hydrate (σ1/2and μ/κ/δ-OR agonist, α3β4/α4β2/α7 nAChR, SERT, NET, NMDA antagonist)

Endomorphin-1 (μOr agonist)

Endomorphin-2 (μOr agonist)

α-Endorphin (μOr agonist)

β-Endorphin, camel (μOr agonist)

β-Endorphin, human (μOr agonist)

β-Endorphin, rat (μOr agonist)

Hemorphin-7 (opioid agonist, ACE inhibitor)

Leu-Enkephalin (δOR and μOR agonist)

Loperamide Hydrochloride (FIASMA, μOR agonist, potential HCN channel blocker)

Met-Enkephalin (δOR and μOR agonist)

Met-Enkephalin Amide (δOR and μOR agonist)

Naltriben (δ2OR antagonist)

Nociceptin (NOP agonist)

Opioid Receptor Antagonist Ac-RFMWMK-NH2 (μ/δ/κ-OR inhibitor)

Trimebutine Maleate (L-type Ca2+ channel blocker, BK K+ channel modulator, potential opioid agonist)

Tyr-MIF-1 (μOR antagonist)

Tyr-W-MIF-1 (μOR antagonist)

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Orexin Receptors

Orexin B, human (OX2 agonist)

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Orphan Receptors

A-779 (Mas antagonist)

Bombesin (bombesin and GRP agonist, hERG K+ channel blocker)

[Tyr4]-Bombesin (bombesin and GRP agonist, hERG K+ channel blocker)

Gastrin Releasing Peptide, human (GRP agonist)

Gastrin Releasing Peptide, pig (GRP agonist)

Pancreastatin, pig (GRP78 inhibitor)

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P2Y Receptors

Clopidogrel Sulfate (P2Y12 antagonist)

Prasugrel (P2Y12 antagonist)

Suramin Hexasodium (RyR agonist, SIRT, telomerase, P2Y, GPCR inhibitor)

Ticagrelor (P2Y12 antagonist)

Ticlopidine Hydrochloride (P2Y12 antagonist)

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Parathyroid Hormone Receptors

Parathyroid Hormone (1-34), cow (PTH1/2 agonist)

Parathyroid Hormone-Related Protein (1-34), human/rat (PTH1 agonist)

Teriparatide Acetate (PTH1R agonist)

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Prolactin-releasing peptide Receptor

Prolactin-Releasing Peptide (1-31), human (GPR10 agonist)

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Prostanoid Receptors

MK-0524 (DP1 antagonist)

Ramatroban (CRTH2 inhibitor, TxA2 antagonist)

Seratrodast (TxA2 antagonist)

TM3-0089 Sodium Monohydrate (CRTH2 inhibitor)

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Proteinase-activated Receptors

SFLLR (PAR1 agonist)

Thrombin Receptor Agonist Peptide (PAR1 agonist)

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Somatostatin Receptors

Cortistatin-14 (somatostatin and ghrelin agonist)

Octreotide Acetate (somatostatin agonist)

Somatostatin-14 (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-25 (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-28 (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-28 (1-12) (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Somatostatin-28 (1-14) (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

[Tyr1]-Somatostatin (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

[Tyr11]-Somatostatin (somatostatin agonist, GABA modulator, P/Q-type, N-type, and L-type voltage-gated Ca2+ channel modulator)

Vapreotide (somatostatin 2 agonist, NK1 antagonist)

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Tachykinin Receptors

Aprepitant (NK1 antagonist)

Eledoisin (NK agonist)

Eledoisin Related Peptide (NK agonist)

Kassinin (NK2 agonist)

Men 10376 (NK2 antagonist)

Neurokinin A (4-10) (NK1/2 agonist)

Neuropeptide K, pig (NK2 agonist)

γ-Neuropeptide, rabbit (NK2 agonist)

Phyllomedusin (NK1 activator)

Substance P (NK1 agonist)

Substance P (1-4) (NK1 agonist)

Substance P (1-7) (NK1 agonist)

Substance P (1-9) (NK1 agonist)

Substance P (7-11) (NK1 agonist)

Substance P, Free Acid (NK1 agonist)

[Nle11]-Substance P (NK1 agonist)

[Pro9]-Substance P (NK1 agonist)

[Sar9]-Substance P (NK1 agonist)

[Tyr8]-Substance P (NK1 agonist)

Uperolein (NK-1 agonist)

Vapreotide (somatostatin 2 agonist, NK1 antagonist)

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Thyrotropin-releasing Hormone Receptors

Thyrotropin-releasing Hormone (TRHR agonist)

Thyrotropin-releasing Hormone, Free Acid (TRHR agonist)

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Trace Amine Receptor

Synephrine (adrenergic, TAAR-1, 5-HT agonist)

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Urotensin Receptor

Urotensin II, frog (UT agonist)

Urotensin II, human (UT agonist)

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Vasopressin and Oxytocin Receptors

Atosiban Acetate (V1/2 and OXTR antagonist)

Desmopressin (V2R agonist)

Desmopressin Acetate (V2 agonist)

Oxytocin (OXTR agonist, acid-sensing ion channel blocker)

Terlipressin Acetate (AVPR1 agonist)

Tolvaptan (V2 antagonist)

[Lys8]-Vasopressin (V1/2 agonist)

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VIP and PACAP Receptors

C-Myc Peptide (PAC1 agonist, CK2 activator)

Peptide Histidine Isoleucine, pig (VPAC2 agonist)

Peptide Histidine Isoleucine, rat (VPAC2 activator)

Pituitary Adenylate Cyclase-activating Peptide (6-38), human/sheep/rat (PAC1 and VPAC1/2 agonist)

Pituitary Adenylate Cyclase-activating Polypeptide (1-27), human, sheep, rat (PAC1 and VPAC1/2 agonist)

Pituitary Adenylate Cyclase-activating Polypeptide (1-38), frog (PAC1 and VPAC1/2 agonist)

Pituitary Adenylate Cyclase-activating Polypeptide (1-38), human, sheep, rat (PAC1 and VPAC1/2 agonist)

Pituitary Adenylate Cyclase-activating Polypeptide (6-27), human, sheep, rat (PAC1 and VPAC1/2 agonist)

Pituitary Adenylate Cyclase-activating Polypeptide-related Peptide, human (PAC1 and VPAC1/2 agonist)

Pituitary Adenylate Cyclase-activating Polypeptide-related Peptide, rat (PAC1 and VPAC1/2 agonist)

Vasoactive Intestinal Peptide (VPAC1/2 agonist)

Vasoactive Intestinal Peptide, guinea pig (VPAC1/2 agonist)

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