GPCR/G-Protein

Benzylthiouracil (6-Benzyl-2-thiouracil) induces ANCA-associated glomerulonephritis in Graves' disease patients and is used to study hyperthyroidism.

Rolofylline (KW-3902) is an adenosine A1 receptor antagonist used to study acute congestive heart failure and renal dysfunction.

Bucindolol (BMY 13105) is a novel and potent β1-adrenergic receptor blocker that mediates vasodilation and can be used to study chronic heart failure.

A2ti-1 is an annexin A2/S100A10 heterotetramer (A2t) inhibitor that inhibits Src activation and can be used to study human papillomavirus type 16 infection.

Latrepirdine dihydrochloride (Dimebolin dihydrochloride) is an orally active, and neuroactive antagonist of multiple drug targets.

CP-105696 is a potent and selective leukotriene B4 (LTB4) receptor antagonist for the study of allograft rejection.

LP-533401 hydrochloride is a peripheral Tph inhibitor that does not cross the BBB and can be used to study periodontal disease and hepatic steatosis.

5-LOX inhibitor (1-(sec-Butyl)-4-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one) is an itraconazole impurity, a LOX-5 inhibitor.

Rizatriptan (Risatriptan) is a selective 5-hydroxytryptamine 1B/1D receptor agonist used in the study of migraine.

L-368,899 hydrochloride is an OXTR antagonist that prevents oxytocin-induced antiabnormal pain and anti-nausea, and may be used in the study of depression.

Jatrorrhizine chloride (Neprotine chloride) is an alkaloid isolated from Rhizoma coptidis with neuroprotective, antimicrobial, and antiplasmodial activities.

Ketanserin tartrate (KJK-945 tartrate) is a 5-HT2A receptor and α1-adrenergic receptor antagonist for the study of systemic sclerosis.

Trazpiroben (TAK-906) is a selective dopamine D2/D3 receptor antagonist used in the study of gastroparesis.

Setiptiline (Org-8282) is a norepinephrine reuptake inhibitor, 2-adrenergic receptor antagonist, H1 receptor inverse agonist with antidepressant activity.

Alfuzosin (SL 77499) is an alpha-1 adrenergic antagonist used to treat benign prostatic hypertrophy and urethral dysfunction.

ACT-462206 is a Orexin 1/Orexin 2 receptor antagonist.ACT-462206 is highly potent and can be used to study sleep and anxiety.

S1RA (E-52862)(E-52862) is a potent, selective antagonist of the sigma-1 receptor (σ1R, Ki=17 nM), demonstrating significant selectivity over the sigma-2

Syk inhibitor II, a cell-permeable, ATP-competitive, pyrimidine-carboxamide compound, selectively and reversibly inhibits Syk (IC50 = 41 nM).

(S)-Pramipexole-(N-Propyl-2,2,3,3,3-d5) Dihydrochloride is a deuterated compound of (S)-Pramipexole Dihydrochloride. (S)-Pramipexole Dihydrochloride has a CAS number of 104632-25-9. Pramipexole dihydrochloride could be used to treat Parkinson disease.

Hydroxyzine-d8 DiHCl is a deuterated compound of Hydroxyzine DiHCl. Hydroxyzine DiHCl has a CAS number of 2192-20-3.

R 59-022 (DKGI-I) is a DGK inhibitor and a 5-HT Receptor antagonist that blocks filovirus internalization in host cells.

SR59230A hydrochloride (SR59230A HCl) is a beta3-adrenergic receptor antagonist that inhibits ultradian brown adipose tissue thermogenesis.

L-745870 is a D4 receptor antagonist that also inhibits D2 receptors, 5-HT2 receptors, and α-adrenergic receptors.

Ropinirole, D2-like agonist, no D1 affinity, Ki 29 nM for D2, treats Parkinson's.

Travoprost (Fluprostenol isopropyl ester) is used to treat glaucoma and ocular hypertension,is a potent and selective FP prostaglandin receptor agonist.

<p>Cyproheptadine hydrochloride (Periactin hydrochloride) is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist.</p>

PACAP (1-38), human, ovine, rat (Pituitary Adenylate Cyclase Activating Polypeptide 38) is a neuropeptide with 38 amino acid residues.

Carlumab is a high-affinity human monoclonal antibody that targets CCL2, suppressing the recruitment of monocytes/macrophages in the tumour microenvironment.

Uliledlimab, a humanized monoclonal antibody against CD73, reduces extracellular adenosine production and modulates immunosuppressive pathways.

Ziprasidone, an antipsychotic agent, functions as a dual antagonist of 5-HT (serotonin) and dopamine receptors.

Blontuvetmab (AT 004), a caninized CD20 monoclonal antibody, is utilized in the study of Canine B-cell lymphoma [1].

N-Methyl amisulpride (Amisulpride impurity H) is a 5-HT7 receptor, D2 receptor, and D3 receptor antagonist used in the study of acute schizophrenia.

Escitalopram (Seroplex), a serotonin inhibitor for depression, curbs alcohol intake and is favored over tricyclics for tardive dyskinesia.

Arazasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27.

Risperidone Mesylate is a selective serotonin 5-HT2 receptor and dopamine D2 receptor blocker.

P2Y14R antagonist 1 (compound I-17) is a selective oral that inhibits inflammatory response in acute gouty arthritis the NLRP3/GSDMD y and cellular pyroptosis.

GPR183-IN-1 (compound 15) is an effective orally active inhibitor of GPR183. It inhibits Ca2+ mobilization with an IC50 value of 39.97 nM. GPR183-IN-1 holds potential for research in cancer, autoimmune diseases, pain, and osteoporosis.

Rocatinlimab (AMG 451) (KHK4083) is a fully human, non-fucosylated IgG1 anti-OX40 monoclonal antibody indicated for atopic dermatitis (AD) research [1].

Methaphenilene hydrochloride is an H1 receptor antagonist with antihistaminic and anticholinergic activity, in allergic inflammation and autonomic research.

Olopatadine is an antihistamine and anti-allergy medication for itchy eyes, also possibly treats red skin syndrome.

Triflupromazine is a dopamine receptor D1/D2 antagonist and LHDA inhibitor that suppresses dopamine activity in (CNS)mental disorders, sedation, and antiemesis.

DL-Phenylephrine HCl is a selective agonist of the alpha1-adrenergic receptor.

Metoxibutropate is a biochemical.

Fremanezumab (TEV-48125) is a humanised monoclonal antibody targeting CGRP, capable of neutralising human, mouse and rat CGRP, migraine.

<p>PF-610355 is a long-acting and potent β2-adrenergic receptor agonist (EC50: 0.26 nM).PF-610355 can be used to study asthma and COPD.</p>

Mibavademab is a humanized anti-leptin receptor (LEPR) mAb under investigation for treating congenital leptin deficiency.

Methicillin: Narrow-spectrum beta-lactam, penicillin-type antibiotic for certain gram-positive bacterial infections.

Tulobuterol is mainly used for the prevention and treatment of bronchial asthma, asthmatic bronchitis and chronic bronchitis. Research shows that it could inhibit rhinovirus infection in primary cultures of human tracheal epithelial cells.

Buflomedil is a vasoactive compound. Buflomedil has been used for peripheral arterial diseases.

<p>Eptinezumab is a humanised monoclonal antibody targeting CGRP (calcitonin gene-related peptide), which prevents CGRP binding to its receptor, migraine.</p>

17-phenyl trinor PGF2α N-ethyl amide is an F-series prostaglandin analog which has been approved for use as an ocular hypotensive drug, sold under the Allergan

GLP-1 Receptormodulator 1 (Compound 7) is an effective positive allosteric modulator of the GLP-1 receptor. It is utilized in the research of obesity and type 2 diabetes.

Amitriptyline-d6 Hydrochloride is a deuterated compound of Amitriptyline Hydrochloride. Amitriptyline Hydrochloride has a CAS number of 549-18-8. Amitriptyline Hydrochloride is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities.

Mirtazapine D3 is a deuterium labeled Mirtazapine. Mirtazapine is an inhibitor of 5-HT receptor .

Brexpiprazole D8 is a deuterium-modified partial agonist of 5-HT1A and dopamine receptors, with Ki values of 0.12 nM and 0.3 nM respectively.

Mianserin-d3 is a deuterated compound of Mianserin. Mianserin has a CAS number of 24219-97-4. Mianserin, an H1 receptor reverse agonist, is a psychoactive compound in the tetracyclic antidepressant (TeCA) treatment family. Mianserin has antidepressant, antianxiety, antiemetic, hypotrophic, hypnotic and antihistamine effects, and can be used as a combination of norepinephrine and specific serotonin to treat depression.

15-keto Prostaglandin F2α is a metabolite of Prostaglandin F2α that lowers intraocular pressure in rabbits.

Cinnarizine D8 is a deuterium-labeled Cinnarizine which is an antihistamine and a calcium channel blocker.

Dapagliflozin D5 (BMS-512148 D5) is deuterated Dapagliflozin. Dapagliflozin is a competitive SGLT2 inhibitor.

Roxatidine acetate: anti-ulcer, blocks histamine, reduces acid. Safer at lower doses.

MCI-225 dehydratase is an oral, selective inhibitor of noradrenaline reuptake, and functions as a 5-HT3 antagonist, exhibiting antidepressant effects in vivo .

Penbutolol sulfate ((-)-Terbuclomine) is able to bind to both β2-adrenergic receptor and β1-adrenergic receptor, thus making it a non-selective β blocker.

AR244555 is a bioactive chemical.

S 25585 is a neuropeptide Y (NPY) Y5 receptor antagonist.

SB 271046 hydrochloride (SB 271046A) is selective, orally active 5-HT6 antagonist and is > 200-fold selective over 55 other receptors, enzymes and ion channels.

R-138727 is a novel P2Y12 receptor inhibitor.

Pardoprunox (SLV-308) is a partial dopamine D2 agonist and noradrenergic agonist with serotonin 5-HT1A agonist properties.

Bethanidine sulfate and its ortho-chloro derivative (BW 392C60) are potent adrenergic neuron blockers exhibiting sympathomimetic effects similar to those of bromobenzamine and guanethidine in various animal models, particularly in cats. These compounds inhibit the release of norepinephrine during neural stimulation and enhance the responsiveness of smooth muscle to epinephrine and norepinephrine. Notably, bethanidine sulfate increases the pressor response to tyramine, although this effect diminishes with higher doses. Unlike guanethidine, bethanidine sulfate does not deplete pressor amines in the iris of cats following administration. Additionally, it temporarily suppresses autonomic cholinergic mechanisms and can cause transient neuromuscular paralysis at large doses, contrasting its long-term adrenergic neuron blocking effects.

Diclofensine (Ro 8-4650) inhibits the uptake of serotonin, noradrenaline and dopamine.

Ticlopidine (PCR 5332) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor.

<p>Ketanserinol is a metabolite of the antihypertensive drug ketanserin, which blocks 5-HT2 receptors to treat protamine-induced pulmonary hypertension.</p>

MK-447 is a nonsteroidal antiinflammatory agent.

6-Hydroxy Buspirone, an active metabolite of the anxiolytic compound buspirone, is produced via the cytochrome P450 (CYP) isoform CYP3A4.

Litorin suppresses appetite and stimulates smooth muscle, gastrin, gastric acid, and pancreatic secretion.

<p>Itopride HCl combats dyspepsia and GERD, inhibiting AChE and blocking D2 receptors.</p>

Isoproterenol sulfate anhydrous is a useful alkaloid. It is used for biological research.

7-Desmethyl-3-hydroxyagomelatine, less active than parent drug Agomelatine, is a melatonergic agonist and 5-HT2C antagonist.

Amidephrine is an adrenergic agent.

Compound 17, a dopamine D4 receptor ligand, exhibits high potency and selectivity with IC 50 values of 0.057 nM for D4, and >1000, 220, and 270 nM for D2, 5-HT1A, and α1 receptors, respectively [1].

ICI-118551 Hydrochloride (ICI-118,551) is a highly selective β2-adrenergic receptor antagonist with Ki values of 0.7, 49.5 and 611 nM for β2, β1 and β3

Ciproxifan (FUB-359) is a highly effective and specific histamin H3-receptor antagonist (IC50: 9.2 nM).

5-Methyltryptamine hydrochloride is a high-affinity 5-HT1C receptor ligand and a partial agonist of 5-HT. 5-Methyltryptamine hydrochloride protects mice subjected to burn, tourniquet and endotoxin shock.