GPCR/G-Protein

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

Norreticuline is a potential adrenoceptor-α/β agonist and CYP2D6 and D2 receptor inhibitor for the study of neurodegenerative diseases.

Hydroxy ziprasidone is an impurity of Ziprasidone. Ziprasidone, an antipsychotic agent, is a 5-HT and dopamine receptor antagonist.

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

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

Proxyfan Oxalate is a potent antagonist of the histamine H3 receptor (histamine H3 receptor), with Ki values of 2.9 nM for rats and 2.7 nM for humans. Its inhibitory effect on H3 receptors is over 1000 times stronger than its effect on other histamine receptors.

Caerulein, desulfated (FI-6934, desulfated) is a desulfated compound formed after caerulein hydrolysis, a neuropeptide with lower smooth muscle activity.

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.

MK-447 is a nonsteroidal antiinflammatory agent.

Amidephrine hydrochloride is a biochemical.

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

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

7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene is a liver receptor homolog-1 (LRH-1) antagonist (IC50: 3.1 μM).

AR244555 is a bioactive chemical.

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

R-138727 is a novel P2Y12 receptor inhibitor.

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.

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.

Dehydroabiethylamine (NSC-2955) boosts liver CYP2B, blocks PDKs & cholesterol transport, and has anti-tumor effects.