human d1 receptor

NCGC00135472 (DRV1 (GPR32) agonist C2A) is a human Resolvin DI receptor DRV1 agonist with pro-catabolic properties that activates the human soluble protein D1 receptor DRV1 GPR32 receptor in beta-blocker and cAMP assays with EC50s of 0.37 uM and 0.05 uM, respectively.NCGC00135472 induces in cells overexpressing recombinant DRV1 rapid impedance changes that stimulate phagocytosis of serum-treated zymoglycans.

dopamine D1 receptor antagonist

Iloperidone (HP 873) is an atypical antipsychotic agent that is used for treatment of schizophrenia.

Chlorprothixene (Truxal) is a typical antipsychotic drug of the thioxanthene class, which was the first of the series to be synthesized.

UCM-1306 is a potent and orally active allosteric modulator (PAM) of the human dopamine D1 receptor. It increases the maximal effect of endogenous dopamine (DA) in both human and mouse D1 receptors. UCM-1306 could improve motor symptoms and address key comorbid cognitive impairment associated with long-term Parkinson's disease (PD).

Protectin D1 (also known as neuroprotectin D1 when produced in neuronal tissues) is a DHA-derived dihydroxy fatty acid that exhibits potent protective and anti-inflammatory activities. 10(S),17(S)-DiHDHA is a DHA metabolite, also referred to as protectin DX (PDX). It is produced by an apparent double lipoxygenase (LO)-mediated reaction in murine peritonitis exudates, in suspensions of human leukocytes, or by soybean 15-LO incubated with DHA. It differs from protectin D1 with respect to the stereochemistry of the C-10 hydroxyl and the double bond configuration at the 13 and 15 positions. 10(S),17(S)-DiHDHA blocks neutrophil infiltration in murine peritonitis by 20-25% at a dose of 1 ng/mouse. It also inhibits platelet activation by both impairing thromboxane (TX) synthesis and TX receptor activation.

Iloperidone hydrochloride is a D(2) 5-HT(2) receptor antagonist. It is also an atypical antipsychotic for the treatment of schizophrenia symptoms.

A-381393 is a selective and brain penetrate dopamine D4 receptor antagonist (Kis: 1.9 1.5 1.6 nM for human dopamine D4.2 D4.4 D4.7 receptor).

PF2562 is a dopamine D1 ligand. It is used as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor (Ki: 113 nM). PF2562 shows activity against human D1 cAMP (EC50: 568 nM in HTRF assay).

DETQ, a selective, allosteric, and orally active potentiator of the dopamine D1 receptor (Dopamine Receptor), enhances cAMP production in HEK293 cells expressing the human D1 receptor, achieving an EC50 of 5.8 nM and a K b of 26 nM. It demonstrates approximately 30-fold reduced potency at rat and mouse D1 receptors and shows no activity at the human D5 receptor [1].

PF-06256142 is a potent and selective orthosteric D1 receptor agonist(D1 EC50=30 nM ).

Chlorprothixene hydrochloride (Truxal hydrochloride) brings strong blocking effects by blocking the 5-HT2 D1, D2, D3, histamine H1, muscarinic and alpha1 adrenergic receptors. Chlorprothixene hydrochloride s a typical antipsychotic drug of the thioxanthene (tricyclic) class.

LY3154207 is a subtype selective, potent, and orally available human dopamine D1 receptor positive allosteric modulator (PAM) with minimal allosteric agonist activity (EC50=3 nM).

Iloperidone metabolite P95 is a metabolite of the atypical antipsychotic iloperidone . It binds to the serotonin (5-HT) receptor subtype 5-HT2A and α1-, α2B-, and α2C-adrenergic receptors with mean Ki values of 7.08, 21.38, 83.18, and 47.86 nM, respectively, but does not cross the blood-brain barrier.

GR 103691, a potent and selective dopamine D3 receptor antagonist (Ki: 0.4 nM), exhibits more than 100-fold selectivity for human dopamine D3 receptors over human D4 and D1 sites.