d5 receptor

dopamine D1 receptor antagonist

Nuciferine ((-)-Nuciferine) is an alkaloid found within the plants Nymphaea caerulea and Nelumbo nucifera. It has a profile of action associated with dopamine receptor blockade.

SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist, specifically targeting D1 and D5 receptors with Ki values of 0.2 nM and 0.3 nM, respectively.

SKF 38393 hydrochloride (SKF38393 HCl) is a selective dopamine D1/D5 receptor agonist.

D1/D5 Receptor agonist-1 is an orally active D1/D5 receptor agonist with the ability to cross the blood-brain barrier. It demonstrates significant efficacy in the cAMP pathway and β-arrestin recruitment, with EC50 values of 3.7 nM for D1R cAMP, 91 nM for D1R β-arrestin, and 129 nM for D1R internalization, and a Ki value of 111 nM for D1R binding affinity. In rats, D1/D5 Receptor agonist-1 inhibits β-arrestin signaling involved in L-DOPA-induced dyskinesia. This compound is applicable in Parkinson's disease research.

SKF83959, a benzazepine analog, is a selective and potent partial agonist of the dopamine D1 receptor with Ki values of 1.18, 7.56, 920, and 399 nM for rat D1, D5, D2, and D3 receptors, respectively.SKF83959 is a potent variant modulator of the sigma (σ)-1 receptor, which ameliorates cognitive dysfunction for the study depression and Alzheimer's disease.

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

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

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.

(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine, a full agonist of the dopamine receptor and a partial agonist of the 5-HT1A receptor.

Tavapadon (CVL-751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist.

Rotigotine Hydrochloride (N-0924), a dopamine receptor agonist prefering for D3 receptors over D1 and D2, has effective activity of anti-Parkinsonian. Racemic rotigotine hydrochloride is about 50 times as potent as quinpirole, the gold standard D2 agonist.

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

SKF 83959 hydrobromide is a Dopamine D1-like receptor partial agonist.

5-HT2A serotonin and selective D2-like dopamine receptor antagonist

Ecopipam (UNII-0X748O646K) is a potent, selective, and orally active antagonist of dopamine D1/D5 receptors, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam demonstrates more than 40-fold selectivity over D2, D4, 5-HT, and α2a receptors (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). It is used in research on schizophrenia and obesity.

Ecopipam (SCH 39166) hydrochloride is a highly potent, selective, and orally active antagonist of dopamine D1/D5 receptors. It exhibits impressive binding affinities, with Ki values of 1.2 nM and 2.0 nM for D1 and D5 receptors, respectively. Ecopipam hydrochloride demonstrates remarkable selectivity, displaying over 40-fold selectivity compared to D2, D4, 5-HT, and α2a receptors, with Ki values of 0.98 μM, 5.52 μM, 0.08 μM, and 0.73 μM, respectively. Its application extends to various areas of research, including schizophrenia, cocaine addiction, and obesity [1] [3].

Rotigotine (N-0923) is a non-ergot dopamine receptor agonist used in the therapy of Parkinson disease and restless leg syndrome. Administered as a once-daily transdermal patch, Rotigotine has not been associated with serum enzyme elevations during treatment or with episodes of clinically apparent liver injury.

Ecopipam (SCH 39166) hydrobromide is a highly potent, specific, and orally active dopamine D1/D5 receptor antagonist with K i values of 1.2 nM for D1 and 2.0 nM for D5 receptors. It shows over 40-fold greater selectivity for D1/D5 over D2, D4, 5-HT, and α2a receptors, with K i values of 0.98, 5.52, 0.08, and 0.73 μM, respectively, and is relevant for schizophrenia and obesity research.

NGD 94-1 is a selective D4 receptor antagonist with an affinity of 3 nM for the D4 receptor and greater than 2 pM for the D1, D2, D3, and D5 receptors.NGD 94-1 can be used in the study of cognitive disorders and other psychiatric disorders.

Azilsartan-D5 is the deuterium-labeled Azilsartan. Azilsartan (T1057) is a specific antagonist of the angiotensin II type 1 receptor.

Blonanserin-D5 is a deuterium-labeled Blonanserin. Blonanserin (T1180) (AD-5423) is a dopamine D2/5-HT2 receptor antagonist with an atypical antipsychotic effect.

Solifenacin-D5 hydrochloride is a deuterium-labeled Solifenacin hydrochloride (T23379), which acts as an antagonist of muscarinic receptors with pKis of 7.6, 6.9, and 8.0 for M1, M2, and M3 receptors, respectively.

Tamoxifen-d5 is a deuterated form of Tamoxifen. Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that blocks estrogen action in breast cells while activating estrogenic activity in other cells, such as those in bone, liver, and uterus. Tamoxifen is also a potent activator of Hsp90 and enhances the ATPase activity of the Hsp90 molecular chaperone.