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dopamine D1/D2/D3/D4 receptor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Dopamine Receptor (25) 5-HT Receptor (10) Adrenergic Receptor (14) Chloride Channel (1) Histamine Receptor (2) Isotope-Labeled Compounds (5) mAChR (2) Parasite (1) PERK (1) Reference Standards (4) Sigma Receptor (2) STAT (2)
By Research Areas:	Cancer (2) Endocrinology (9) Inflammation/Immunology (1) Neurological Disease (22)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Dopamine Receptor Dopamine β-hydroxylase Dopamine Transporter

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-75502

Rotigotine 3 Publications Verification N-0923; (-)-N 0437	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
Rotigotine is a potent **dopamine receptor agonist with K_i** values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research .

HY-A0007

Rotigotine Hydrochloride 3 Publications Verification N-0923 Hydrochloride	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease
Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of **dopamine receptor*, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_i* of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-116941

A-381393	Dopamine Receptor	Neurological Disease
A-381393 is a potent, selective, brain penetrate **dopamine D₄ receptor antagonist, with K_i*s of 1.5, 1.9 and 1.6 nM for human dopamine* D_4.4, D_4.2, and D_4.7 receptor, respectively, >2700-fold selectivity over D₁, D₂, D₃ and D₅ dopamine receptors. A-381393 shows moderate affinity for 5-HT_2A (K_i, 370 nM) .

HY-B1371A

Spiperone hydrochloride 2 Publications Verification Spiroperidol hydrochloride	Dopamine Receptor 5-HT Receptor Adrenergic Receptor Chloride Channel	Neurological Disease Inflammation/Immunology
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective **dopamine D₂ receptor (K_i** values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D₂, D₃, D₄, D₁ and D₅ receptors, respectively) and 5-HT_2A/5-HT_1A receptor (K_is of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities .

HY-N0927

(-)-Isocorypalmine Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine	Dopamine Receptor	Others Neurological Disease
(-)-Isocorypalmine (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) is a **dopamine receptor** ligand and modulator capable of crossing the blood-brain barrier. (-)-Isocorypalmine exhibits receptor selectivity, acting as a partial agonist of dopamine D1 and D5 receptors (coupled via Gs proteins), as well as an antagonist of D2, D3 and D4 receptors (by blocking Gi protein-mediated signaling). (-)-Isocorypalmine shows no significant binding to various non-dopamine receptors, ion channels and transporters. (-)-Isocorypalmine is metabolically stable in vivo, effectively inhibits spontaneous and cocaine-induced hyperlocomotion, sensitization and conditioned place preference in mice, and does not induce addictive place preference when administered alone. (-)-Isocorypalmine can be used in addiction research .

HY-103409

ABT-724 trihydrochloride	Dopamine Receptor	Neurological Disease
ABT-724 trihydrochloride is a potent and highly selective **dopamine D₄ receptor agonist with an EC₅₀** of 12.4 nM for human dopamine D₄ receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D₄ (EC₅₀ of 14.3 nM) and the ferret D₄ receptor (EC₅₀ of 23.2 nM), and has no effect on dopamine D₁, D₂, D₃, or D₅ receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .

HY-15394

(Rac)-Rotigotine hydrochloride N-0437 hydrochloride	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
(Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of **dopamine receptor*, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine* D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-12697

NGB 2904	Dopamine Receptor	Neurological Disease
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of **dopamine D3 receptor, with a K_i** of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .

HY-14330

ABT-724	Dopamine Receptor	Neurological Disease
ABT-724, a chemical probe, is a potent and highly selective **dopamine D₄ receptor agonist with an EC₅₀** of 12.4 nM for human dopamine D₄ receptor. ABT-724 is a potent partial agonist at the rat D₄ (EC₅₀ of 14.3 nM) and the ferret D₄ receptor (EC₅₀ of 23.2 nM). ABT-724 has no effect on dopamine D₁, D₂, D₃, or D₅ receptors. ABT-724 could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .

HY-12987S

Pimozide-d4 R6238-d₄	Dopamine Receptor Adrenergic Receptor STAT	Neurological Disease Endocrinology Cancer
Pimozide-d₄ is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with K_is of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a K_i of 39 nM; Pimozide also inhibits STAT3 and STAT5 .

HY-15394S

(Rac)-Rotigotine-d7 (hydrochloride) N-0437-d₇ (hydrochloride)	Isotope-Labeled Compounds Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
(Rac)-Rotigotine-d₇ (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-A0007S

Rotigotine-d7 hydrochloride N-0923 D7 Hydrochloride	Isotope-Labeled Compounds Dopamine Receptor	Neurological Disease
Rotigotine-d₇ (N-0923-d₇) hydrochloride is the deuterium labeled Rotigotine(HY-75502). Rotigotine is a potent dopamine receptor agonist with K_i values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.

HY-167901

Dinoxyline	Dopamine Receptor	Neurological Disease
Dinoxyline is a potent agonist at **dopamine receptors (K_i** = 7 nM, 6 nM, 5 nM, 43 nM for D1, D2, D3 and D4). Dinoxyline can be utilized in neurological research .

HY-103414S

Raclopride-d5 hydrochloride	Isotope-Labeled Compounds Dopamine Receptor	Neurological Disease
Raclopride-d₅ hydrochloride is the deuterium labeled Raclopride. Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (K_is) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively .

HY-15394A

(Rac)-Rotigotine N-0437	Adrenergic Receptor 5-HT Receptor Dopamine Receptor	Neurological Disease Endocrinology
(Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of **dopamine receptor*, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine* D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-15394S1

(Rac)-Rotigotine-d3 hydrochloride N-0437-D3 hydrochloride	Isotope-Labeled Compounds Adrenergic Receptor Dopamine Receptor 5-HT Receptor	Endocrinology
(Rac)-Rotigotine-d₃ hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of **dopamine receptor*, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine* D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-A0139

Thiothixene NSC 108165; Navan; Navane	Sigma Receptor mAChR Histamine Receptor Dopamine Receptor Adrenergic Receptor	Others
Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

HY-12987S2

Pimozide-d4-1 R6238-d₄-1	Dopamine Receptor Adrenergic Receptor STAT Parasite	Neurological Disease Endocrinology Cancer
Pimozide-d₄-1 is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with K_is of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a K_i of 39 nM; Pimozide also inhibits STAT3 and STAT5 .

HY-12697A

NGB 2904 hydrochloride	Dopamine Receptor	Neurological Disease
NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of **dopamine D3 receptor, with a K_i** of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis .

HY-A0007R

Rotigotine Hydrochloride (Standard) N-0923 Hydrochloride (Standard)	Reference Standards Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease
Rotigotine (Hydrochloride) (Standard) is the analytical standard of Rotigotine (Hydrochloride). This product is intended for research and analytical applications. Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of **dopamine receptor*, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_i* of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-15394R

(Rac)-Rotigotine hydrochloride (Standard) N-0437 hydrochloride (Standard)	Dopamine Receptor Adrenergic Receptor 5-HT Receptor Reference Standards	Neurological Disease Endocrinology
(Rac)-Rotigotine (hydrochloride) (Standard) is the analytical standard of (Rac)-Rotigotine (hydrochloride). This product is intended for research and analytical applications. (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-75502R

Rotigotine (Standard) N-0923 (Standard); (-)-N 0437 (Standard)	Reference Standards Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
Rotigotine (Standard) is the analytical standard of Rotigotine. This product is intended for research and analytical applications. Rotigotine is a potent **dopamine receptor agonist with K_i** values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research .

HY-175504

MLS6357	Dopamine Receptor PERK	Neurological Disease
MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC₅₀s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC₅₀ > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC₅₀ of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .

HY-103409R

ABT-724 trihydrochloride (Standard)	Reference Standards Dopamine Receptor	Neurological Disease
ABT-724 trihydrochloride (Standard) is the analytical standard of ABT-724 trihydrochloride (HY-103409). This product is intended for research and analytical applications. ABT-724 trihydrochloride is a potent and highly selective dopamine D4 receptor agonist with an EC₅₀ of 12.4 nM for human dopamine D4 receptor. ABT-724 trihydrochloride is a potent partial agonist at the rat D4 (EC₅₀ of 14.3 nM) and the ferret D4 receptor (EC₅₀ of 23.2 nM), and has no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 trihydrochloride could be useful for the treatment of erectile dysfunction and has favorable side-effect profile .

HY-W748758

(Z)-Thiothixene-d8 NSC 108165-d₈; Navan-d₈; Navane-d₈	Isotope-Labeled Compounds Dopamine Receptor Histamine Receptor mAChR Adrenergic Receptor Sigma Receptor	Others
(Z)-Thiothixene-d₈ (NSC 108165-d₈; Navan-d₈; Navane-d₈) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

Cat. No.	Product Name

HY-L165

Dopamine Receptor Compound Library	267 compounds
Dopamine receptor (DAR), widely distributed in the brain, plays a key role in regulating motor function, motivation, driving force and cognition. The role of DA is mediated by D1-type (D1, D5) and D2-type receptors (D2S, D2L, D3, D4), which are distributed in presynaptic, postsynaptic and extrasynaptic, projection neurons and interneurons. Each receptor has a different function. D1 and D5 receptors couple with G stimulation sites and activate Adenylyl cyclase. The activation of Adenylyl cyclase leads to the production of the second messenger cAMP, which leads to the production of protein kinase A (PKA), which leads to further transcription in the nucleus. D2 to D4 receptors are coupled to G inhibitory sites to inhibit adenylyl cyclase and activate potassium Ion channel. These receptors utilize phosphorylation cascades or direct membrane interactions to affect the functions of voltage-gated and neurotransmitter-gated channels, cytoplasmic enzymes, and transcription factors. Dopamine receptor plays an important role in daily life. MCE designs a unique collection of 267 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.

Dopamine Receptor Compound Library

267 compounds

Dopamine receptor (DAR), widely distributed in the brain, plays a key role in regulating motor function, motivation, driving force and cognition. The role of DA is mediated by D1-type (D1, D5) and D2-type receptors (D2S, D2L, D3, D4), which are distributed in presynaptic, postsynaptic and extrasynaptic, projection neurons and interneurons. Each receptor has a different function. D1 and D5 receptors couple with G stimulation sites and activate Adenylyl cyclase. The activation of Adenylyl cyclase leads to the production of the second messenger cAMP, which leads to the production of protein kinase A (PKA), which leads to further transcription in the nucleus. D2 to D4 receptors are coupled to G inhibitory sites to inhibit adenylyl cyclase and activate potassium Ion channel. These receptors utilize phosphorylation cascades or direct membrane interactions to affect the functions of voltage-gated and neurotransmitter-gated channels, cytoplasmic enzymes, and transcription factors. Dopamine receptor plays an important role in daily life.

MCE designs a unique collection of 267 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0927

(-)-Isocorypalmine Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine	Alkaloids Structural Classification Monophenols other families Classification of Application Fields Other Diseases Phenols Plants Isoquinoline Alkaloids Disease Research Fields Source Classification	Dopamine Receptor
(-)-Isocorypalmine (Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine) is a **dopamine receptor** ligand and modulator capable of crossing the blood-brain barrier. (-)-Isocorypalmine exhibits receptor selectivity, acting as a partial agonist of dopamine D1 and D5 receptors (coupled via Gs proteins), as well as an antagonist of D2, D3 and D4 receptors (by blocking Gi protein-mediated signaling). (-)-Isocorypalmine shows no significant binding to various non-dopamine receptors, ion channels and transporters. (-)-Isocorypalmine is metabolically stable in vivo, effectively inhibits spontaneous and cocaine-induced hyperlocomotion, sensitization and conditioned place preference in mice, and does not induce addictive place preference when administered alone. (-)-Isocorypalmine can be used in addiction research .

Cat. No.	Product Name	Chemical Structure

HY-12987S

Pimozide-d4
Pimozide-d₄ is a deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with K_is of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a K_i of 39 nM; Pimozide also inhibits STAT3 and STAT5 .

HY-15394S

(Rac)-Rotigotine-d7 (hydrochloride)
(Rac)-Rotigotine-d₇ (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

(Rac)-Rotigotine-d7 (hydrochloride)

(Rac)-Rotigotine-d₇ (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-A0007S

Rotigotine-d7 hydrochloride
Rotigotine-d₇ (N-0923-d₇) hydrochloride is the deuterium labeled Rotigotine(HY-75502). Rotigotine is a potent dopamine receptor agonist with K_i values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.

Rotigotine-d7 hydrochloride

Rotigotine-d₇ (N-0923-d₇) hydrochloride is the deuterium labeled Rotigotine(HY-75502). Rotigotine is a potent dopamine receptor agonist with K_i values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.

HY-103414S

Raclopride-d5 hydrochloride
Raclopride-d₅ hydrochloride is the deuterium labeled Raclopride. Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (K_is) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively .

HY-15394S1

(Rac)-Rotigotine-d3 hydrochloride
(Rac)-Rotigotine-d₃ hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of **dopamine receptor*, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine* D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

(Rac)-Rotigotine-d3 hydrochloride

(Rac)-Rotigotine-d₃ hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with K_is of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-12987S2

Pimozide-d4-1
Pimozide-d₄-1 is the deuterium labeled Pimozide. Pimozide is a dopamine receptor antagonist, with K_is of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a K_i of 39 nM; Pimozide also inhibits STAT3 and STAT5 .

HY-W748758

(Z)-Thiothixene-d8
(Z)-Thiothixene-d₈ (NSC 108165-d₈; Navan-d₈; Navane-d₈) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

(Z)-Thiothixene-d8

(Z)-Thiothixene-d₈ (NSC 108165-d₈; Navan-d₈; Navane-d₈) is the deuterium labeled Thiothixene (HY-A0139). Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.

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