presynaptic receptor

By Targets:	5-HT Receptor (4) Adenosine Receptor (1) Dopamine Receptor (2) Dopamine Transporter (2) GABA Receptor (7) Isotope-Labeled Compounds (1) mGluR (1) nAChR (2) Neuropeptide Y Receptor (1)
By Research Areas:	Neurological Disease (17)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-124501

LY 165163 p-NH2-PE-TFMPP	5-HT Receptor	Neurological Disease
LY 165163 is a potent 5-HT presynaptic receptor agonist. LY 165163 significantly decreases 5-HTP accumulation and increases DOPA accumulation in the cortex and striatum .

HY-19733

Lumateperone tosylate ITI-007 tosylate	5-HT Receptor Dopamine Receptor	Neurological Disease
Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia .

HY-P10148

N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) Ac-[Leu28,31]-NPY (24-36)	Neuropeptide Y Receptor	Neurological Disease
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) attenuates cardiac vagal action in anaesthetised rats .

HY-101226

MSOP

MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent K_D of 51 μM for the L-AP4-sensitive presynaptic mGluR.
HY-116495

(-)-OSU6162

PNU-96391
Dopamine Receptor Neurological Disease

(-)-OSU6162 (PNU-96391) is a presynaptic dopamine receptor antagonist .

MSOP
MSOP is a selective group III metabotropic glutamate receptor antagonist with apparent K_D of 51 μM for the L-AP4-sensitive presynaptic mGluR.

(-)-OSU6162 PNU-96391	Dopamine Receptor	Neurological Disease
(-)-OSU6162 (PNU-96391) is a presynaptic dopamine receptor antagonist .

HY-103518

CGP36216	GABA Receptor	Neurological Disease
CGP36216 is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a K_i value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .

HY-103518A

CGP36216 hydrochloride	GABA Receptor	Neurological Disease
CGP36216 hydrochloride is a selective antagonist at GABA presynaptic receptor. CGP36216 binds to GABAB receptor with a K_i value of 0.3 μM. CGP36216 hydrochloride can be used for research of anxiety and trauma-related disorders .

HY-117575A

WAY-100135 dihydrochloride	5-HT Receptor	Neurological Disease
WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT_1A receptor, with an IC₅₀ of 34 nM at the rat hippocampal 5-HT_1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties .

HY-17637

Lumateperone ITI-007
Lumateperone (ITI-007) is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia .

HY-B0979

Lobeline hydrochloride α-Lobeline hydrochloride; L-Lobeline hydrochloride	nAChR Dopamine Transporter	Neurological Disease
Lobeline (α-Lobeline) hydrochloride is a brain-penetrant nicotinic receptor agonist. Lobeline hydrochloride increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline hydrochloride is effective in smoking cessation .

HY-B1423

Lobeline α-Lobeline; L-Lobeline
Lobeline (α-Lobeline) is a brain-penetrant nicotinic receptor agonist. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline is effective in smoking cessation .

HY-116076

S-15535	5-HT Receptor	Neurological Disease
S-15535 is a highly selective 5-HT_1A receptor ligand. S-15535 is an antagonist of postsynaptic 5-HT_1A receptors and an agonist of presynaptic 5-HT_1A receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety .

HY-128420

Lobeline sulfate α-Lobeline sulfate; L-Lobeline sulfate	nAChR Dopamine Transporter	Neurological Disease
Lobeline (α-Lobeline) sulfate is a brain-penetrant nicotinic receptor agonist. Lobeline sulfate increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline sulfate is effective in smoking cessation .

HY-B0007

Baclofen 4 Publications Verification	GABA Receptor	Neurological Disease
Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic *GABA_B receptor* (GABA_BR)** agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

HY-B0007C

Baclofen hydrochloride	GABA Receptor	Neurological Disease
Baclofen hydrochloride, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic *GABA_B receptor* (GABA_BR)** agonist. Baclofen hydrochloride mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen hydrochloride has high blood brain barrier penetrance. Baclofen hydrochloride has the potential for muscle spasticity research .

HY-110146

XAP044	mGluR	Neurological Disease
XAP044 is a potent and selective antagonist of mGlu7. The metabotropic glutamate receptor subtype 7 (mGlu7) is an important presynaptic regulator of neurotransmission in the mammalian CNS. XAP044 demonstrates good brain exposure and wide spectrum anti-stress and antidepressant- and anxiolytic-like efficacy in rodent behavioral paradigms .

HY-B0007S

Baclofen-d4	GABA Receptor	Neurological Disease
Baclofen-d₄ is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].

HY-B0007R

Baclofen (Standard)	GABA Receptor	Neurological Disease
Baclofen (Standard) is the analytical standard of Baclofen. This product is intended for research and analytical applications. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic *GABA_B receptor* (GABA_BR)** agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

HY-B0007S2

Baclofen-d5 hydrochloride	GABA Receptor Isotope-Labeled Compounds	Neurological Disease
Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic *GABA_B receptor* (GABA_BR)** agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

HY-10965

Rolofylline KW-3902	Adenosine Receptor	Neurological Disease
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment. Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP₄₅₀) . Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases .

Cat. No.	Product Name

HY-L165

Dopamine Receptor Compound Library	199 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 199 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.

Dopamine Receptor Compound Library

199 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 199 small molecules related to dopamine receptor. It is a good tool for screening drugs from nervous system disease.

Cat. No.	Product Name	Target	Research Area

HY-P10148

N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) Ac-[Leu28,31]-NPY (24-36)	Neuropeptide Y Receptor	Neurological Disease
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) attenuates cardiac vagal action in anaesthetised rats .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0979

Lobeline hydrochloride α-Lobeline hydrochloride; L-Lobeline hydrochloride	Alkaloids Structural Classification Source classification Campanulaceae Pyridine Alkaloids Plants Lobelia chinensis Lour.	nAChR Dopamine Transporter
Lobeline (α-Lobeline) hydrochloride is a brain-penetrant nicotinic receptor agonist. Lobeline hydrochloride increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline hydrochloride is effective in smoking cessation .

HY-128420

Lobeline sulfate α-Lobeline sulfate; L-Lobeline sulfate	Alkaloids Structural Classification other families Source classification Pyridine Alkaloids Plants Endogenous metabolite	nAChR Dopamine Transporter
Lobeline (α-Lobeline) sulfate is a brain-penetrant nicotinic receptor agonist. Lobeline sulfate increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline sulfate is effective in smoking cessation .

Cat. No.	Product Name	Chemical Structure

HY-B0007S

Baclofen-d4
Baclofen-d₄ is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].

Baclofen-d4

Baclofen-d₄ is the deuterium labeled Baclofen. Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABAB receptor (GABABR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABAB receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research[1][2][3].

HY-B0007S2

Baclofen-d5 hydrochloride
Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic *GABA_B receptor* (GABA_BR)** agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

Baclofen-d5 hydrochloride

Baclofen-d₅ hydrochloride is deuterated labeled Baclofen (HY-B0007). Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropic GABA_B receptor (GABA_BR) agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_B receptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research .

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