CNS toxicity

By Targets:	5-HT Receptor (1) Amyloid-β (1) Bacterial (1) CXCR (1) DNA/RNA Synthesis (2) Ferroptosis (2) Microtubule/Tubulin (1) Parasite (1) PGE synthase (1) Sodium Channel (2)
By Research Areas:	Cancer (4) Cardiovascular Disease (1) Infection (2) Inflammation/Immunology (1) Neurological Disease (7)

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-119974

Caracemide NSC-253272	DNA/RNA Synthesis Bacterial	Infection Cancer
Caracemide (NSC-253272) inhibits the enzyme ribonucleotide reductase of Escherichia coli. Caracemide is a novel anticancer agent derived from a hydroxamic acid and has demonstrated to produce severe central nervous system (CNS) toxicity .

HY-14905

Uridine triacetate Tri-O-acetyl uridine	Others	Neurological Disease
Uridine triacetate (Tri-O-acetyl uridine) is an orally active proagent of Uridine (HY-B1449). Uridine triacetate is quickly absorbed in the gut, and is rapidly deacetylated in the circulation to yield free uridine. Uridine triacetate is used for the research of 5-fluorouracil (5-FU) and capecitabine toxicity, or early-onset cardiac or central nervous system (CNS) .

HY-B0653A

Levobupivacaine hydrochloride 2 Publications Verification (S)-(-)-Bupivacaine monohydrochloride	Sodium Channel Ferroptosis	Cardiovascular Disease Neurological Disease Cancer
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .

HY-107790

5-Methoxyflavone	DNA/RNA Synthesis	Neurological Disease
5-Methoxyflavone, belonged to Flavonoid family, is a DNA polymerase-beta inhibitor and neuroprotective agent against beta-amyloid toxicity. possess central nervous system (CNS) depressant effect mediated through the ionotropic GABA_A receptors.

HY-B0770

Artemotil β-Arteether; (+)-Arteether; Arteether	CXCR Parasite	Infection Cancer
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant *Plasmodium falciparum* malaria with an IC₅₀ of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .

HY-105066

Davunetide 1 Publications Verification	Microtubule/Tubulin Amyloid-β	Neurological Disease
Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity .

HY-B0653

Levobupivacaine (S)-(-)-Bupivacaine	Sodium Channel Ferroptosis	Neurological Disease Cancer
Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .

HY-15344A

(S,S)-Ketone monoester	Others	Neurological Disease
(S,S)-Ketone monoester is a (S,S)-enantiomer of Ketone monoester (HY-15344). Ketone monoester elevates the AcAc and acetone levels, thereby produces sustained ketosis and significantly delays central nervous system oxygen toxicity (CNS-OT) seizures .

HY-167893

AGH-107	5-HT Receptor	Neurological Disease
AGH-107 is a high selective and brain-penetrant agonist of 5-HT7 receptor, with a K_i of 6 nM and EC₅₀ of 19 nM. AGH-107 exhibits high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures .

HY-146662

HPGDS inhibitor 3	PGE synthase	Inflammation/Immunology
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC₅₀ value of 9.4 nM and EC₅₀ of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity .

Cat. No.	Product Name

HY-L0124V

Chemspace CNS-Focused Library	13,082 compounds
The basic requirements for the compounds that are supposed to penetrate the blood-brain barrier are somewhat different from those for the majority of drug discovery projects. Alongside the known problem with delivery of the large and non-polar compounds and their penetrability through the cell membrane, the other issue arises as well: small and polar compounds are not able to pass the Blood-Brain Barrier. Chemspace CNS-focused library comprises quite small, non-polar compounds that are also free from PAINS/toxic fragments and aggregators.

Chemspace CNS-Focused Library

13,082 compounds

The basic requirements for the compounds that are supposed to penetrate the blood-brain barrier are somewhat different from those for the majority of drug discovery projects. Alongside the known problem with delivery of the large and non-polar compounds and their penetrability through the cell membrane, the other issue arises as well: small and polar compounds are not able to pass the Blood-Brain Barrier. Chemspace CNS-focused library comprises quite small, non-polar compounds that are also free from PAINS/toxic fragments and aggregators.

Cat. No.	Product Name	Target	Research Area

HY-105066

Davunetide 1 Publications Verification	Microtubule/Tubulin Amyloid-β	Neurological Disease
Davunetide is an eight amino acid snippet derived from activity-dependent neuroprotective protein (ADNP), a neurotrophic factor that exists in the mammalian CNS. Davunetide possesses neuroprotective, neurotrophic and cognitive protective roperties. Davunetide, a microtubule-stabilizing peptide, interacts with and stabilises neuron-specific βIII-tubulin in vitro. Davunetide penetrates the blood-brain barrier and is non-toxic. Davunetide inhibits Aβ aggregation and Aβ-induced neurotoxicity .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B0770

Artemotil β-Arteether; (+)-Arteether; Arteether	Structural Classification Natural Products Classification of Application Fields Source classification Artemisia carvifolia Buch.-Ham. ex Roxb. Plants Compositae Disease Research Fields Cancer	CXCR Parasite
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant *Plasmodium falciparum* malaria with an IC₅₀ of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .

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