GABA Receptor Ligand

Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC₅₀ of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC₅₀ of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.

Difludiazepam (Ro 07-4065), a benzodiazepine derivative, is a GABAA receptor ligand with an IC₅₀ of 4.1 nM. Difludiazepam binds to an allosteric site on the GABAA receptor to potentiate the receptor's response to GABA, reducing neuron excitability. Difludiazepam contains halogenated groups at the ortho position of its phenyl ring.

K1 peptide TFA is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP).

Chlormadinone acetate is a progestogen with potent progestogenic activity and antiandrogenic effects. Chlormadinone acetate acts on glucocorticoid receptor, progesterone receptor, androgen receptor, and GABA_A receptor. Chlormadinone acetate induces endometrial proliferation in estrogen-pretreated rabbits, inhibits testosterone-stimulated growth of the prostate and seminal vesicles in castrated rats, and reduces the thymus and adrenal weights in juvenile rats. Chlormadinone acetate is applicable to research related to diseases such as depression and reproductive metabolic disorders.

4''-Oxoavermectin B1a is a potentiator targeting GABA (γ-aminobutyric acid) and glutamate-gated chloride channels with insecticidal and acaricidal activities. 4''-Oxoavermectin B1a is promising for research of agricultural pests.

Bentazepam (Thiadipone) is a compound with short-action anxiolytic effect. Bentazepam shows anticonvulsant and sedative properties. Bentazepam can be used for the research of depressive disorder and anxiety.

GATT-44 is a blood-brain barrier-permeable, selective GABA transporter 1 (GAT-1) ligand with an IC₅₀ of 126 nM. GATT-44 shows selectivity for GAT-2, GAT-3 and BGT-1 subtypes, and undergoes copper-mediated ¹⁸F-radiofluorination. The radiolabeled GATT-44 ([¹⁸F]GATT-44) exhibits brain uptake, metabolic stability and high GAT-1 binding specificity in non-human primates. GATT-44 is applicable for research on neurodegenerative and neuropsychiatric diseases.

Ro 22-8515 is a ligand of Benzodiazepine receptor.

Nitrazolam is a benzodiazepine compound, that may exhibit CNS depressant properties as traditional benzodiazepines, including sedation, hypnosis, anxiolysis, and anticonvulsant effects, by acting on GABA receptors.

SSR180575 is a specific and potent peripheral benzodiazepine receptor ligand. SSR180575 irreversibly and specifically binds with high affinity on rat heart mitochondria (K_d = 1.95 nM). SSR180575 can be used in the research of cardiovascular diseases.

K1 peptide is a high-affinity peptide ligand for GABAA receptor-associated protein (GABARAP).

Leporin A is an insecticide. Leporin A binds to GABA receptors or sodium channels to disrupt neurotransmission.

AHN 070 is an irreversible peripheral benzodiazepine receptor (PBR) ligand. AHN 070 can bind to PBR with nanomolar affinity and is pH-dependent. AHN 070 can be used for studying the structure and function of PBR.

GABA-A Receptor Ligand-1 (Compound 4) is a ligand for GABA-A receptor with a pK_i of 7.27. GABA-A Receptor Ligand-1 reduces mitochondrial dysfunction, promotes neurite outgrowth and neuronal regeneration. GABA-A Receptor Ligand-1 exhibits neuroprotective efficacy in rats ischemic stroke models.

CGS-17867A hydrochloride is a benzodiazepine receptor ligand. CGS-17867A hydrochloride has a weak sedative effect and can increase palatable food intake.

Ciclotizolam (WE-973) is a thienotriazolodiazepine with anticonvulsant and anti-aggressive activities. Ciclotizolam binds to benzodiazepine receptors in the central nervous system. Ciclotizolam decreases total sleep time in cats.