Target type: cellularcomponent
A synapse in which an action potential in the presynaptic cell reduces the probability of an action potential occurring in the postsynaptic cell. [GOC:dph, GOC:ef]
Inhibitory synapses are specialized junctions between neurons that transmit inhibitory signals, preventing or reducing the likelihood of the postsynaptic neuron firing an action potential. These synapses are characterized by the release of neurotransmitters that bind to receptors on the postsynaptic neuron, opening ion channels that allow the flow of ions that hyperpolarize the cell, making it less likely to fire.
The cellular component of an inhibitory synapse can be broadly divided into the presynaptic terminal, the synaptic cleft, and the postsynaptic density.
**Presynaptic Terminal:**
* **Synaptic Vesicles:** Small, membrane-bound sacs that store and release neurotransmitters. They contain inhibitory neurotransmitters like GABA, glycine, or others depending on the synapse.
* **Active Zone:** Specialized region of the presynaptic membrane where synaptic vesicles fuse and release neurotransmitters.
* **Calcium Channels:** Voltage-gated calcium channels located near the active zone. When an action potential arrives at the presynaptic terminal, it opens these channels, allowing calcium ions to flow into the terminal. Calcium influx triggers the fusion of synaptic vesicles with the presynaptic membrane and the release of neurotransmitters into the synaptic cleft.
* **Mitochondria:** Provide energy for the synthesis and recycling of neurotransmitters, as well as other cellular processes.
**Synaptic Cleft:**
* **Extracellular Matrix:** A gel-like substance that fills the space between the presynaptic and postsynaptic membranes. It provides structural support and helps to regulate the diffusion of neurotransmitters.
**Postsynaptic Density:**
* **Receptors:** Specialized proteins embedded in the postsynaptic membrane that bind to neurotransmitters. Inhibitory synapses typically have receptors for GABA, glycine, or other inhibitory neurotransmitters.
* **Ion Channels:** These channels are linked to the receptors and open when a neurotransmitter binds. In inhibitory synapses, these channels allow the flow of ions like chloride (Cl-) or potassium (K+), leading to hyperpolarization of the postsynaptic neuron.
* **Scaffolding Proteins:** These proteins help to organize the receptors, ion channels, and other components of the postsynaptic density, ensuring proper function of the synapse.
* **Signaling Molecules:** Various signaling molecules, including kinases and phosphatases, are present in the postsynaptic density. These molecules are involved in regulating the strength and plasticity of the inhibitory synapse.
The precise composition and organization of the cellular components of inhibitory synapses vary depending on the type of synapse, the neurons involved, and the specific neurotransmitters used. However, the general principles of presynaptic neurotransmitter release, diffusion across the synaptic cleft, and postsynaptic receptor activation and signaling are common to all inhibitory synapses.
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| Protein | Definition | Taxonomy |
|---|---|---|
| Gamma-aminobutyric acid receptor subunit alpha-2 | A gamma-aminobutyric acid receptor subunit alpha-2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P47869] | Homo sapiens (human) |
| Glycine receptor subunit alpha-1 | A glycine receptor subunit alpha-1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P23415] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| gamma-aminobutyric acid | gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4. gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system. | amino acid zwitterion; gamma-amino acid; monocarboxylic acid | human metabolite; neurotransmitter; Saccharomyces cerevisiae metabolite; signalling molecule |
| glycine | alpha-amino acid; amino acid zwitterion; proteinogenic amino acid; serine family amino acid | EC 2.1.2.1 (glycine hydroxymethyltransferase) inhibitor; fundamental metabolite; hepatoprotective agent; micronutrient; neurotransmitter; NMDA receptor agonist; nutraceutical | |
| phenytoin | imidazolidine-2,4-dione | anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent | |
| alprazolam | alprazolam : A member of the class of triazolobenzodiazepines that is 4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepine carrying methyl, phenyl and chloro substituents at positions 1, 6 and 8 respectively. Alprazolam is only found in individuals that have taken this drug. Alprazolam: A triazolobenzodiazepine compound with antianxiety and sedative-hypnotic actions, that is efficacious in the treatment of PANIC DISORDERS, with or without AGORAPHOBIA, and in generalized ANXIETY DISORDERS. (From AMA Drug Evaluations Annual, 1994, p238) | organochlorine compound; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA agonist; muscle relaxant; sedative; xenobiotic |
| astemizole | astemizole : A piperidine compound having a 2-(4-methoxyphenyl)ethyl group at the 1-position and an N-[(4-fluorobenzyl)benzimidazol-2-yl]amino group at the 4-position. Astemizole: Antihistamine drug now withdrawn from the market in many countries because of rare but potentially fatal side effects. | benzimidazoles; piperidines | anti-allergic agent; anticoronaviral agent; H1-receptor antagonist |
| chlordiazepoxide | chlordiazepoxide : A benzodiazepine that is 3H-1,4-benzodiazepine 4-oxide substituted by a chloro group at position 7, a phenyl group at position 5 and a methylamino group at position 2. Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal. | benzodiazepine | |
| clonazepam | clonazepam : 1,3-Dihydro-2H-1,4-benzodiazepin-2-one in which the hydrogens at positions 5 and 7 are substituted by 2-chlorophenyl and nitro groups, respectively. It is used in the treatment of all types of epilepsy and seizures, as well as myoclonus and associated abnormal movements, and panic disorders. However, its use can be limited by the development of tolerance and by sedation. Clonazepam: An anticonvulsant used for several types of seizures, including myotonic or atonic seizures, photosensitive epilepsy, and absence seizures, although tolerance may develop. It is seldom effective in generalized tonic-clonic or partial seizures. The mechanism of action appears to involve the enhancement of GAMMA-AMINOBUTYRIC ACID receptor responses. | 1,4-benzodiazepinone; monochlorobenzenes | anticonvulsant; anxiolytic drug; GABA modulator |
| nordazepam | nordazepam : A 1,4-benzodiazepinone having phenyl and chloro substituents at positions 5 and 7 respectively; it has anticonvulsant, anxiolytic, muscle relaxant and sedative properties but is used primarily in the treatment of anxiety. Nordazepam: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam. | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; GABA modulator; human metabolite; sedative |
| diazepam | diazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a methyl group at position 1 and a phenyl group at position 5. Diazepam: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic |
| fipronil | 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-4-[(trifluoromethyl)sulfinyl]-1H-pyrazole-3-carbonitrile : A member of the class of pyrazoles that is 1H-pyrazole that is substituted at positions 1, 3, 4, and 5 by 2,6-dichloro-4-(trifluoromethyl)phenyl, cyano, (trifluoromethyl)sulfinyl, and amino groups, respectively. fipronil : A racemate comprising equimolar amounts of (R)- and (S)-fipronil. fipronil: has low mammalian toxicity; structure given in first source | (trifluoromethyl)benzenes; dichlorobenzene; nitrile; primary amino compound; pyrazoles; sulfoxide | |
| flumazenil | flumazenil : An organic heterotricyclic compound that is 5,6-dihydro-4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted at positions 3, 5, 6, and 8 by ethoxycarbonyl, methyl, oxo, and fluoro groups, respectively. It is used as an antidote to benzodiazepine overdose. Flumazenil: A potent benzodiazepine receptor antagonist. Since it reverses the sedative and other actions of benzodiazepines, it has been suggested as an antidote to benzodiazepine overdoses. | ethyl ester; imidazobenzodiazepine; organofluorine compound | antidote to benzodiazepine poisoning; GABA antagonist |
| flunitrazepam | flunitrazepam : A 1,4-benzodiazepinone that is nitrazepam substituted by a methyl group at position 1 and by a fluoro group at position 2'. It is a potent hypnotic, sedative, and amnestic drug used to treat chronic insomnia. Flunitrazepam: A benzodiazepine with pharmacologic actions similar to those of DIAZEPAM that can cause ANTEROGRADE AMNESIA. Some reports indicate that it is used as a date rape drug and suggest that it may precipitate violent behavior. The United States Government has banned the importation of this drug. | 1,4-benzodiazepinone; C-nitro compound; monofluorobenzenes | anxiolytic drug; GABAA receptor agonist; sedative |
| fluoxetine | fluoxetine : A racemate comprising equimolar amounts of (R)- and (S)-fluoxetine. A selective serotonin reuptake inhibitor (SSRI), it is used (generally as the hydrochloride salt) for the treatment of depression (and the depressive phase of bipolar disorder), bullimia nervosa, and obsessive-compulsive disorder. Fluoxetine: The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants. N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine : An aromatic ether consisting of 4-trifluoromethylphenol in which the hydrogen of the phenolic hydroxy group is replaced by a 3-(methylamino)-1-phenylpropyl group. | (trifluoromethyl)benzenes; aromatic ether; secondary amino compound | |
| fluspirilene | Fluspirilene: A long-acting injectable antipsychotic agent used for chronic schizophrenia. | diarylmethane | |
| hydroxyurea | one-carbon compound; ureas | antimetabolite; antimitotic; antineoplastic agent; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; genotoxin; immunomodulator; radical scavenger; teratogenic agent | |
| isoguvacine | isoguvacine: A GABA agonist; RN given refers to parent cpd; structure | tetrahydropyridine | |
| 4-piperidinecarboxylic acid | 4-piperidinecarboxylic acid: structure in first source | ||
| kynurenic acid | kynurenic acid : A quinolinemonocarboxylic acid that is quinoline-2-carboxylic acid substituted by a hydroxy group at C-4. Kynurenic Acid: A broad-spectrum excitatory amino acid antagonist used as a research tool. | monohydroxyquinoline; quinolinemonocarboxylic acid | G-protein-coupled receptor agonist; human metabolite; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist; Saccharomyces cerevisiae metabolite |
| mefloquine hydrochloride | [2,8-bis(trifluoromethyl)quinolin-4-yl]-(2-piperidyl)methanol : An organofluorine compound that consists of quinoline bearing trifluoromethyl substituents at positions 2 and 8 as well as a (2-piperidinyl)hydroxymethyl substituent at position 4. | organofluorine compound; piperidines; quinolines; secondary alcohol | |
| muscimol | muscimol : A member of the class of isoxazoles that is 1,2-oxazol-3(2H)-one substituted by an aminomethyl group at position 5. It has been isolated from mushrooms of the genus Amanita. Muscimol: A neurotoxic isoxazole isolated from species of AMANITA. It is obtained by decarboxylation of IBOTENIC ACID. Muscimol is a potent agonist of GABA-A RECEPTORS and is used mainly as an experimental tool in animal and tissue studies. | alkaloid; isoxazoles; primary amino compound | fungal metabolite; GABA agonist; oneirogen; psychotropic drug |
| nitrazepam | nitrazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one which is substituted at positions 5 and 7 by phenyl and nitro groups, respectively. It is used as a hypnotic for the short-term management of insomnia and for the treatment of epileptic spasms in infants (West's syndrome). Nitrazepam: A benzodiazepine derivative used as an anticonvulsant and hypnotic. | 1,4-benzodiazepinone; C-nitro compound | anticonvulsant; antispasmodic drug; drug metabolite; GABA modulator; sedative |
| cm 7116 | norflutoprazepam: structure | benzodiazepine | |
| pentobarbital | pentobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and sec-pentyl groups. Pentobarbital: A short-acting barbiturate that is effective as a sedative and hypnotic (but not as an anti-anxiety) agent and is usually given orally. It is prescribed more frequently for sleep induction than for sedation but, like similar agents, may lose its effectiveness by the second week of continued administration. (From AMA Drug Evaluations Annual, 1994, p236) | barbiturates | GABAA receptor agonist |
| piperidine-4-sulfonic acid | piperidine-4-sulfonic acid: specific GABA agonist | ||
| propofol | propofol : A phenol resulting from the formal substitution of the hydrogen at the 2 position of 1,3-diisopropylbenzene by a hydroxy group. Propofol: An intravenous anesthetic agent which has the advantage of a very rapid onset after infusion or bolus injection plus a very short recovery period of a couple of minutes. (From Smith and Reynard, Textbook of Pharmacology, 1992, 1st ed, p206). Propofol has been used as ANTICONVULSANTS and ANTIEMETICS. | phenols | anticonvulsant; antiemetic; intravenous anaesthetic; radical scavenger; sedative |
| risperidone | risperidone : A member of the class of pyridopyrimidines that is 2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one carrying an additional 2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl group at position 2. Risperidone: A selective blocker of DOPAMINE D2 RECEPTORS and SEROTONIN 5-HT2 RECEPTORS that acts as an atypical antipsychotic agent. It has been shown to improve both positive and negative symptoms in the treatment of SCHIZOPHRENIA. | 1,2-benzoxazoles; heteroarylpiperidine; organofluorine compound; pyridopyrimidine | alpha-adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; psychotropic drug; second generation antipsychotic; serotonergic antagonist |
| ro 15-4513 | Ro 15-4513: a partial inverse agonist of benzodiazepine receptors | organic heterotricyclic compound; organonitrogen heterocyclic compound | |
| temazepam | Temazepam: A benzodiazepine that acts as a GAMMA-AMINOBUTYRIC ACID modulator and anti-anxiety agent. | benzodiazepine | |
| (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid | (1,2,5,6-tetrahydropyridin-4-yl)methylphosphinic acid: a GABA-C receptor antagonist; structure in first source | ||
| triazolam | Triazolam: A short-acting benzodiazepine used in the treatment of insomnia. Some countries temporarily withdrew triazolam from the market because of concerns about adverse reactions, mostly psychological, associated with higher dose ranges. Its use at lower doses with appropriate care and labeling has been reaffirmed by the FDA and most other countries. | triazolobenzodiazepine | sedative |
| zaleplon | zaleplon : A pyrazolo[1,5-a]pyrimidine having a nitrile group at position 3 and a 3-(N-ethylacetamido)phenyl substituent at the 7-position. zaleplon: an azabicyclo(4.3.0)nonane; a nonbenzodiazepine; one of the so-called of Z drugs (zopiclone, eszopiclone, zolpidem, and zaleplon) for which there is some correlation with tumors; a hypnotic with less marked effect on psychomotor functions compared to lorazepam | nitrile; pyrazolopyrimidine | anticonvulsant; anxiolytic drug; central nervous system depressant; sedative |
| zolpidem | zolpidem : An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position. Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA. | imidazopyridine | central nervous system depressant; GABA agonist; sedative |
| triiodothyronine | 3,3',5-triiodo-L-thyronine : An iodothyronine compound having iodo substituents at the 3-, 3'- and 5-positions. Although some is produced in the thyroid, most of the 3,3',5-triiodo-L-thyronine in the body is generated by mono-deiodination of L-thyroxine in the peripheral tissues. Its metabolic activity is about 3 to 5 times that of L-thyroxine. The sodium salt is used in the treatment of hypothyroidism. Triiodothyronine: A T3 thyroid hormone normally synthesized and secreted by the thyroid gland in much smaller quantities than thyroxine (T4). Most T3 is derived from peripheral monodeiodination of T4 at the 5' position of the outer ring of the iodothyronine nucleus. The hormone finally delivered and used by the tissues is mainly T3. | 2-halophenol; amino acid zwitterion; iodophenol; iodothyronine | human metabolite; mouse metabolite; thyroid hormone |
| bicuculline | bicuculline : A benzylisoquinoline alkaloid that is 6-methyl-5,6,7,8-tetrahydro[1,3]dioxolo[4,5-g]isoquinoline which is substituted at the 5-pro-S position by a (6R)-8-oxo-6,8-dihydrofuro[3,4-e][1,3]benzodioxol-6-yl group. A light-sensitive competitive antagonist of GABAA receptors. It was originally identified in 1932 in plant alkaloid extracts and has been isolated from Dicentra cucullaria, Adlumia fungosa, Fumariaceae, and several Corydalis species. Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors. | benzylisoquinoline alkaloid; isoquinoline alkaloid; isoquinolines | agrochemical; central nervous system stimulant; GABA-gated chloride channel antagonist; GABAA receptor antagonist; neurotoxin |
| flavone | flavone : The simplest member of the class of flavones that consists of 4H-chromen-4-one bearing a phenyl substituent at position 2. flavone: RN given refers to unlabeled cpd; structure given in first source | flavones | metabolite; nematicide |
| dronabinol | Delta(9)-tetrahydrocannabinol : A diterpenoid that is 6a,7,8,10a-tetrahydro-6H-benzo[c]chromene substituted at position 1 by a hydroxy group, positions 6, 6 and 9 by methyl groups and at position 3 by a pentyl group. The principal psychoactive constituent of the cannabis plant, it is used for treatment of anorexia associated with AIDS as well as nausea and vomiting associated with cancer chemotherapy. Dronabinol: A psychoactive compound extracted from the resin of Cannabis sativa (marihuana, hashish). The isomer delta-9-tetrahydrocannabinol (THC) is considered the most active form, producing characteristic mood and perceptual changes associated with this compound. | benzochromene; diterpenoid; phytocannabinoid; polyketide | cannabinoid receptor agonist; epitope; hallucinogen; metabolite; non-narcotic analgesic |
| pimozide | pimozide : A member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which one of the nitrogens is substituted by a piperidin-4-yl group, which in turn is substituted on the nitrogen by a 4,4-bis(p-fluorophenyl)butyl group. Pimozide: A diphenylbutylpiperidine that is effective as an antipsychotic agent and as an alternative to HALOPERIDOL for the suppression of vocal and motor tics in patients with Tourette syndrome. Although the precise mechanism of action is unknown, blockade of postsynaptic dopamine receptors has been postulated. (From AMA Drug Evaluations Annual, 1994, p403) | benzimidazoles; heteroarylpiperidine; organofluorine compound | antidyskinesia agent; dopaminergic antagonist; first generation antipsychotic; H1-receptor antagonist; serotonergic antagonist |
| chlordesmethyldiazepam | benzodiazepine | ||
| 6-aminonicotinic acid | 6-aminonicotinic acid : An aminonicotinic acid in which the amino group is situated at position 6 of the pyridine ring. 6-aminonicotinic acid: RN given refers to parent cpd | aminonicotinic acid; aminopyridine; aromatic amine | metabolite |
| halazepam | halazepam: structure | organic molecular entity | |
| phenazepam | |||
| progabide | progabide: GABA agonist; structure | diarylmethane | |
| adapalene | adapalene : A naphthoic acid that is CD437 in which the phenolic hydroxy group has been converted to its methyl ether. Adapalene: A naphthalene derivative that has specificity for RETINOIC ACID RECEPTORS. It is used as a DERMATOLOGIC AGENT for the treatment of ACNE. | adamantanes; monocarboxylic acid; naphthoic acid | dermatologic drug; EC 2.7.11.22 (cyclin-dependent kinase) inhibitor; non-steroidal anti-inflammatory drug |
| duloxetine | duloxetine | ||
| norharman | beta-carboline : The parent compound of the beta-carbolines, a tricyclic structure comprising an indole ring system ortho- fused to C-3 and C-4 of a pyridine ring. norharman: RN given refers to parent cpd | beta-carbolines; mancude organic heterotricyclic parent | fungal metabolite; marine metabolite |
| baicalin | dihydroxyflavone; glucosiduronic acid; glycosyloxyflavone; monosaccharide derivative | antiatherosclerotic agent; antibacterial agent; anticoronaviral agent; antineoplastic agent; antioxidant; cardioprotective agent; EC 2.7.7.48 (RNA-directed RNA polymerase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; ferroptosis inhibitor; neuroprotective agent; non-steroidal anti-inflammatory drug; plant metabolite; prodrug | |
| abecarnil | |||
| telmisartan | telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension. Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION. | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| honokiol | biphenyls | ||
| 2-aminonicotinic acid | 2-aminonicotinic acid : An aminonicotinic acid in which the amino group is situated at position 2 of the pyridine ring. 2-aminonicotinic acid: structure in first source aminonicotinic acid : An aromatic amino acid that is nicotinic acid in which one of the hydrogens attached to the pyridine ring is replaced by an amino group. A 'closed class'. | aminonicotinic acid; aminopyridine | metabolite |
| n-desmethylflunitrazepam | |||
| 7-aminonitrazepam | 7-aminonitrazepam: urinary metabolite of nitrazepam | benzodiazepine | |
| ro 20-1815 | 7-aminoflunitrazepam: flunitrazepam metabolite; structure given in first source | benzodiazepine | |
| brexanolone | brexanolone : A 3-hydroxy-5alpha-pregnan-20-one in which the hydroxy group at position 3 has alpha-configuration. It is a metabolite of the sex hormone progesterone and used for the treatment of postpartum depression in women. brexanolone: a mixture of allopregnanolone and sulfobutylether‐beta‐cyclodextrin for treatment of postpartum depression | 3-hydroxy-5alpha-pregnan-20-one | antidepressant; GABA modulator; human metabolite; intravenous anaesthetic; sedative |
| imidazoleacetic acid | imidazol-4-ylacetic acid : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens has been replaced by an imidazol-4-yl group. imidazol-5-ylacetic acid : A monocarboxylic acid that is acetic acid in which one of the methyl hydrogens has been replaced by an imidazol-5-yl group. imidazoleacetic acid: RN given refers to cpd without specific location of acetic acid attachment identified; structure | imidazoles; monocarboxylic acid | metabolite; mouse metabolite |
| 2,5-dihydro-2-(4-methoxyphenyl)-3h-pyrazolo(4,3-c)quinolin-3-one | |||
| alphaxalone | alphaxalone: RN given refers to (3alpha,5alpha)-isomer; structure | corticosteroid hormone | |
| methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate | methyl 6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate: structure given in first source | beta-carbolines | |
| beta-carboline-3-carboxylic acid ethyl ester | beta-carboline-3-carboxylic acid ethyl ester: isolated from brain tissue & urine; extremely potent displacer of diazepam from brain benzodiazepam receptors; structure in first source | beta-carbolines | |
| beta-carboline-3-carboxylic acid methyl ester | beta-carboline-3-carboxylic acid methyl ester: structure given in first source | beta-carbolines | |
| bretazenil | bretazenil: RN given for (S) isomer | ||
| cl 218872 | CL 218872: shows specific action on benzodiazepine receptors; structure | pyridazines; ring assembly | |
| ro 15-3505 | |||
| zk 93426 | ZK 93426: GABA-A receptor antag | beta-carbolines | |
| zk 93423 | beta-carbolines | ||
| 3-ethoxy-beta-carboline | 3-ethoxy-beta-carboline: high affinity benzodiazepine receptor ligand with partial inverse agonist properties | ||
| tert-butyl beta-carboline-3-carboxylate | tert-butyl beta-carboline-3-carboxylate: benzodiazepine receptor antagonist | ||
| ro 14-7437 | Ro 14-7437: benzodiazepine antag; no other info available 8/16/83 | ||
| 3',6-dinitroflavone | |||
| l 663581 | L 663581: structure given in first source; partial agonist at the benzodiazepine receptor | ||
| cgp 36742 | (3-aminopropyl)(n-butyl)phosphinic acid: interacts preferably with GABA-B RECEPTORS (IC50=38 μM) and GABA-C receptors (IC50=62 μM) over GABA-A RECEPTORS (IC50=508 μM) | ||
| pitrazepin | pitrazepin: effects are not tissue specific; induced a bursting discharge pattern in cultures derived from hippocampus & hypothalamus; structure given in first source | N-arylpiperazine | |
| cinacalcet | cinacalcet : A secondary amino compound that is (1R)-1-(naphthalen-1-yl)ethanamine in which one of the hydrogens attached to the nitrogen is substituted by a 3-[3-(trifluoromethyl)phenyl]propyl group. | (trifluoromethyl)benzenes; naphthalenes; secondary amino compound | calcimimetic; P450 inhibitor |
| 7-aminoclonazepam | benzodiazepine | ||
| zg 63 | ZG 63: structure given in first source; a high affinity ligand for diazepam-insensitive benzodiazepine receptors | ||
| ro 5-3438 | Ro 5-3438: structure | ||
| strychnine | strychnine : A monoterpenoid indole alkaloid that is strychnidine bearing a keto substituent at the 10-position. Strychnine: An alkaloid found in the seeds of STRYCHNOS NUX-VOMICA. It is a competitive antagonist at glycine receptors and thus a convulsant. It has been used as an analeptic, in the treatment of nonketotic hyperglycinemia and sleep apnea, and as a rat poison. | monoterpenoid indole alkaloid; organic heteroheptacyclic compound | avicide; cholinergic antagonist; glycine receptor antagonist; neurotransmitter agent; rodenticide |
| cocaine | cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca. Cocaine: An alkaloid ester extracted from the leaves of plants including coca. It is a local anesthetic and vasoconstrictor and is clinically used for that purpose, particularly in the eye, ear, nose, and throat. It also has powerful central nervous system effects similar to the amphetamines and is a drug of abuse. Cocaine, like amphetamines, acts by multiple mechanisms on brain catecholaminergic neurons; the mechanism of its reinforcing effects is thought to involve inhibition of dopamine uptake. | benzoate ester; methyl ester; tertiary amino compound; tropane alkaloid | adrenergic uptake inhibitor; central nervous system stimulant; dopamine uptake inhibitor; environmental contaminant; local anaesthetic; mouse metabolite; plant metabolite; serotonin uptake inhibitor; sodium channel blocker; sympathomimetic agent; vasoconstrictor agent; xenobiotic |
| 6-bromoflavone | 6-bromoflavone: a high affinity ligand for the central benzodiazepine receptors; structure given in first source | ||
| n-desmethylflunitrazepam | N-desmethylflunitrazepam: metabolite of flunitrazepam | ||
| ro 05-4082 | ID 690: methyl deriv of clonazepam; structure | ||
| l 364373 | benzodiazepine | ||
| etomidate | etomidate : The ethyl ester of 1-[(1R)-1-phenylethyl]-1H-imidazole-5-carboxylic acid. It is an intravenous general anaesthetic with no analgesic activity. Etomidate: Imidazole derivative anesthetic and hypnotic with little effect on blood gases, ventilation, or the cardiovascular system. It has been proposed as an induction anesthetic. | ethyl ester; imidazoles | intravenous anaesthetic; sedative |
| eszopiclone | eszopiclone : The (5S)- (active) enantiomer of zopiclone. Unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia, eszopiclone is approved by the U.S. Food and Drug Administration for long-term use. Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA. | zopiclone | central nervous system depressant; sedative |
| sulindac | sulindac : A monocarboxylic acid that is 1-benzylidene-1H-indene which is substituted at positions 2, 3, and 5 by methyl, carboxymethyl, and fluorine respectively, and in which the phenyl group of the benzylidene moiety is substituted at the para position by a methylsulfinyl group. It is a prodrug for the corresponding sulfide, a non-steroidal anti-inflammatory drug, used particularly in the treatment of acute and chronic inflammatory conditions. Sulindac: A sulfinylindene derivative prodrug whose sulfinyl moiety is converted in vivo to an active NSAID analgesic. Specifically, the prodrug is converted by liver enzymes to a sulfide which is excreted in the bile and then reabsorbed from the intestine. This helps to maintain constant blood levels with reduced gastrointestinal side effects. | monocarboxylic acid; organofluorine compound; sulfoxide | analgesic; antineoplastic agent; antipyretic; apoptosis inducer; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; non-narcotic analgesic; non-steroidal anti-inflammatory drug; prodrug; tocolytic agent |
| 1-(1h-indol-3-ylcarbonyl)-n-(4-methoxybenzyl)formamide | 1-(1H-Indol-3-ylcarbonyl)-N-(4-methoxybenzyl)formamide: structure in first source | ||
| 2-[(2-ethoxyphenoxy)-phenylmethyl]morpholine | aromatic ether | ||
| meclonazepam | |||
| isothaz | isothaz: muscimol antagonist | ||
| n-(indol-3-ylglyoxylyl)benzylamine | N-(indol-3-ylglyoxylyl)benzylamine: structure given in first source | ||
| 6-bromo-3'-nitroflavone | 6-bromo-3'-nitroflavone: a synthetic flavonoid with high affinity for the benzodiazepine receptors | ||
| 3-propoxy-beta-carboline | 3-propoxy-beta-carboline: structure in first source | ||
| apigenin | Chamomile: Common name for several daisy-like plants (MATRICARIA; TRIPLEUROSPERMUM; ANTHEMIS; CHAMAEMELUM) native to Europe and Western Asia, now naturalized in the United States and Australia. | trihydroxyflavone | antineoplastic agent; metabolite |
| cholecalciferol | calciol : A hydroxy seco-steroid that is (5Z,7E)-9,10-secocholesta-5,7,10(19)-triene in which the pro-S hydrogen at position 3 has been replaced by a hydroxy group. It is the inactive form of vitamin D3, being hydroxylated in the liver to calcidiol (25-hydroxyvitamin D3), which is then further hydroxylated in the kidney to give calcitriol (1,25-dihydroxyvitamin D3), the active hormone. Cholecalciferol: Derivative of 7-dehydroxycholesterol formed by ULTRAVIOLET RAYS breaking of the C9-C10 bond. It differs from ERGOCALCIFEROL in having a single bond between C22 and C23 and lacking a methyl group at C24. | D3 vitamins; hydroxy seco-steroid; seco-cholestane; secondary alcohol; steroid hormone | geroprotector; human metabolite |
| harman | harman : An indole alkaloid fundamental parent with a structure of 9H-beta-carboline carrying a methyl substituent at C-1. It has been isolated from the bark of Sickingia rubra, Symplocus racemosa, Passiflora incarnata, Peganum harmala, Banisteriopsis caapi and Tribulus terrestris, as well as from tobacco smoke. It is a specific, reversible inhibitor of monoamine oxidase A. harman: a beta-carboline; RN given refers to parent cpd; structure | harmala alkaloid; indole alkaloid; indole alkaloid fundamental parent | anti-HIV agent; EC 1.4.3.4 (monoamine oxidase) inhibitor; plant metabolite |
| amentoflavone | biflavonoid; hydroxyflavone; ring assembly | angiogenesis inhibitor; antiviral agent; cathepsin B inhibitor; P450 inhibitor; plant metabolite | |
| baicalein | trihydroxyflavone | angiogenesis inhibitor; anti-inflammatory agent; antibacterial agent; anticoronaviral agent; antifungal agent; antineoplastic agent; antioxidant; apoptosis inducer; EC 1.13.11.31 (arachidonate 12-lipoxygenase) inhibitor; EC 1.13.11.33 (arachidonate 15-lipoxygenase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; EC 3.4.22.69 (SARS coronavirus main proteinase) inhibitor; EC 4.1.1.17 (ornithine decarboxylase) inhibitor; ferroptosis inhibitor; geroprotector; hormone antagonist; plant metabolite; prostaglandin antagonist; radical scavenger | |
| chrysin | chrysin : A dihydroxyflavone in which the two hydroxy groups are located at positions 5 and 7. | 7-hydroxyflavonol; dihydroxyflavone | anti-inflammatory agent; antineoplastic agent; antioxidant; EC 2.7.11.18 (myosin-light-chain kinase) inhibitor; hepatoprotective agent; plant metabolite |
| hispidulin | hispidulin : A monomethoxyflavone that is scutellarein methylated at position 6. | monomethoxyflavone; trihydroxyflavone | anti-inflammatory agent; anticonvulsant; antineoplastic agent; antioxidant; apoptosis inducer; plant metabolite |
| scutellarein | scutellarein : Flavone substituted with hydroxy groups at C-4', -5, -6 and -7. scutellarein: aglycone of scutellarin from Scutellaria baicalensis; carthamidin is 2S isomer of scutellarein; do not confuse with isoscutellarein and/or isocarthamidin which are respective regioisomers, or with the scutelarin protein | tetrahydroxyflavone | metabolite |
| wogonin | wogonin : A dihydroxy- and monomethoxy-flavone in which the hydroxy groups are positioned at C-5 and C-7 and the methoxy group is at C-8. wogonin: structure in first source | dihydroxyflavone; monomethoxyflavone | angiogenesis inhibitor; antineoplastic agent; cyclooxygenase 2 inhibitor; plant metabolite |
| cholesta-3,5-dien-7-one | |||
| l 655,708 | |||
| ry 80 | |||
| 1-Ethyl-9H-pyrido[3,4-b]indole | harmala alkaloid | ||
| ginkgolide b | |||
| dutasteride | dutasteride : An aza-steroid that is inasteride in which the tert-butyl group is replaced by a 2,5-bis(trifluoromethyl)phenyl group. A synthetic 4-azasteroid, dutasteride is a selective inhibitor of both the type 1 and type 2 isoforms of steroid 5alpha-reductase, an intracellular enzyme that converts testosterone to 5alpha-dihydrotestosterone. Dutasteride is used for the treatment of symptomatic benign prostatic hyperplasia in men with an enlarged prostate gland. Dutasteride: A 5-ALPHA-REDUCTASE INHIBITOR that is reported to inhibit both type-1 and type2 isoforms of the enzyme and is used to treat BENIGN PROSTATIC HYPERPLASIA. | (trifluoromethyl)benzenes; aza-steroid; delta-lactam | antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor |
| ganaxolone | ganaxolone: a selective, high-affinity, steroid modulator of the GABA(A) receptor; structure given in first source; RN given refers to (3alpha,5alpha)-isomer | corticosteroid hormone | |
| mrk 016 | MRK 016: an inverse agonist of GABA(A) alpha5 receptors; structure in first source | ||
| 6,6-dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6,7-dihydro-2-benzothiophen-4(5h)-one | 6,6-dimethyl-3-(2-hydroxyethyl)thio-1-(thiazol-2-yl)-6,7-dihydro-2-benzothiophen-4(5H)-one: a GABA-A alpha5 receptor inverse agonist; structure in first source | ||
| bis(7)-tacrine | secondary amino compound | apoptosis inhibitor; EC 1.14.13.39 (nitric oxide synthase) inhibitor; EC 3.1.1.7 (acetylcholinesterase) inhibitor; neuroprotective agent | |
| qh-ii-66 | QH-II-66: a alpha5-GABAA receptor agonist | ||
| l 838,417 | L 838,417: structure in first source | ||
| bn 52020 | |||
| ry 024 | RY 024: structure in first source | ||
| pwz-029 | PWZ-029: a compound with moderate inverse agonist functional selectivity at GABA(A) receptors containing alpha5 subunits, improves passive, but not active, avoidance learning in rats; structure in first source | ||
| batatasin-iii | stilbenoid | ||
| regorafenib | (trifluoromethyl)benzenes; aromatic ether; monochlorobenzenes; monofluorobenzenes; phenylureas; pyridinecarboxamide | antineoplastic agent; hepatotoxic agent; tyrosine kinase inhibitor | |
| naluzotan | naluzotan: an antidepressant and anti-anxiety agent; structure in first source | ||
| basimglurant | |||
| ro 4956371 | 2-chloro-4-((2,5-dimethyl-1-(4-(trifluoromethoxy)phenyl)-1H-imidazol-4-yl)ethynyl)pyridine: a metabotropic glutamate receptor 5 antagonist; structure in first source | ||
| mdv 3100 | (trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound | androgen antagonist; antineoplastic agent | |
| valproate sodium | Epilim: oral sodium valproate used as antidepressive agent sodium valproate : The sodium salt of valproic acid. valproate : A branched-chain saturated fatty acid anion that is the conjugate base of valproic acid. | organic sodium salt | geroprotector |
| 4-amino-8-(2-fluoro-6-methoxy-phenyl)-n-propylcinnoline-3-carboxamide | 4-amino-8-(2-fluoro-6-methoxy-phenyl)-N-propylcinnoline-3-carboxamide: a GABA(A) alpha2,3 receptor modulator; structure in first source | ||
| 4-amino-8-(2,5-dimethoxyphenyl)-n-propylcinnoline-3-carboxamide | |||
| apalutamide | |||
| nitd 609 | NITD 609: an antimalarial and coccidiostat; structure in first source |