2-phenylpyrazolo(4,3-c)quinolin-3(5H)-one: a mixed agonist/antagonist of the benzodiazepine receptor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 104916 |
| SCHEMBL ID | 1466280 |
| SCHEMBL ID | 10749256 |
| MeSH ID | M0104707 |
| Synonym |
|---|
| 77779-60-3 |
| 2-phenyl-1,2-dihydro-pyrazolo[4,3-c]quinolin- 3-one |
| BB 0221405 |
| AKOS002682173 |
| cgs-8216 |
| cgs 8216 |
| 2,5-dihydro-2-phenyl-3h-pyrazolo(4,3-c)quinolin-3-one |
| brn 4257286 |
| 3h-pyrazolo(4,3-c)quinolin-3-one, 2,5-dihydro-2-phenyl- |
| 2-phenylpyrazolo(4,3-c)quinolin-3(5h)-one |
| PDSP1_001763 |
| PDSP2_001746 |
| 2-phenyl-1,2-dihydro-3h-pyrazolo[4,3-c]quinolin-3-one |
| bdbm50017009 |
| cgs 8216, 1 |
| 2-phenyl-2,3a-dihydro-pyrazolo[4,3-c]quinolin-3-one(cgs 8216) |
| 2-phenyl-2,5-dihydro-pyrazolo[4,3-c]quinolin-3-one(cgs-8216) |
| 2-phenyl-2,5-dihydro-pyrazolo[4,3-c]quinolin-3-one(cgs 8216) |
| 2-phenyl-2h-pyrazolo[4,3-c]quinolin-3(5h)-one |
| 2-phenyl-2,5-dihydro-pyrazolo[4,3-c]quinolin-3-one (cgs 8216) |
| 2-phenyl-2,5-dihydro-pyrazolo[4,3-c]quinolin-3-one |
| 2-phenyl-1h-pyrazolo[4,3-c]quinolin-3-one |
| yxh2c8e92n , |
| unii-yxh2c8e92n |
| SCHEMBL1466280 |
| 2-phenyl-1h-pyrazolo[4,5-c]quinolin-3-one |
| 2-phenyl-1h,2h,3h-pyrazolo[4,3-c]quinolin-3-one |
| cgs8216 |
| gtpl4156 |
| gtpl4366 |
| [3h]cgs8216 |
| 2,5-dihydro-2-phenyl-3h-pyrazolo[4,3-c]quinolin-3-one |
| 2-phenyl-2,5-dihydro-pyrazolo-(4,3-c) quinolin-3-one |
| WRHJCJHWJSQAHY-UHFFFAOYSA-N |
| SCHEMBL10749256 |
| STL490581 |
| 2-phenylpyrazolo[4,3-c]quinoline-3(5h)-one |
| Q15634053 |
| DTXSID00998973 |
| 2-phenyl-2,5-dihydropyrazolo[4,3-c]quinolin-3(3h)-one |
| 3h-pyrazolo[4,3-c]quinolin-3-one, 2,5-dihydro-2-phenyl- |
| AKOS040748125 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " The method is applied to a pharmacokinetic study of CGS-8216 in the rat." | ( A pharmacokinetic study of CGS-8216, a benzodiazepine receptor ligand, in the rat. File, SE; Greenblatt, DJ; Lister, RG, 1984) | 0.27 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "The beta-carboline FG 7142 was studied alone and in combination with Ro 15-1788, CGS 8216 and lorazepam in squirrel monkeys trained to respond under a fixed-interval (FI) schedule of food presentation." | ( Behavioral studies with the beta-carboline FG 7142 combined with related drugs in monkeys. Wettstein, JG, 1989) | 0.28 |
| "The effects of several compounds believed to act at the GABA-benzodiazepine receptor complex and which have anticonvulsant or proconvulsant properties when administered in combination with picrotoxin and pentetrazol (leptazol, pentylenetetrazole) were investigated in combination with the convulsant benzodiazepine Ro 5-4864." | ( Pro- and anti-convulsant drug effects in combination with the convulsant benzodiazepine Ro 5-4864. File, SE; Pellow, S, 1985) | 0.27 |
| "30 mg/kg) alone, and in combination with the BDZ receptor antagonists flumazenil, ZK 93426, and CGS 8216 (20 mg/kg) in selectively bred alcohol-preferring (P) rats provided a two-bottle choice test between ethanol (EtOH) (10% v/v), and a palatable saccharin (0." | ( Effects of the benzodiazepine inverse agonist RO19-4603 alone and in combination with the benzodiazepine receptor antagonists flumazenil, ZK 93426 and CGS 8216, on ethanol intake in alcohol-preferring (P) rats. Cason, CR; Cox, R; Duemler, SE; Greene, TL; Hite, ML; June, HL; Li, TK; Lumeng, L; Mellon-Burke, J; Murphy, JM; Torres, L; Williams, JA, 1996) | 0.29 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " This antagonism was characterized both by a shift to the right and a decrease in the maximal stimulation, for the dose-response curves of diazepam and zopiclone." | ( Benzodiazepine receptor modulation of [35S]TBPS binding to the chloride channel. Noncompetitive inhibition of classical benzodiazepines and competitive inhibition of the partial agonist, CGS 9895, by CGS 8216. Braunwalder, A; Loo, P; Wood, PL, 1987) | 0.27 |
| ") shifted the dose-response curve of FG 7142 progressively to the right indicating pharmacological antagonism at benzodiazepine recognition sites." | ( Behavioral studies with the beta-carboline FG 7142 combined with related drugs in monkeys. Wettstein, JG, 1989) | 0.28 |
| "CGS-8216, a benzodiazepine antagonist, was administered to rats acutely dosed with diazepam, and to rats chronically dosed with diazepam or pentobarbital." | ( Benzodiazepine antagonist, CGS-8216, in diazepam- or pentobarbital-dependent and non-dependent rats. Martin, WR; McNicholas, LF, 1986) | 0.27 |
| " When the diazepam and zolpidem dose-response curves were re-established in the presence of a dose of Ro 15-1788 or CGS 8216 the depressant effects of the higher doses were antagonised." | ( Investigation of the actions of the benzodiazepine antagonists Ro 15-1788 and CGS 8216 using the schedule-controlled behavior of rats. Sanger, DJ, 1986) | 0.27 |
| " Flumazenil caused dose-related increases in the NPAS scores of both diazepam- and nordiazepam-dependent dogs; the slopes of the two dose-response lines were not different." | ( Precipitation of abstinence in nordiazepam- and diazepam-dependent dogs. Martin, WR; McNicholas, LF; Sloan, JW; Wala, E, 1988) | 0.27 |
| "Dogs, surgically implanted with a gastric fistula, were chronically dosed with diazepam or lorazepam." | ( Physical dependence on diazepam and lorazepam in the dog. Cherian, S; Martin, WR; McNicholas, LF, 1983) | 0.27 |
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 145 (80.11) | 18.7374 |
| 1990's | 29 (16.02) | 18.2507 |
| 2000's | 6 (3.31) | 29.6817 |
| 2010's | 1 (0.55) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.
| This Compound (8.75) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 10 (5.43%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 174 (94.57%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Substance | Relationship Strength | Studies | Trials | Classes | Roles |
|---|---|---|---|---|---|
| gamma-aminobutyric acid gamma-Aminobutyric Acid: The most common inhibitory neurotransmitter in the central nervous system.. gamma-aminobutyric acid : A gamma-amino acid that is butanoic acid with the amino substituent located at C-4. | 6.31 | 21 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid | human metabolite; neurotransmitter; Saccharomyces cerevisiae metabolite; signalling molecule |
| ammonium hydroxide azane : Saturated acyclic nitrogen hydrides having the general formula NnHn+2. | 1.98 | 1 | 0 | azane; gas molecular entity; mononuclear parent hydride | EC 3.5.1.4 (amidase) inhibitor; metabolite; mouse metabolite; neurotoxin; NMR chemical shift reference compound; nucleophilic reagent; refrigerant |
| chlorine chloride : A halide anion formed when chlorine picks up an electron to form an an anion. | 4.45 | 7 | 0 | halide anion; monoatomic chlorine | cofactor; Escherichia coli metabolite; human metabolite |
| 8-hydroxy-2-(di-n-propylamino)tetralin 8-Hydroxy-2-(di-n-propylamino)tetralin: A serotonin 1A-receptor agonist that is used experimentally to test the effects of serotonin.. 8-OH-DPAT : A tetralin substituted at positions 1 and 7 by hydroxy and dipropylamino groups respectively | 1.97 | 1 | 0 | phenols; tertiary amino compound; tetralins | serotonergic antagonist |
| pk 11195 PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine | 4.16 | 5 | 0 | aromatic amide; isoquinolines; monocarboxylic acid amide; monochlorobenzenes | antineoplastic agent |
| enprofylline enprofylline : Xanthine bearing a propyl substituent at position 3. A bronchodilator, it is used for the symptomatic treatment of asthma and chronic obstructive pulmonary disease, and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy. | 1.97 | 1 | 0 | oxopurine | anti-arrhythmia drug; anti-asthmatic drug; bronchodilator agent; non-steroidal anti-inflammatory drug |
| ro 5-4864 4'-chlorodiazepam: selectively binds peripheral benzodiazepine receptor | 4.45 | 7 | 0 | ||
| phenytoin [no description available] | 3.46 | 2 | 0 | imidazolidine-2,4-dione | anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent |
| 8-phenyltheophylline 8-phenyltheophylline: purinergic P1 receptor antagonist | 1.97 | 1 | 0 | ||
| alprazolam 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). 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. | 1.97 | 1 | 0 | organochlorine compound; triazolobenzodiazepine | anticonvulsant; anxiolytic drug; GABA agonist; muscle relaxant; sedative; xenobiotic |
| theophylline [no description available] | 3.47 | 2 | 0 | dimethylxanthine | adenosine receptor antagonist; anti-asthmatic drug; anti-inflammatory agent; bronchodilator agent; drug metabolite; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; fungal metabolite; human blood serum metabolite; immunomodulator; muscle relaxant; vasodilator agent |
| aniracetam [no description available] | 1.97 | 1 | 0 | N-acylpyrrolidine; pyrrolidin-2-ones | |
| baclofen [no description available] | 1.97 | 1 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant |
| buspirone Buspirone: An anxiolytic agent and serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the BENZODIAZAPINES, but it has an efficacy comparable to DIAZEPAM.. buspirone : An azaspiro compound that is 8-azaspiro[4.5]decane-7,9-dione substituted at the nitrogen atom by a 4-(piperazin-1-yl)butyl group which in turn is substituted by a pyrimidin-2-yl group at the N(4) position. | 2.88 | 4 | 0 | azaspiro compound; N-alkylpiperazine; N-arylpiperazine; organic heteropolycyclic compound; piperidones; pyrimidines | anxiolytic drug; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; sedative; serotonergic agonist |
| caffeine [no description available] | 3.75 | 3 | 0 | purine alkaloid; trimethylxanthine | adenosine A2A receptor antagonist; adenosine receptor antagonist; adjuvant; central nervous system stimulant; diuretic; EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; environmental contaminant; food additive; fungal metabolite; geroprotector; human blood serum metabolite; mouse metabolite; mutagen; plant metabolite; psychotropic drug; ryanodine receptor agonist; xenobiotic |
| cgs 15943 9-chloro-2-(2-furyl)-(1,2,4)triazolo(1,5-c)quinazolin-5-imine: non-xanthine triazoloquinazoline adenosine antagonist. CGS 15943 : A member of the class of triazoloquinazolines that is [1,2,4]triazolo[1,5-c]quinazoline substited at positions 2, 5 and 9 by furan-2-yl, amino and chloro groups respectively. A potent antagonist at adenosine A1 and adenosine A2A receptors. | 2.38 | 2 | 0 | aromatic amine; biaryl; furans; organochlorine compound; primary amino compound; quinazolines; triazoloquinazoline | adenosine A1 receptor antagonist; adenosine A2A receptor antagonist; antineoplastic agent; central nervous system stimulant |
| chlordiazepoxide Chlordiazepoxide: An anxiolytic benzodiazepine derivative with anticonvulsant, sedative, and amnesic properties. It has also been used in the symptomatic treatment of alcohol withdrawal.. 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. | 5.87 | 19 | 0 | benzodiazepine | |
| chlorpromazine Chlorpromazine: The prototypical phenothiazine antipsychotic drug. Like the other drugs in this class chlorpromazine's antipsychotic actions are thought to be due to long-term adaptation by the brain to blocking DOPAMINE RECEPTORS. Chlorpromazine has several other actions and therapeutic uses, including as an antiemetic and in the treatment of intractable hiccup.. chlorpromazine : A substituted phenothiazine in which the ring nitrogen at position 10 is attached to C-3 of an N,N-dimethylpropanamine moiety. | 1.97 | 1 | 0 | organochlorine compound; phenothiazines; tertiary amine | anticoronaviral agent; antiemetic; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; phenothiazine antipsychotic drug |
| clonazepam 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.. 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. | 3.06 | 5 | 0 | 1,4-benzodiazepinone; monochlorobenzenes | anticonvulsant; anxiolytic drug; GABA modulator |
| clonidine Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group. | 1.97 | 1 | 0 | clonidine; imidazoline | |
| cyproheptadine Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia. | 1.96 | 1 | 0 | piperidines; tertiary amine | anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist |
| desipramine Desipramine: A tricyclic dibenzazepine compound that potentiates neurotransmission. Desipramine selectively blocks reuptake of norepinephrine from the neural synapse, and also appears to impair serotonin transport. This compound also possesses minor anticholinergic activity, through its affinity to muscarinic receptors.. desipramine : A dibenzoazepine consisting of 10,11-dihydro-5H-dibenzo[b,f]azepine substituted on nitrogen with a 3-(methylamino)propyl group. | 1.97 | 1 | 0 | dibenzoazepine; secondary amino compound | adrenergic uptake inhibitor; alpha-adrenergic antagonist; antidepressant; cholinergic antagonist; drug allergen; EC 3.1.4.12 (sphingomyelin phosphodiesterase) inhibitor; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; H1-receptor antagonist; serotonin uptake inhibitor |
| nordazepam Nordazepam: An intermediate in the metabolism of DIAZEPAM to OXAZEPAM. It may have actions similar to those of diazepam.. 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. | 1.97 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; GABA modulator; human metabolite; sedative |
| amphetamine Amphetamine: A powerful central nervous system stimulant and sympathomimetic. Amphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulation of release of monamines, and inhibiting monoamine oxidase. Amphetamine is also a drug of abuse and a psychotomimetic. The l- and the d,l-forms are included here. The l-form has less central nervous system activity but stronger cardiovascular effects. The d-form is DEXTROAMPHETAMINE.. 1-phenylpropan-2-amine : A primary amine that is isopropylamine in which a hydrogen attached to one of the methyl groups has been replaced by a phenyl group.. amphetamine : A racemate comprising equimolar amounts of (R)-amphetamine (also known as levamphetamine or levoamphetamine) and (S)-amphetamine (also known as dexamfetamine or dextroamphetamine. | 1.96 | 1 | 0 | primary amine | |
| diazepam 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.. 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. | 7.39 | 64 | 0 | 1,4-benzodiazepinone; organochlorine compound | anticonvulsant; anxiolytic drug; environmental contaminant; sedative; xenobiotic |
| valproic acid Valproic Acid: A fatty acid with anticonvulsant and anti-manic properties that is used in the treatment of EPILEPSY and BIPOLAR DISORDER. The mechanisms of its therapeutic actions are not well understood. It may act by increasing GAMMA-AMINOBUTYRIC ACID levels in the brain or by altering the properties of VOLTAGE-GATED SODIUM CHANNELS.. valproic acid : A branched-chain saturated fatty acid that comprises of a propyl substituent on a pentanoic acid stem. | 2.37 | 2 | 0 | branched-chain fatty acid; branched-chain saturated fatty acid | anticonvulsant; antimanic drug; EC 3.5.1.98 (histone deacetylase) inhibitor; GABA agent; neuroprotective agent; psychotropic drug; teratogenic agent |
| etazolate Etazolate: A potent phosphodiesterase inhibitor proposed as an antipsychotic agent.. etazolate : A pyrazolopyridine that is 1H-pyrazolo[3,4-b]pyridine which is substituted at positions 1, 4, and 5 by ethyl, 2-isopropylidenehydrazino, and ethoxycarbonyl groups, respectively. A phosphodiesterase IV inhibitor with antidepressant and anxiolytic properties. | 3.06 | 1 | 0 | ethyl ester; hydrazone; pyrazolopyridine | alpha-secretase activator; antidepressant; antipsychotic agent; anxiolytic drug; GABA agent; neuroprotective agent; phosphodiesterase IV inhibitor |
| flumazenil 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.. 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. | 8.58 | 98 | 0 | ethyl ester; imidazobenzodiazepine; organofluorine compound | antidote to benzodiazepine poisoning; GABA antagonist |
| flunitrazepam 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.. 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. | 3.98 | 14 | 0 | 1,4-benzodiazepinone; C-nitro compound; monofluorobenzenes | anxiolytic drug; GABAA receptor agonist; sedative |
| flurazepam Flurazepam: A benzodiazepine derivative used mainly as a hypnotic.. flurazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a 2-(diethylamino)ethyl group, 2-fluorophenyl group and chloro group at positions 1, 5 and 7, respectively. It is a partial agonist of GABAA receptors and used for the treatment of insomnia. | 2.88 | 4 | 0 | 1,4-benzodiazepinone; monofluorobenzenes; organochlorine compound; tertiary amino compound | anticonvulsant; anxiolytic drug; GABAA receptor agonist; sedative |
| gaboxadol gaboxadol: GABA agonist; inhibitor of GABA uptake systems; structure | 2.39 | 2 | 0 | oxazole | |
| harmaline Harmaline: A beta-carboline alkaloid isolated from seeds of PEGANUM.. harmaline : A harmala alkaloid in which the harman skeleton is methoxy-substituted at C-7 and has been reduced across the 3,4 bond. | 1.96 | 1 | 0 | harmala alkaloid | oneirogen |
| imipramine Imipramine: The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group.. imipramine : A dibenzoazepine that is 5H-dibenzo[b,f]azepine substituted by a 3-(dimethylamino)propyl group at the nitrogen atom. | 1.97 | 1 | 0 | dibenzoazepine | adrenergic uptake inhibitor; antidepressant; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor |
| isoniazid Hydra: A genus of freshwater polyps in the family Hydridae, order Hydroida, class HYDROZOA. They are of special interest because of their complex organization and because their adult organization corresponds roughly to the gastrula of higher animals.. hydrazide : Compounds derived from oxoacids RkE(=O)l(OH)m (l =/= 0) by replacing -OH by -NRNR2 (R groups are commonly H). (IUPAC). | 1.96 | 1 | 0 | carbohydrazide | antitubercular agent; drug allergen |
| ketamine Ketamine: A cyclohexanone derivative used for induction of anesthesia. Its mechanism of action is not well understood, but ketamine can block NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE) and may interact with sigma receptors.. ketamine : A member of the class of cyclohexanones in which one of the hydrogens at position 2 is substituted by a 2-chlorophenyl group, while the other is substituted by a methylamino group. | 1.96 | 1 | 0 | cyclohexanones; monochlorobenzenes; secondary amino compound | analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic |
| lorazepam Lorazepam: A benzodiazepine used as an anti-anxiety agent with few side effects. It also has hypnotic, anticonvulsant, and considerable sedative properties and has been proposed as a preanesthetic agent. | 4.16 | 5 | 0 | benzodiazepine | |
| meprobamate Meprobamate: A carbamate with hypnotic, sedative, and some muscle relaxant properties, although in therapeutic doses reduction of anxiety rather than a direct effect may be responsible for muscle relaxation. Meprobamate has been reported to have anticonvulsant actions against petit mal seizures, but not against grand mal seizures (which may be exacerbated). It is used in the treatment of ANXIETY DISORDERS, and also for the short-term management of INSOMNIA but has largely been superseded by the BENZODIAZEPINES. (From Martindale, The Extra Pharmacopoeia, 30th ed, p603) | 2.66 | 3 | 0 | organic molecular entity | |
| midazolam Midazolam: A short-acting hypnotic-sedative drug with anxiolytic and amnestic properties. It is used in dentistry, cardiac surgery, endoscopic procedures, as preanesthetic medication, and as an adjunct to local anesthesia. The short duration and cardiorespiratory stability makes it useful in poor-risk, elderly, and cardiac patients. It is water-soluble at pH less than 4 and lipid-soluble at physiological pH.. midazolam : An imidazobenzodiazepine that is 4H-imidazo[1,5-a][1,4]benzodiazepine which is substituted by a methyl, 2-fluorophenyl and chloro groups at positions 1, 6 and 8, respectively. | 4.96 | 7 | 0 | imidazobenzodiazepine; monofluorobenzenes; organochlorine compound | anticonvulsant; antineoplastic agent; anxiolytic drug; apoptosis inducer; central nervous system depressant; GABAA receptor agonist; general anaesthetic; muscle relaxant; sedative |
| muscimol 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.. 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. | 2.37 | 2 | 0 | alkaloid; isoxazoles; primary amino compound | fungal metabolite; GABA agonist; oneirogen; psychotropic drug |
| fg 7142 FG 7142: benzodiazepine receptor agonist | 5.51 | 22 | 0 | beta-carbolines | |
| nifedipine Nifedipine: A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. | 1.96 | 1 | 0 | C-nitro compound; dihydropyridine; methyl ester | calcium channel blocker; human metabolite; tocolytic agent; vasodilator agent |
| oxazepam Oxazepam: A benzodiazepine used in the treatment of anxiety, alcohol withdrawal, and insomnia.. oxazepam : A 1,4-benzodiazepinone that is 1,3-dihydro-2H-1,4-benzodiazepin-2-one substituted by a chloro group at position 7, a hydroxy group at position 3 and phenyl group at position 5. | 1.97 | 1 | 0 | 1,4-benzodiazepinone; organochlorine compound | anxiolytic drug; environmental contaminant; xenobiotic |
| pargyline Pargyline: A monoamine oxidase inhibitor with antihypertensive properties. | 1.97 | 1 | 0 | aromatic amine | |
| pentobarbital 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). 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. | 3.76 | 11 | 0 | barbiturates | GABAA receptor agonist |
| phenobarbital Phenobarbital: A barbituric acid derivative that acts as a nonselective central nervous system depressant. It potentiates GAMMA-AMINOBUTYRIC ACID action on GABA-A RECEPTORS, and modulates chloride currents through receptor channels. It also inhibits glutamate induced depolarizations.. phenobarbital : A member of the class of barbiturates, the structure of which is that of barbituric acid substituted at C-5 by ethyl and phenyl groups. | 2.37 | 2 | 0 | barbiturates | anticonvulsant; drug allergen; excitatory amino acid antagonist; sedative |
| sch 16134 quazepam: structure given in first source | 1.96 | 1 | 0 | benzodiazepine | |
| ro 15-4513 Ro 15-4513: a partial inverse agonist of benzodiazepine receptors | 3.23 | 6 | 0 | organic heterotricyclic compound; organonitrogen heterocyclic compound | |
| rolipram [no description available] | 1.97 | 1 | 0 | pyrrolidin-2-ones | antidepressant; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor |
| saccharin Saccharin: Flavoring agent and non-nutritive sweetener.. saccharin : A 1,2-benzisothiazole having a keto-group at the 3-position and two oxo substituents at the 1-position. It is used as an artificial sweetening agent. | 2.67 | 3 | 0 | 1,2-benzisothiazole; N-sulfonylcarboxamide | environmental contaminant; sweetening agent; xenobiotic |
| tofisopam tofisopam: structure; dextofisopam is the R-enantiomer of tofisopam & antidiarrheal | 1.96 | 1 | 0 | organic molecular entity | |
| ici 136,753 [no description available] | 2.66 | 3 | 0 | pyrazolopyridine | |
| 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. | 2.67 | 3 | 0 | triazolobenzodiazepine | sedative |
| urethane [no description available] | 1.97 | 1 | 0 | carbamate ester | fungal metabolite; mutagen |
| zolpidem Zolpidem: An imidazopyridine derivative and short-acting GABA-A receptor agonist that is used for the treatment of INSOMNIA.. 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. | 2.67 | 3 | 0 | imidazopyridine | central nervous system depressant; GABA agonist; sedative |
| zopiclone zopiclone: S(+)-enantiomer of racemic zopiclone; 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; was term of zopiclone 2004-2007. zopiclone : A pyrrolo[3,4-b]pyrazine compound having a 4-methylpiperazine-1-carboxyl group at the 5-position, a 5-chloropyridin-2-yl group at the 6-position and an oxo-substituent at the 7-position. | 3.75 | 3 | 0 | monochloropyridine; pyrrolopyrazine | central nervous system depressant; sedative |
| corticosterone [no description available] | 2.88 | 4 | 0 | 11beta-hydroxy steroid; 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; C21-steroid; glucocorticoid; primary alpha-hydroxy ketone | human metabolite; mouse metabolite |
| hexobendine Hexobendine: A potent vasoactive agent that dilates cerebral and coronary arteries, but slightly constricts femoral arteries, without any effects on heart rate, blood pressure or cardiac output. | 1.96 | 1 | 0 | trihydroxybenzoic acid | |
| pentylenetetrazole Pentylenetetrazole: A pharmaceutical agent that displays activity as a central nervous system and respiratory stimulant. It is considered a non-competitive GAMMA-AMINOBUTYRIC ACID antagonist. Pentylenetetrazole has been used experimentally to study seizure phenomenon and to identify pharmaceuticals that may control seizure susceptibility.. pentetrazol : An organic heterobicyclic compound that is 1H-tetrazole in which the hydrogens at positions 1 and 5 are replaced by a pentane-1,5-diyl group. A central and respiratory stimulant, it was formerly used for the treatment of cough and other respiratory tract disorders, cardiovascular disorders including hypotension, and pruritis. | 3.67 | 10 | 0 | organic heterobicyclic compound; organonitrogen heterocyclic compound | |
| physostigmine Physostigmine: A cholinesterase inhibitor that is rapidly absorbed through membranes. It can be applied topically to the conjunctiva. It also can cross the blood-brain barrier and is used when central nervous system effects are desired, as in the treatment of severe anticholinergic toxicity. | 3.06 | 1 | 0 | carbamate ester; indole alkaloid | antidote to curare poisoning; EC 3.1.1.8 (cholinesterase) inhibitor; miotic |
| carbostyril Quinolones: A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID.. quinolin-2(1H)-one : A quinolone that is 1,2-dihydroquinoline substituted by an oxo group at position 2. | 2.68 | 3 | 0 | monohydroxyquinoline; quinolone | bacterial xenobiotic metabolite |
| desoxycorticosterone Desoxycorticosterone: A steroid metabolite that is the 11-deoxy derivative of CORTICOSTERONE and the 21-hydroxy derivative of PROGESTERONE | 1.97 | 1 | 0 | 20-oxo steroid; 21-hydroxy steroid; 3-oxo-Delta(4) steroid; mineralocorticoid; primary alpha-hydroxy ketone | human metabolite; mouse metabolite |
| barbituric acid barbituric acid: RN given refers to parent cpd; structure from Merck Index, 9th ed, #966. barbituric acid : A barbiturate, the structure of which is that of perhydropyrimidine substituted at C-2, -4 and -6 by oxo groups. Barbituric acid is the parent compound of barbiturate drugs, although it is not itself pharmacologically active. | 1.96 | 1 | 0 | barbiturates | allergen; xenobiotic |
| phencyclidine Phencyclidine: A hallucinogen formerly used as a veterinary anesthetic, and briefly as a general anesthetic for humans. Phencyclidine is similar to KETAMINE in structure and in many of its effects. Like ketamine, it can produce a dissociative state. It exerts its pharmacological action through inhibition of NMDA receptors (RECEPTORS, N-METHYL-D-ASPARTATE). As a drug of abuse, it is known as PCP and Angel Dust.. phencyclidine : A member of the class of piperidines that is piperidine in which the nitrogen is substituted with a 1-phenylcyclohexyl group. Formerly used as an anaesthetic agent, it exhibits both hallucinogenic and neurotoxic effects. | 1.96 | 1 | 0 | benzenes; piperidines | anaesthetic; neurotoxin; NMDA receptor antagonist; psychotropic drug |
| 2-chloroadenosine 5-chloroformycin A: structure given in first source | 1.97 | 1 | 0 | purine nucleoside | |
| quinazolines Quinazolines: A group of aromatic heterocyclic compounds that contain a bicyclic structure with two fused six-membered aromatic rings, a benzene ring and a pyrimidine ring.. quinazoline : A mancude organic heterobicyclic parent that is naphthalene in which the carbon atoms at positions 1 and 3 have been replaced by nitrogen atoms.. quinazolines : Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives. | 2.38 | 2 | 0 | azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines | |
| isoxazoles Isoxazoles: Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.. isoxazole : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing three carbon atoms and an oxygen and nitrogen atom adjacent to each other. It is the parent of the class of isoxazoles.. isoxazoles : Oxazoles in which the N and O atoms are adjacent. | 2.67 | 3 | 0 | isoxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | |
| oxazoles Oxazoles: Five-membered heterocyclic ring structures containing an oxygen in the 1-position and a nitrogen in the 3-position, in distinction from ISOXAZOLES where they are at the 1,2 positions.. 1,3-oxazole : A five-membered monocyclic heteroarene that is an analogue of cyclopentadiene with O in place of CH2 at position 1 and N in place of CH at position 3.. oxazole : An azole based on a five-membered heterocyclic aromatic skeleton containing one N and one O atom. | 2 | 1 | 0 | 1,3-oxazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene | |
| aminophylline Aminophylline: A drug combination that contains THEOPHYLLINE and ethylenediamine. It is more soluble in water than theophylline but has similar pharmacologic actions. It's most common use is in bronchial asthma, but it has been investigated for several other applications.. aminophylline : A mixture comprising of theophylline and ethylenediamine in a 2:1 ratio. | 2.66 | 3 | 0 | mixture | bronchodilator agent; cardiotonic drug |
| methysergide Methysergide: An ergot derivative that is a congener of LYSERGIC ACID DIETHYLAMIDE. It antagonizes the effects of serotonin in blood vessels and gastrointestinal smooth muscle, but has few of the properties of other ergot alkaloids. Methysergide is used prophylactically in migraine and other vascular headaches and to antagonize serotonin in the carcinoid syndrome.. methysergide : A synthetic ergot alkaloid, structurally related to the oxytocic agent methylergonovine and to the potent hallucinogen LSD and used prophylactically to reduce the frequency and intensity of severe vascular headaches. | 1.96 | 1 | 0 | ergoline alkaloid | |
| bicuculline Bicuculline: An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.. 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. | 1.96 | 1 | 0 | benzylisoquinoline alkaloid; isoquinoline alkaloid; isoquinolines | agrochemical; central nervous system stimulant; GABA-gated chloride channel antagonist; GABAA receptor antagonist; neurotoxin |
| 4-amino-3-phenylbutyric acid 4-amino-3-phenylbutyric acid: phenyl deriv of GABA; RN given refers to cpd without isomeric designation; structure | 1.97 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| cyclazocine Cyclazocine: An analgesic with mixed narcotic agonist-antagonist properties. | 1.96 | 1 | 0 | ||
| pregnanolone Pregnanolone: A pregnane found in the urine of pregnant women and sows. It has anesthetic, hypnotic, and sedative properties.. 3alpha-hydroxy-5beta-pregnan-20-one : The 3alpha-stereoisomer of 3-hydroxy-5beta-pregnan-20-one. | 1.97 | 1 | 0 | 3-hydroxy-5beta-pregnan-20-one; 3alpha-hydroxy steroid | human metabolite; intravenous anaesthetic; sedative |
| azides Azides: Organic or inorganic compounds that contain the -N3 group.. azide : Any nitrogen molecular entity containing the group -N3. | 3.07 | 5 | 0 | pseudohalide anion | mitochondrial respiratory-chain inhibitor |
| cartazolate cartazolate: structure | 3.06 | 1 | 0 | ||
| 4-isopropylbicyclophosphate 4-isopropylbicyclophosphate: highly toxic cpd used in spectroscopic studies, potential flame retardants, vinyl resin stabilizers, & antioxidants; are not cholinesterase inhibitors; structure | 1.96 | 1 | 0 | ||
| denzimol denzimol: structure in first source | 1.97 | 1 | 0 | ||
| alpidem [no description available] | 1.97 | 1 | 0 | imidazoles | |
| adenosine quinquefolan B: isolated from roots of Panax quinquefolium L.; RN not in Chemline 10/87; RN from Toxlit | 4.57 | 8 | 0 | adenosines; purines D-ribonucleoside | analgesic; anti-arrhythmia drug; fundamental metabolite; human metabolite; vasodilator agent |
| abecarnil [no description available] | 2.4 | 2 | 0 | ||
| triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms. | 2.67 | 3 | 0 | 1,2,3-triazole | |
| ethanolamine o-sulfate [no description available] | 1.97 | 1 | 0 | ||
| pipequaline pipequaline: anticonflict & anticonvulsant quinoline derivative; structure given in first source | 4.56 | 8 | 0 | ||
| 1,3-dipropyl-8-(2-amino-4-chlorophenyl)xanthine [no description available] | 2.37 | 2 | 0 | ||
| 2,5-dihydro-2-(4-methoxyphenyl)-3h-pyrazolo(4,3-c)quinolin-3-one [no description available] | 4.45 | 7 | 0 | ||
| tetrahydrodeoxycorticosterone tetrahydrodeoxycorticosterone: RN given refers to (3alpha,5beta)-isomer | 1.97 | 1 | 0 | 21-hydroxy steroid | |
| tert-butylbicyclophosphorothionate tert-butylbicyclophosphorothionate: binds to GABA & ion recognition sites; structure given in first source | 2.37 | 2 | 0 | organic thiophosphate | |
| 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 | 4.68 | 9 | 0 | 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 | 5.83 | 18 | 0 | beta-carbolines | |
| bremazocine bremazocine: potent, log-acting opiate kappa-agonist & centrally acting analgesic; RN given refers to (2R)-isomer; structure given in first source | 1.96 | 1 | 0 | ||
| beta-carboline-3-carboxylic acid methyl ester beta-carboline-3-carboxylic acid methyl ester: structure given in first source | 3.47 | 8 | 0 | beta-carbolines | |
| sr 95531 [no description available] | 2.02 | 1 | 0 | methoxybenzenes | |
| bretazenil bretazenil: RN given for (S) isomer | 2.4 | 2 | 0 | ||
| cl 218872 CL 218872: shows specific action on benzodiazepine receptors; structure | 5.08 | 14 | 0 | pyridazines; ring assembly | |
| 2-(4-chlorophenyl)-2,5-dihydropyrazolo(4,3-c)quinoline-3(3h)-one 2-(4-chlorophenyl)-2,5-dihydropyrazolo(4,3-c)quinoline-3(3H)-one: inhibits binding of benzodiazepine cpds to benzodiazepine receptors in the brain | 5.88 | 19 | 0 | ||
| s 135 S 135: GABA receptor agonist; structure given in first source | 2.39 | 2 | 0 | ||
| ro 15-3505 [no description available] | 2 | 1 | 0 | ||
| tifluadom tifluadom: acts on opiate receptors; structure given in first source | 1.96 | 1 | 0 | benzodiazepine | |
| zk 93426 ZK 93426: GABA-A receptor antag | 3.48 | 8 | 0 | beta-carbolines | |
| zk 93423 [no description available] | 2.67 | 3 | 0 | beta-carbolines | |
| propyl beta-carboline-3-carboxylate propyl beta-carboline-3-carboxylate: binds specifically to brain benzodiazepine receptors | 3.46 | 2 | 0 | beta-carbolines | |
| zk 91296 ZK 91296: structure in first source | 3.22 | 6 | 0 | ||
| 3-ethoxy-beta-carboline 3-ethoxy-beta-carboline: high affinity benzodiazepine receptor ligand with partial inverse agonist properties | 2 | 1 | 0 | ||
| tert-butyl beta-carboline-3-carboxylate tert-butyl beta-carboline-3-carboxylate: benzodiazepine receptor antagonist | 2 | 1 | 0 | ||
| ro 19-4603 [no description available] | 1.99 | 1 | 0 | organonitrogen heterocyclic compound; organosulfur heterocyclic compound; tert-butyl ester | |
| ro 14-7437 Ro 14-7437: benzodiazepine antag; no other info available 8/16/83 | 2 | 1 | 0 | ||
| l 663581 L 663581: structure given in first source; partial agonist at the benzodiazepine receptor | 2.4 | 2 | 0 | ||
| ethylketocyclazocine Ethylketocyclazocine: A kappa opioid receptor agonist. The compound has analgesic action and shows positive inotropic effects on the electrically stimulated left atrium. It also affects various types of behavior in mammals such as locomotion, rearing, and grooming. | 1.96 | 1 | 0 | ||
| pk 9084 PK 9084: anticonflict & anticonvulsant quinoline derivative; structure given in first source | 2.88 | 4 | 0 | ||
| cgs 20625 CGS 20625: benzodiazepine receptor agonists; structure given in first source | 3.06 | 1 | 0 | pyrazoles; ring assembly | |
| n(6)-(2-(4-chlorophenyl)bicyclo(2.2.2.)-octyl)(3)-adenosine N(6)-(2-(4-chlorophenyl)bicyclo(2.2.2.)-octyl)(3)-adenosine: enhances diazepam binding to brain benzodiazepine receptors | 3.06 | 1 | 0 | ||
| zg 63 ZG 63: structure given in first source; a high affinity ligand for diazepam-insensitive benzodiazepine receptors | 2 | 1 | 0 | ||
| inositol 1,4,5-trisphosphate Inositol 1,4,5-Trisphosphate: Intracellular messenger formed by the action of phospholipase C on phosphatidylinositol 4,5-bisphosphate, which is one of the phospholipids that make up the cell membrane. Inositol 1,4,5-trisphosphate is released into the cytoplasm where it releases calcium ions from internal stores within the cell's endoplasmic reticulum. These calcium ions stimulate the activity of B kinase or calmodulin. | 2 | 1 | 0 | myo-inositol trisphosphate | mouse metabolite |
| nitroarginine Nitroarginine: An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6). N(gamma)-nitro-L-arginine : An L-arginine derivative that is L-arginine in which the terminal nitrogen of the guanidyl group is replaced by a nitro group. | 2.02 | 1 | 0 | guanidines; L-arginine derivative; N-nitro compound; non-proteinogenic L-alpha-amino acid | |
| strychnine 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.. strychnine : A monoterpenoid indole alkaloid that is strychnidine bearing a keto substituent at the 10-position. | 1.96 | 1 | 0 | monoterpenoid indole alkaloid; organic heteroheptacyclic compound | avicide; cholinergic antagonist; glycine receptor antagonist; neurotransmitter agent; rodenticide |
| diprenorphine Diprenorphine: A narcotic antagonist similar in action to NALOXONE. It is used to remobilize animals after ETORPHINE neuroleptanalgesia and is considered a specific antagonist to etorphine. | 1.97 | 1 | 0 | morphinane alkaloid | |
| cocaine 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.. cocaine : A tropane alkaloid obtained from leaves of the South American shrub Erythroxylon coca. | 1.96 | 1 | 0 | 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 |
| adenosine-5'-(n-ethylcarboxamide) Adenosine-5'-(N-ethylcarboxamide): A stable adenosine A1 and A2 receptor agonist. Experimentally, it inhibits cAMP and cGMP phosphodiesterase activity.. N-ethyl-5'-carboxamidoadenosine : A derivative of adenosine in which the 5'-hydroxymethyl group is replaced by an N-ethylcarboxamido group. | 1.97 | 1 | 0 | adenosines; monocarboxylic acid amide | adenosine A1 receptor agonist; adenosine A2A receptor agonist; antineoplastic agent; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor; vasodilator agent |
| n(6)-cyclopentyladenosine [no description available] | 2.37 | 2 | 0 | ||
| loreclezole loreclezole: RN given for Z-isomer; RN for cpd without isomeric designation not avail 12/90 | 1.98 | 1 | 0 | ||
| quinine [no description available] | 1.96 | 1 | 0 | cinchona alkaloid | antimalarial; muscle relaxant; non-narcotic analgesic |
| u-50488 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer: A non-peptide, kappa-opioid receptor agonist which has also been found to stimulate the release of adrenocorticotropin (ADRENOCORTICOTROPIC HORMONE) via the release of hypothalamic arginine vasopressin (ARGININE VASOPRESSIN) and CORTICOTROPIN-RELEASING HORMONE. (From J Pharmacol Exp Ther 1997;280(1):416-21). U50488 : A monocarboxylic acid amide obtained by formal condensation between the carboxy group of 3,4-dichlorophenylacetic acid and the secondary amino group of (1R,2R)-N-methyl-2-(pyrrolidin-1-yl)cyclohexanamine | 1.96 | 1 | 0 | dichlorobenzene; monocarboxylic acid amide; N-alkylpyrrolidine | analgesic; antitussive; calcium channel blocker; diuretic; kappa-opioid receptor agonist |
| 3-propoxy-beta-carboline 3-propoxy-beta-carboline: structure in first source | 2 | 1 | 0 | ||
| naloxone Naloxone: A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.. naloxone : A synthetic morphinane alkaloid that is morphinone in which the enone double bond has been reduced to a single bond, the hydrogen at position 14 has been replaced by a hydroxy group, and the methyl group attached to the nitrogen has been replaced by an allyl group. A specific opioid antagonist, it is used (commonly as its hydrochloride salt) to reverse the effects of opioids, both following their use of opioids during surgery and in cases of known or suspected opioid overdose. | 2.66 | 3 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary alcohol | antidote to opioid poisoning; central nervous system depressant; mu-opioid receptor antagonist |
| morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn. | 1.97 | 1 | 0 | morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound | anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic |
| l 655,708 [no description available] | 2 | 1 | 0 | ||
| ry 80 [no description available] | 2 | 1 | 0 | ||
| 3-hydroxymethyl-beta-carboline 3-hydroxymethyl-beta-carboline: antagonizes anticonvulsant & anxiolytic actions of diazepam at doses which do not elicit overt behavioral effects in mice | 1.96 | 1 | 0 | beta-carbolines | |
| naltrexone Naltrexone: Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.. naltrexone : An organic heteropentacyclic compound that is naloxone substituted in which the allyl group attached to the nitrogen is replaced by a cyclopropylmethyl group. A mu-opioid receptor antagonist, it is used to treat alcohol dependence. | 2.88 | 4 | 0 | cyclopropanes; morphinane-like compound; organic heteropentacyclic compound | antidote to opioid poisoning; central nervous system depressant; environmental contaminant; mu-opioid receptor antagonist; xenobiotic |
| 1-methyl-beta-carboline-3-carboxylic acid 1-methyl-beta-carboline-3-carboxylic acid: metabolite from cows fed with corn silage; structure in first source | 2.37 | 2 | 0 | ||
| morphinans Morphinans: Compounds based on a partially saturated iminoethanophenanthrene, which can be described as ethylimino-bridged benzo-decahydronaphthalenes. They include some of the OPIOIDS found in PAPAVER that are used as ANALGESICS. | 1.97 | 1 | 0 | isoquinoline alkaloid fundamental parent; morphinane alkaloid | |
| qh-ii-66 QH-II-66: a alpha5-GABAA receptor agonist | 2 | 1 | 0 | ||
| n(6)-cyclohexyladenosine N(6)-cyclohexyladenosine: structure given in first source; receptors, purinergic P1 agonist | 2.88 | 4 | 0 | ||
| ry 024 RY 024: structure in first source | 2 | 1 | 0 | ||
| 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 | 2 | 1 | 0 | ||
| picrotoxin Picrotoxin: A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Picrotoxin blocks the GAMMA-AMINOBUTYRIC ACID-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates.. picrotoxin : A mixture consisting of equimolar amounts of picrotoxinin and picrotin found in the climbing plant Anamirta cocculus. | 5.28 | 10 | 0 | ||
| guanosine triphosphate Guanosine Triphosphate: Guanosine 5'-(tetrahydrogen triphosphate). A guanine nucleotide containing three phosphate groups esterified to the sugar moiety. | 1.96 | 1 | 0 | guanosine 5'-phosphate; purine ribonucleoside 5'-triphosphate | Escherichia coli metabolite; mouse metabolite; uncoupling protein inhibitor |
| flumezapine flumezapine: structure given in first source | 1.97 | 1 | 0 | benzodiazepine | |
| ro 5-3663 Ro 5-3663: RN given refers to parent cpd; structure in first source | 4.26 | 3 | 0 |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS. | 0 | 5.13 | 18 | 0 |
| Encephalopathy, Hepatic [description not available] | 0 | 4.45 | 5 | 0 |
| Hepatic Encephalopathy A syndrome characterized by central nervous system dysfunction in association with LIVER FAILURE, including portal-systemic shunts. Clinical features include lethargy and CONFUSION (frequently progressing to COMA); ASTERIXIS; NYSTAGMUS, PATHOLOGIC; brisk oculovestibular reflexes; decorticate and decerebrate posturing; MUSCLE SPASTICITY; and bilateral extensor plantar reflexes (see REFLEX, BABINSKI). ELECTROENCEPHALOGRAPHY may demonstrate triphasic waves. (From Adams et al., Principles of Neurology, 6th ed, pp1117-20; Plum & Posner, Diagnosis of Stupor and Coma, 3rd ed, p222-5) | 0 | 4.45 | 5 | 0 |
| Ataxia Impairment of the ability to perform smoothly coordinated voluntary movements. This condition may affect the limbs, trunk, eyes, pharynx, larynx, and other structures. Ataxia may result from impaired sensory or motor function. Sensory ataxia may result from posterior column injury or PERIPHERAL NERVE DISEASES. Motor ataxia may be associated with CEREBELLAR DISEASES; CEREBRAL CORTEX diseases; THALAMIC DISEASES; BASAL GANGLIA DISEASES; injury to the RED NUCLEUS; and other conditions. | 0 | 2.37 | 2 | 0 |
| Absence Seizure [description not available] | 0 | 4.16 | 17 | 0 |
| Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder. | 0 | 4.16 | 17 | 0 |
| Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms. | 0 | 2.37 | 2 | 0 |
| Chemical Dependence [description not available] | 0 | 3.22 | 6 | 0 |
| Drug Withdrawal Symptoms [description not available] | 0 | 3.57 | 9 | 0 |
| Action Tremor [description not available] | 0 | 2.36 | 2 | 0 |
| Substance Withdrawal Syndrome Physiological and psychological symptoms associated with withdrawal from the use of a drug after prolonged administration or habituation. The concept includes withdrawal from smoking or drinking, as well as withdrawal from an administered drug. | 0 | 3.57 | 9 | 0 |
| Tremor Cyclical movement of a body part that can represent either a physiologic process or a manifestation of disease. Intention or action tremor, a common manifestation of CEREBELLAR DISEASES, is aggravated by movement. In contrast, resting tremor is maximal when there is no attempt at voluntary movement, and occurs as a relatively frequent manifestation of PARKINSON DISEASE. | 0 | 2.36 | 2 | 0 |
| Substance-Related Disorders Disorders related to substance use or abuse. | 0 | 3.22 | 6 | 0 |
| Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases. | 0 | 2.66 | 3 | 0 |
| Benign Psychomotor Epilepsy, Childhood [description not available] | 0 | 1.96 | 1 | 0 |
| Epilepsy, Temporal Lobe A localization-related (focal) form of epilepsy characterized by recurrent seizures that arise from foci within the TEMPORAL LOBE, most commonly from its mesial aspect. A wide variety of psychic phenomena may be associated, including illusions, hallucinations, dyscognitive states, and affective experiences. The majority of complex partial seizures (see EPILEPSY, COMPLEX PARTIAL) originate from the temporal lobes. Temporal lobe seizures may be classified by etiology as cryptogenic, familial, or symptomatic. (From Adams et al., Principles of Neurology, 6th ed, p321). | 0 | 1.96 | 1 | 0 |
| Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH. | 0 | 2.37 | 2 | 0 |
| Clasp-Knife Spasticity [description not available] | 0 | 2.37 | 2 | 0 |
| Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments. | 0 | 2.65 | 3 | 0 |
| Muscle Relaxation That phase of a muscle twitch during which a muscle returns to a resting position. | 0 | 2.37 | 2 | 0 |
| Muscle Spasticity A form of muscle hypertonia associated with upper MOTOR NEURON DISEASE. Resistance to passive stretch of a spastic muscle results in minimal initial resistance (a free interval) followed by an incremental increase in muscle tone. Tone increases in proportion to the velocity of stretch. Spasticity is usually accompanied by HYPERREFLEXIA and variable degrees of MUSCLE WEAKNESS. (From Adams et al., Principles of Neurology, 6th ed, p54) | 0 | 2.37 | 2 | 0 |
| Alcohol Drinking Behaviors associated with the ingesting of ALCOHOLIC BEVERAGES, including social drinking. | 0 | 2.4 | 2 | 0 |
| Delayed Effects, Prenatal Exposure [description not available] | 0 | 1.97 | 1 | 0 |
| Ache [description not available] | 0 | 1.97 | 1 | 0 |
| Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS. | 0 | 1.97 | 1 | 0 |
| Alcoholic Intoxication An acute brain syndrome which results from the excessive ingestion of ETHANOL or ALCOHOLIC BEVERAGES. | 0 | 1.97 | 1 | 0 |
| Anesthesia A state characterized by loss of feeling or sensation. This depression of nerve function is usually the result of pharmacologic action and is induced to allow performance of surgery or other painful procedures. | 0 | 1.97 | 1 | 0 |
| Ischemia A hypoperfusion of the BLOOD through an organ or tissue caused by a PATHOLOGIC CONSTRICTION or obstruction of its BLOOD VESSELS, or an absence of BLOOD CIRCULATION. | 0 | 1.97 | 1 | 0 |
| Aggression Behavior which may be manifested by destructive and attacking action which is verbal or physical, by covert attitudes of hostility or by obstructionism. | 0 | 2.88 | 1 | 0 |
| Acute Myelogenous Leukemia [description not available] | 0 | 1.97 | 1 | 0 |
| Leukemia, Myeloid, Acute Clonal expansion of myeloid blasts in bone marrow, blood, and other tissue. Myeloid leukemias develop from changes in cells that normally produce NEUTROPHILS; BASOPHILS; EOSINOPHILS; and MONOCYTES. | 0 | 1.97 | 1 | 0 |
| Gastric Fistula Abnormal passage communicating with the STOMACH. | 0 | 1.97 | 1 | 0 |
| Aura [description not available] | 0 | 1.97 | 1 | 0 |
| Epilepsy A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313) | 0 | 1.97 | 1 | 0 |