CGP 56999A: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9800175 |
| SCHEMBL ID | 2956711 |
| MeSH ID | M0268664 |
| Synonym |
|---|
| gtpl1071 |
| 3-[(1r)-1-[[(2s)-3-(cyclohexylmethyl-hydroxyphosphoryl)-2-hydroxypropyl]amino]ethyl]benzoic acid |
| cgp-56999a |
| cgp56999a |
| cgp 56999a |
| SCHEMBL2956711 |
| 153994-97-9 |
| Q27075918 |
| AKOS040748118 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1346001 | Rat GABAB1 (GABAB receptors) | 1997 | Nature, Mar-20, Volume: 386, Issue:6622 | Expression cloning of GABA(B) receptors uncovers similarity to metabotropic glutamate receptors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 5 (35.71) | 18.2507 |
| 2000's | 6 (42.86) | 29.6817 |
| 2010's | 3 (21.43) | 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] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 14 (100.00%) | 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. | 2.7 | 3 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid | human metabolite; neurotransmitter; Saccharomyces cerevisiae metabolite; signalling molecule |
| 3,4-dihydroxyphenylacetic acid 3,4-Dihydroxyphenylacetic Acid: A deaminated metabolite of LEVODOPA.. (3,4-dihydroxyphenyl)acetic acid : A dihydroxyphenylacetic acid having the two hydroxy substituents located at the 3- and 4-positions. It is a metabolite of dopamine.. dihydroxyphenylacetic acid : A dihydroxy monocarboxylic acid consisting of phenylacetic acid having two phenolic hydroxy substituents. | 2.03 | 1 | 0 | catechols; dihydroxyphenylacetic acid | human metabolite |
| 2-amino-5-phosphonovalerate 2-Amino-5-phosphonovalerate: The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors. | 2.13 | 1 | 0 | non-proteinogenic alpha-amino acid | NMDA receptor antagonist |
| 2-hydroxysaclofen 2-hydroxysaclofen: structure given in first source | 1.99 | 1 | 0 | organochlorine compound | |
| baclofen [no description available] | 3.1 | 5 | 0 | amino acid zwitterion; gamma-amino acid; monocarboxylic acid; monochlorobenzenes; primary amino compound | central nervous system depressant; GABA agonist; muscle relaxant |
| isoguvacine isoguvacine: A GABA agonist; RN given refers to parent cpd; structure | 1.99 | 1 | 0 | tetrahydropyridine | |
| oxidopamine Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.. oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease). | 2.03 | 1 | 0 | benzenetriol; catecholamine; primary amino compound | drug metabolite; human metabolite; neurotoxin |
| 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. | 1.99 | 1 | 0 | organic heterobicyclic compound; organonitrogen heterocyclic compound | |
| valine Valine: A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.. valine : A branched-chain amino acid that consists of glycine in which one of the hydrogens attached to the alpha-carbon is substituted by an isopropyl group.. L-valine : The L-enantiomer of valine. | 2.13 | 1 | 0 | L-alpha-amino acid zwitterion; L-alpha-amino acid; proteinogenic amino acid; pyruvate family amino acid; valine | algal metabolite; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite |
| cyclopentane Cyclopentanes: A group of alicyclic hydrocarbons with the general formula R-C5H9.. cyclopentanes : Cyclopentane and its derivatives formed by substitution. | 2.03 | 1 | 0 | cycloalkane; cyclopentanes; volatile organic compound | non-polar solvent |
| 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. | 2.13 | 1 | 0 | benzylisoquinoline alkaloid; isoquinoline alkaloid; isoquinolines | agrochemical; central nervous system stimulant; GABA-gated chloride channel antagonist; GABAA receptor antagonist; neurotoxin |
| kainic acid Kainic Acid: (2S-(2 alpha,3 beta,4 beta))-2-Carboxy-4-(1-methylethenyl)-3-pyrrolidineacetic acid. Ascaricide obtained from the red alga Digenea simplex. It is a potent excitatory amino acid agonist at some types of excitatory amino acid receptors and has been used to discriminate among receptor types. Like many excitatory amino acid agonists it can cause neurotoxicity and has been used experimentally for that purpose. | 2.01 | 1 | 0 | dicarboxylic acid; L-proline derivative; non-proteinogenic L-alpha-amino acid; pyrrolidinecarboxylic acid | antinematodal drug; excitatory amino acid agonist |
| glutamic acid Glutamic Acid: A non-essential amino acid naturally occurring in the L-form. Glutamic acid is the most common excitatory neurotransmitter in the CENTRAL NERVOUS SYSTEM.. glutamic acid : An alpha-amino acid that is glutaric acid bearing a single amino substituent at position 2. | 1.99 | 1 | 0 | glutamic acid; glutamine family amino acid; L-alpha-amino acid; proteinogenic amino acid | Escherichia coli metabolite; ferroptosis inducer; micronutrient; mouse metabolite; neurotransmitter; nutraceutical |
| substance p [no description available] | 1.99 | 1 | 0 | peptide | neurokinin-1 receptor agonist; neurotransmitter; vasodilator agent |
| Arbaclofen [no description available] | 1.99 | 1 | 0 | organonitrogen compound; organooxygen compound | |
| colforsin Colforsin: Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland. | 2.03 | 1 | 0 | acetate ester; cyclic ketone; labdane diterpenoid; organic heterotricyclic compound; tertiary alpha-hydroxy ketone; triol | adenylate cyclase agonist; anti-HIV agent; antihypertensive agent; plant metabolite; platelet aggregation inhibitor; protein kinase A agonist |
| bicuculline methiodide [no description available] | 2.13 | 1 | 0 | ||
| cgp 35348 CGP 35348: antagonizes both GABA-A and GABA-B receptors | 1.99 | 1 | 0 | ||
| saclofen saclofen: GABA-A receptor antagonist | 1.99 | 1 | 0 | organochlorine compound | |
| zd 7288 ICI D2788: a sinoatrial node modulator; may be of use in treatment of ischaemic heart disease by increasing heart rate without impairing cardiac function | 2.13 | 1 | 0 | ||
| 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) | 2.69 | 3 | 0 | ||
| cgp 52432 [no description available] | 1.99 | 1 | 0 | dichlorobenzene | |
| cgp 54626 CGP 54626: RN given for (S-(R*,R*))-isomer | 1.99 | 1 | 0 | ||
| cgp 62349 [no description available] | 1.99 | 1 | 0 | ||
| cgp 64213 CGP 64213: structure in first source | 1.99 | 1 | 0 | ||
| cgp 71872 CGP 71872: structure in first source | 1.99 | 1 | 0 | ||
| 3-aminopropylphosphinic acid 3-aminopropylphosphinic acid: structure given in first source; selective GABA receptor agonist | 1.99 | 1 | 0 | ||
| n,n'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine: structure in first source | 2.03 | 1 | 0 | aryl sulfide | |
| cgp 55845a CGP 55845A: GABA-B receptor antagonist; RN refers to cpd with no isomeric designation; CGP 55845 is the (1S,2S)-isomer | 1.99 | 1 | 0 | ||
| sodium oxybate Sodium Oxybate: The sodium salt of 4-hydroxybutyric acid. It is used for both induction and maintenance of ANESTHESIA. | 2.03 | 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. | 1.99 | 1 | 0 | ||
| cardiovascular agents Cardiovascular Agents: Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume. | 2.13 | 1 | 0 |
| Condition | Indicated | Relationship Strength | Studies | Trials |
|---|---|---|---|---|
| Aura [description not available] | 0 | 2.43 | 2 | 0 |
| Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time. | 0 | 2.05 | 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 | 2.43 | 2 | 0 |
| Hyperactivity, Motor [description not available] | 0 | 2.07 | 1 | 0 |
| Absence Seizure [description not available] | 0 | 2.93 | 4 | 0 |
| Encephalitis, Limbic [description not available] | 0 | 2.07 | 1 | 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 | 2.93 | 4 | 0 |
| Autosomal Dominant Juvenile Parkinson Disease [description not available] | 0 | 2.03 | 1 | 0 |
| Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases. | 0 | 2.03 | 1 | 0 |
| Parkinsonian Disorders A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA. | 0 | 2.03 | 1 | 0 |
| Disease Exacerbation [description not available] | 0 | 2.04 | 1 | 0 |
| Absence Seizure Disorder [description not available] | 0 | 2.4 | 2 | 0 |
| Epilepsy, Absence A seizure disorder usually occurring in childhood characterized by rhythmic electrical brain discharges of generalized onset. Clinical features include a sudden cessation of ongoing activity usually without loss of postural tone. Rhythmic blinking of the eyelids or lip smacking frequently accompanies the SEIZURES. The usual duration is 5-10 seconds, and multiple episodes may occur daily. Juvenile absence epilepsy is characterized by the juvenile onset of absence seizures and an increased incidence of myoclonus and tonic-clonic seizures. (Menkes, Textbook of Child Neurology, 5th ed, p736) | 0 | 2.4 | 2 | 0 |