pitolisant profile

pitolisant: functions as both inverse agonist and antagonist of histamine H3 receptors; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	9948102
CHEMBL ID	462605
CHEBI ID	134709
SCHEMBL ID	117648
MeSH ID	M0506516

Synonym
HY-12199
pitolisant
CHEBI:134709
1-(3-(3-(4-chlorophenyl)propoxy)propyl)piperidine
bdbm50247053
1-[3-[3-(4-chlorophenyl)propoxy]propyl]piperidine
CHEMBL462605 ,
bf-2.649
bf-2649
bf2.649
hbs-101
tiprolisant
4bc83l4piy ,
362665-56-3
unii-4bc83l4piy
wakix
pitolisant [usan:inn]
CS-0666
piperidine, 1-[3-[3-(4-chlorophenyl)propoxy]propyl]-
3-(4-chlorophenyl)propyl 3-piperidinopropyl ether
1-{3-[3-(4-chlorophenyl)propoxy]propyl}piperidine
pitolisant [who-dd]
pitolisant [inn]
piperidine, 1-(3-(3-(4-chlorophenyl)propoxy)propyl)-
pitolisant [mi]
pitolisant [usan]
NNACHAUCXXVJSP-UHFFFAOYSA-N
1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidine
SCHEMBL117648
pitolisant (bf2.649)
D10749
pitolisant (usan/inn)
gtpl8924
ozawade
tiprolisant [usan]
AKOS028108820
1-[3-[3-(4-chlorophenyl)propoxy]propyl]-piperidinehydrochloride
EX-A3601
Q426044
DB11642
mfcd18782650
BCP13114
tirolisant
bf2649; bf-2649; bf 2649; pitolisant
SB17037
HMS3743C05
NCGC00370823-03
DTXSID30957654
AS-57273
A855975
EN300-7385525
pitolisantum
n07xx11

Excerpt	Reference	Relevance
"Pitolisant is an orally active selective histamine H3 receptor (H3R) antagonist/inverse agonist, which enhances histaminergic transmissions in the brain and thereby elicits strong wake-promoting effects."	( Efficacy of Pitolisant 20 mg in Reducing Excessive Daytime Sleepiness and Fatigue in Patients with Obstructive Sleep Apnoea Syndrome: An Individual Patient Data Meta-analysis. Lehert, P, 2022)	1.82
"Pitolisant is a histamine 3-receptor antagonist/inverse agonist effective and safe for the treatment of excessive daytime sleepiness and cataplexy in narcolepsy. "	( Dissociative episode and panic attacks triggered by pitolisant in a narcoleptic patient. Brunetti, V; Della Marca, G; Marano, G; Marotta, J; Mazza, M; Simoncini Malucelli, G, 2023)	2.6
"Pitolisant is a new drug with a different mechanism of action that offers a new treatment option."	( [Real-life WAKE study in narcolepsy patients with cataplexy treated with pitolisant and unresponsive to previous treatments]. Del Río-Villegas, R; Gaig-Ventura, C; Gómez-Barrera, M; Martínez-Orozco, FJ; Romero-Santo Tomás, O; Yébenes-Cortés, M, 2022)	1.67
"Pitolisant is an inverse histamine 3 receptor agonist and has been approved for the treatment of adult narcolepsy with or without cataplexy by EMA and FDA."	( Real-world treatment of pediatric narcolepsy with pitolisant: A retrospective, multicenter study. Kallweit, U; Lecendreux, M; Lieberich, L; Pech de Laclause, A; Pizza, F; Plazzi, G; Rezaei, R; Triller, A; Vandi, S, 2023)	1.88
"Pitolisant is an antagonist/inverse agonist of the histamine H3 autoreceptor."	( Evaluating pitolisant as a narcolepsy treatment option. de Biase, S; Gigli, GL; Pellitteri, G; Valente, M, 2021)	1.73
"Pitolisant is a selective histamine H3-receptor antagonist with wake-promoting effects."	( Pitolisant for Residual Excessive Daytime Sleepiness in OSA Patients Adhering to CPAP: A Randomized Trial. Attali, V; Belev, G; Buyse, B; Dauvilliers, Y; Dokic, D; Fietze, I; Georgiev, O; Lecomte, I; Lecomte, JM; Lévy, P; Partinen, M; Pépin, JL; Schwartz, JC; Tamisier, R; Tiholov, R; Verbraecken, J, 2021)	2.79
"Pitolisant is a novel selective histamine H3 receptor antagonist approved for improving excessive daytime sleepiness."	( Pitolisant versus placebo for excessive daytime sleepiness in narcolepsy and obstructive sleep apnea: A meta-analysis from randomized controlled trials. Chen, G; Gao, H; Li, X; Wang, J; Wang, T; Xu, J; Xu, Z; Yang, S, 2021)	2.79
"Pitolisant is an antagonist/inverse agonist of the human histamine H3 receptor."	( The European Medicines Agency review of pitolisant for treatment of narcolepsy: summary of the scientific assessment by the Committee for Medicinal Products for Human Use. Demolis, P; Emmerich, J; Haas, M; Kollb-Sielecka, M; Markey, G; Salmonson, T, 2017)	1.44
"Pitolisant (Wakix®) is an inverse agonst at the histamine-3 (H3) receptor."	( Pitolisant for the treatment of narcolepsy with or without cataplexy. Bruhn, C, 2016)	2.6
"Pitolisant is a first-in-class new drug currently authorized by the European Medicines Agency to treat narcolepsy with or without cataplexy in adults and with an expanded evaluation for the treatment of neurologic diseases such as Parkinson's disease and epilepsy."	( Profile of pitolisant in the management of narcolepsy: design, development, and place in therapy. Centonze, D; Franco, V; Lo Giudice, T; Romigi, A; Vitrani, G, 2018)	1.59
"Pitolisant (BF2.649) is a nonimidazole histamine 3 receptor antagonist. "	( Exploratory Phase II Trial to Evaluate the Safety and the Antiepileptic Effect of Pitolisant (BF2.649) in Refractory Partial Seizures, Given as Adjunctive Treatment During 3 Months. Biraben, A; Collart Dutilleul, P; Collongues, N; De Seze, J; Hirsch, E; Kahane, P; Ryvlin, P; Schwartz, JC; Semah, F; Vercueil, L, )	1.8
"Pitolisant (Wakix™) is an inverse agonist of the histamine H3 receptor that is being developed by Bioproject. "	( Pitolisant: First Global Approval. Syed, YY, 2016)	3.32
"Pitolisant (BF2.649) is a selective inverse agonist for the histamine H(3) receptor and was developed for the treatment of excessive daytime sleepiness in Parkinson disease, narcolepsy, and schizophrenia. "	( Overdose of the histamine H₃ inverse agonist pitolisant increases thermal pain thresholds. Sander, K; Scholich, K; Schuh, CD; Sisignano, M; Stark, H; Zhang, DD, 2012)	2.08

Excerpt	Reference	Relevance
"Pitolisant treatment resulted in an improvement in narcolepsy symptoms in children, although the UNS was not validated for use in children with narcolepsy when our study began. "	( Safety and efficacy of pitolisant in children aged 6 years or older with narcolepsy with or without cataplexy: a double-blind, randomised, placebo-controlled trial. Caussé, C; Dauvilliers, Y; Franco, P; Lammers, GJ; Lecendreux, M; Lecomte, I; Lecomte, JM; Lehert, P; Plazzi, G; Poluektov, M; Schwartz, JC, 2023)	2.66
"Pitolisant treatment was increased from 10 to 30 mg (n = 1) and 40 mg (n = 3)."	( Pitolisant, an inverse agonist of the histamine H3 receptor: an alternative stimulant for narcolepsy-cataplexy in teenagers with refractory sleepiness. Arnulf, I; Bastuji, H; Franco, P; Inocente, C; Lin, JS; Raoux, A; Reimão, R; Thibault-Stoll, A, )	2.3
"Treatment with pitolisant was well tolerated."	( Real-world treatment of pediatric narcolepsy with pitolisant: A retrospective, multicenter study. Kallweit, U; Lecendreux, M; Lieberich, L; Pech de Laclause, A; Pizza, F; Plazzi, G; Rezaei, R; Triller, A; Vandi, S, 2023)	1.5

Excerpt	Reference	Relevance
" All adverse events were assessed in the safety population, defined as all participants who took at least one dose of study medication."	( Safety and efficacy of pitolisant in children aged 6 years or older with narcolepsy with or without cataplexy: a double-blind, randomised, placebo-controlled trial. Caussé, C; Dauvilliers, Y; Franco, P; Lammers, GJ; Lecendreux, M; Lecomte, I; Lecomte, JM; Lehert, P; Plazzi, G; Poluektov, M; Schwartz, JC, 2023)	1.22
" Treatment-emergent adverse events were reported in 22 (31%) of 72 patients in the pitolisant group and 13 (34%) of 38 patients in the placebo group."	( Safety and efficacy of pitolisant in children aged 6 years or older with narcolepsy with or without cataplexy: a double-blind, randomised, placebo-controlled trial. Caussé, C; Dauvilliers, Y; Franco, P; Lammers, GJ; Lecendreux, M; Lecomte, I; Lecomte, JM; Lehert, P; Plazzi, G; Poluektov, M; Schwartz, JC, 2023)	1.45

Excerpt	Reference	Relevance
" This method was applied to quantify samples obtained from the pharmacokinetic and brain penetration studies in male wistar rats."	( LC-MS/MS method for the determination of pitolisant: application to rat pharmacokinetic and brain penetration studies. Ajjala, DR; Bhyrapuneni, G; Jonnala, MR; Kandikere, V; Muddana, NR; Nirogi, R; Pantangi, HR; Vurimindi, H, 2013)	0.66
"Of the 25 enrolled patients, 24 were included in the pharmacokinetic analysis."	( Pharmacokinetics of pitolisant in children and adolescents with narcolepsy. Duvauchelle, T; Franco, P; Jacqz-Aigrain, E; Lecendreux, M; Plazzi, G; Robert, P; Schwartz, JC, 2020)	0.88

Excerpt	Relevance	Reference
" Treatment lasted 8 weeks: 3 weeks of flexible dosing according to investigator's judgment (10 mg, 20 mg, or 40 mg a day of pitolisant; 100 mg, 200 mg or 400 mg a day of modafinil) followed by 5 weeks of stable dosing."	( Pitolisant versus placebo or modafinil in patients with narcolepsy: a double-blind, randomised trial. Arnulf, I; Bassetti, C; Dauvilliers, Y; Ding, CL; Lammers, GJ; Lecomte, JM; Lehert, P; Mayer, G; Rodenbeck, A; Schwartz, JC, 2013)	2.04
" Treatment lasted for 7 weeks: 3 weeks of flexible dosing decided by investigators according to efficacy and tolerance (5 mg, 10 mg, or 20 mg oral pitolisant), followed by 4 weeks of stable dosing (5 mg, 10 mg, 20 mg, or 40 mg)."	( Safety and efficacy of pitolisant on cataplexy in patients with narcolepsy: a randomised, double-blind, placebo-controlled trial. Dauvilliers, Y; Jankovic, S; Krylov, S; Lecomte, I; Lecomte, JM; Lehert, P; Mikhaylov, V; Poverennova, I; Schwartz, JC; Sonka, K; Szakacs, Z, 2017)	0.97
" Zolpidem has been marketed in new dosage forms that include sublingual tablets and oral spray formulations."	( New pharmacologic agents for insomnia and hypersomnia. Earl, DC; Van Tyle, KM, 2020)	0.56
"Recent advancements in the treatment of insomnia includes agents with novel mechanisms, new indications, and new dosage forms."	( New pharmacologic agents for insomnia and hypersomnia. Earl, DC; Van Tyle, KM, 2020)	0.56
" The dose-response curves showed that the anticonvulsant activity of pitolisant changed in a dose-dependent manner."	( Anticonvulsant activity of the histamine H3 receptor inverse agonist pitolisant in an electrical kindling model of epilepsy. Beheshti, S; Wesal, MW, 2022)	1.19

Class	Description
organochlorine compound	An organochlorine compound is a compound containing at least one carbon-chlorine bond.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus	Potency	31.6228	0.0096	10.5250	35.4813	AID1479145
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Histamine H1 receptor	Homo sapiens (human)	Ki	1.1481	0.0000	0.5110	10.0000	AID1125547
Histamine H3 receptor	Mus musculus (house mouse)	Ki	0.0140	0.0006	0.0181	0.0680	AID1495456
Cholinesterase	Equus caballus (horse)	IC50 (µMol)	8.4100	0.0000	2.2214	9.4000	AID1578229; AID1704812
Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)	IC50 (µMol)	1.7000	0.0009	1.9014	10.0000	AID1633048
Muscarinic acetylcholine receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0117	0.0001	0.6120	3.8019	AID1633040
Histamine H4 receptor	Homo sapiens (human)	Ki	70.0000	0.0006	0.4787	10.0000	AID1125546; AID1359280; AID1729011
Histamine H3 receptor	Cavia porcellus (domestic guinea pig)	Ki	0.0002	0.0001	0.0030	0.0126	AID1615603; AID415431
Histamine H3 receptor	Rattus norvegicus (Norway rat)	Ki	0.0170	0.0001	0.2963	8.5110	AID1387798; AID1495457; AID1729010
Histamine H3 receptor	Homo sapiens (human)	IC50 (µMol)	0.0120	0.0005	0.4668	5.9000	AID389212
Histamine H3 receptor	Homo sapiens (human)	Ki	0.0060	0.0001	0.3399	8.5110	AID1125545; AID1163942; AID1359279; AID1387797; AID1495455; AID1578221; AID1633040; AID1690419; AID1704810; AID1704816; AID1705451; AID1729009; AID1829881; AID1829899; AID1833215; AID1833218; AID353208; AID375698; AID409910; AID415426; AID415429; AID415432; AID516381; AID516504; AID599203
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Histamine H3 receptor	Cavia porcellus (domestic guinea pig)	EC50 (µMol)	0.0015	0.0015	0.7932	1.5849	AID415430
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Histamine H3 receptor	Homo sapiens (human)	Kb	0.0022	0.0002	0.2097	2.0000	AID1690422; AID1690425; AID1690427
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
inflammatory response	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
memory	Histamine H1 receptor	Homo sapiens (human)
visual learning	Histamine H1 receptor	Homo sapiens (human)
regulation of vascular permeability	Histamine H1 receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Histamine H1 receptor	Homo sapiens (human)
regulation of synaptic plasticity	Histamine H1 receptor	Homo sapiens (human)
cellular response to histamine	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H1 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H1 receptor	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by hormone	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of DNA-templated transcription	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion homeostasis	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cardiac muscle contraction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cellular response to xenobiotic stimulus	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane depolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of heart rate by cardiac conduction	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potential	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
positive regulation of potassium ion transmembrane transport	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
negative regulation of potassium ion export across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
potassium ion import across plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inflammatory response	Histamine H4 receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Histamine H4 receptor	Homo sapiens (human)
biological_process	Histamine H4 receptor	Homo sapiens (human)
regulation of MAPK cascade	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H4 receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H4 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H4 receptor	Homo sapiens (human)
neurotransmitter secretion	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Histamine H3 receptor	Homo sapiens (human)
chemical synaptic transmission	Histamine H3 receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
histamine receptor activity	Histamine H1 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H1 receptor	Homo sapiens (human)
neurotransmitter receptor activity	Histamine H1 receptor	Homo sapiens (human)
transcription cis-regulatory region binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
delayed rectifier potassium channel activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
ubiquitin protein ligase binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
identical protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
protein homodimerization activity	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
C3HC4-type RING finger domain binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
scaffold protein binding	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
histamine receptor activity	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H4 receptor	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Histamine H4 receptor	Homo sapiens (human)
histamine receptor activity	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Histamine H3 receptor	Homo sapiens (human)
G protein-coupled serotonin receptor activity	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytosol	Histamine H1 receptor	Homo sapiens (human)
plasma membrane	Histamine H1 receptor	Homo sapiens (human)
synapse	Histamine H1 receptor	Homo sapiens (human)
dendrite	Histamine H1 receptor	Homo sapiens (human)
plasma membrane	Histamine H1 receptor	Homo sapiens (human)
virion membrane	Spike glycoprotein	Severe acute respiratory syndrome-related coronavirus
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
cell surface	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
perinuclear region of cytoplasm	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
voltage-gated potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
inward rectifier potassium channel complex	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Potassium voltage-gated channel subfamily H member 2	Homo sapiens (human)
plasma membrane	Histamine H4 receptor	Homo sapiens (human)
plasma membrane	Histamine H4 receptor	Homo sapiens (human)
dendrite	Histamine H4 receptor	Homo sapiens (human)
synapse	Histamine H4 receptor	Homo sapiens (human)
plasma membrane	Histamine H3 receptor	Homo sapiens (human)
presynapse	Histamine H3 receptor	Homo sapiens (human)
plasma membrane	Histamine H3 receptor	Homo sapiens (human)
synapse	Histamine H3 receptor	Homo sapiens (human)
dendrite	Histamine H3 receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Assay ID	Title	Year	Journal	Article
AID353208	Displacement of [125I]iodoproxyfan from human histamine H3 receptor expressed in HEL293 cells	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Fluorinated non-imidazole histamine H3 receptor antagonists.
AID599203	Displacement of [3H]N-alpha-methylhistamine from human histamine H3 receptor expressed in SK-N-MC cells	2009	European journal of medicinal chemistry, Nov, Volume: 44, Issue:11	Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.
AID1633048	Inhibition of human ERG expressed in CHO cells at holding potential of -90 mV by patch clamp method
AID1633040	Displacement of [3H]-N-alpha-methylhistamine from human recombinant full length H3R expressed in HEK293 cell membranes incubated for 90 mins by liquid scintillation counting method
AID1704815	Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI cells at 1 uM using p-tyramine as substrate by fluorometric assay relative to control
AID415429	Displacement of [125I]Iodoproxyfran from human histamine H3 receptor expressed in CHO-K1 cells	2009	Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8	Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
AID1495455	Displacement of [125I]-iodoproxyfan from human striatal full length H3 receptor after 60 mins by gamma counting method
AID1359280	Inhibition of human H4 receptor	2018	European journal of medicinal chemistry, May-25, Volume: 152	Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H
AID1359272	Reversal of RAMH-induced dipsogenia in Krf:(WI) WU rat assessed as inhibition of drinking response at 1.25 mg/kg, ip pretreated for 30 mins followed by RAMH stimulation for 20 mins measured for 30 mins relative to control	2018	European journal of medicinal chemistry, May-25, Volume: 152	Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H
AID415426	Displacement of [125I]Iodoproxyfran from human histamine H3 receptor expressed in HEK293 cells	2009	Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8	Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
AID1615603	Inhibition of Guinea Pig Ileum H3R	2019	European journal of medicinal chemistry, Nov-01, Volume: 181	Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
AID1833218	Antagonist activity at histamine H3 receptor (unknown origin)	2021	Bioorganic & medicinal chemistry, 11-15, Volume: 50	Histamine H
AID1690420	Displacement of bodilisant from recombinant human histamine H3 receptor stably transfected in HEK-293T cells membrane at 1 to 10 uM incubated for 60 mins by fluorescence-polarization assay	2020	European journal of medicinal chemistry, Apr-01, Volume: 191	Novel pyrrolidinone derivative lacks claimed histamine H
AID516381	Displacement of [125I]Iodoproxyfan from human histamine H3 receptor expressed in HEK293 cells	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.
AID409912	Antagonist activity at histamine H3 receptor in po dosed Swiss mouse cerebral cortex assessed as Ntau-methylhistamine level after 90 mins by radioimmunoassay	2008	Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18	Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
AID1125545	Displacement of [3H]N-alpha-methylhistamine from human H3 receptor expressed in HEK-293 cell membrane after 90 mins by liquid scintillation counting analysis	2014	European journal of medicinal chemistry, Apr-22, Volume: 77	Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.
AID1495456	Displacement of [125I]-iodoproxyfan from mouse brain cortex H3 receptor after 60 mins by gamma counting method
AID415427	Binding affinity to histamine H3 receptor in rat cerebral cortex	2009	Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8	Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
AID1729011	Binding affinity to human H4R	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Structural modifications in the distal, regulatory region of histamine H
AID1690419	Displacement of [3H]Nalpha-methylhistamine from recombinant human histamine H3 receptor stably transfected in HEK-293T cells membrane incubated for 90 mins by scintillation counting method	2020	European journal of medicinal chemistry, Apr-01, Volume: 191	Novel pyrrolidinone derivative lacks claimed histamine H
AID415430	Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay	2009	Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8	Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
AID1704814	Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI cells at 1 uM using p-tyramine as substrate by fluorometric assay relative to control
AID1705451	Antagonist activity at recombinant human H3 receptor expressed in CHO-K1 cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay	2020	European journal of medicinal chemistry, Nov-01, Volume: 205	New drug approvals for 2019: Synthesis and clinical applications.
AID1387799	Antiinflammatory activity in po dosed mouse brain assessed as activation in HA release measured after 90 mins
AID1704816	Displacement of [3H]N-alpha-Methylhistamine from recombinant human histamine H3 receptor expressed in human HEK293 cells incubated for 90 mins by microbeta scintillation analysis
AID1578228	Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate at 10 uM preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method relative to control	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Search for new multi-target compounds against Alzheimer's disease among histamine H
AID1387797	Binding affinity to human histamine H3 receptor
AID389212	Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding	2008	Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21	Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
AID415433	Activity at histamine H3 receptor in po dosed mouse by central H3R receptor assay	2009	Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8	Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
AID415431	Antagonist activity at human histamine H3 receptor expressed in HEK293 cells by [35S]GTPgammaS binding assay	2009	Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8	Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
AID415428	Antagonist activity at histamine H3 receptor in isolated guinea pig ileum	2009	Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8	Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
AID1729010	Binding affinity to rat H3R	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Structural modifications in the distal, regulatory region of histamine H
AID1704810	Displacement of [3H]N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cells by microbeta scintillation analysis
AID415432	Displacement of [125I]Iodoproxyfran from human histamine H3 receptor expressed in rat C6 cells	2009	Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8	Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
AID1829899	Binding affinity in Nluc-hH3R assessed in HEK293T cells by NanoBRET binding assay	2021	Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15	A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H
AID1125549	Anticonvulsant activity in Wistar rat assessed as protection against maximal electroshock-induced convulsions at 10 mg/kg, ip administered 30 mins before MES challenge	2014	European journal of medicinal chemistry, Apr-22, Volume: 77	Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.
AID1633043	Reversal of RAMH-induced dipsogenia in Wistar rat (Krf:(WI) WU) assessed as inhibition of RAMH-induced drinking response at 1.25 mg/kg, ip pretreated for 30 mins followed by RAMH stimulation for 20 mins and measured for 30 mins
AID375698	Antagonist activity at human histamine H3 receptor expressed in HEK293 cells by [35S]gammaS binding assay	2009	Journal of medicinal chemistry, Jul-09, Volume: 52, Issue:13	5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.
AID1163942	Displacement of [3H]N-alpha-Methylhistamine from human recombinant H3 receptor expressed in HEK293 cells by competitive binding assay	2014	European journal of medicinal chemistry, Oct-30, Volume: 86	Studies on molecular properties prediction and histamine H3 receptor affinities of novel ligands with uracil-based motifs.
AID1578221	Displacement of [3H]-N-alpha-methylhistamine from human histamine H3 receptor stably expressed in HEK293 cell membrane after 90 mins	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Search for new multi-target compounds against Alzheimer's disease among histamine H
AID1597727	Half life in human at 18 to 36 mg	2019	Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16	Sleep modulating agents.
AID1125546	Displacement of [3H]histamine from human H4 receptor expressed in Sf9 cell membrane co-transfected with Galphai2 and Gbeta1gamma2 after 60 mins by liquid scintillation counting analysis	2014	European journal of medicinal chemistry, Apr-22, Volume: 77	Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.
AID1387798	Binding affinity to rat histamine H3 receptor
AID1704812	Inhibition of equine serum BChE using BTCI as substrate incubated for 5 mins followed by substrate addition and measured after 5 mins by spectrophotometric based Ellman's method
AID1690422	Antagonist activity at human H3 receptor expressed in HEK293 cells assessed as reversion of (R)alpha-MeHA induced activity preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting method	2020	European journal of medicinal chemistry, Apr-01, Volume: 191	Novel pyrrolidinone derivative lacks claimed histamine H
AID1359279	Inhibition of human H3 receptor	2018	European journal of medicinal chemistry, May-25, Volume: 152	Synthesis and biological activity of novel tert-butyl and tert-pentylphenoxyalkyl piperazine derivatives as histamine H
AID1495457	Displacement of [125I]-iodoproxyfan from rat brain cortex H3 receptor after 60 mins by gamma counting method
AID1495361	In vivo antagonist activity at H3 receptor in RAMH-induced dipsogenic Wistar (Krf:(WI) WU) rat model assessed as inhibition of RAMH-water intake at 1.25 mg/kg, ip administered 30 mins prior to RAMH induction
AID1578225	Inhibition of electric eel AChE using acetylthiocholine iodide as substrate at 10 uM preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method relative to control	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Search for new multi-target compounds against Alzheimer's disease among histamine H
AID409910	Displacement of [125I]iodoproxyfan from human recombinant histamine H3 receptor expressed in CHO-K1 cells	2008	Bioorganic & medicinal chemistry, Sep-15, Volume: 16, Issue:18	Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
AID1690427	Antagonist activity at human H3 receptor expressed in CHO cells assessed as decrease in cAMP accumulation by measuring increase in forskolin level incubated for 4 hrs in presence of histamine by CRE/MRE-luciferase reporter gene assay	2020	European journal of medicinal chemistry, Apr-01, Volume: 191	Novel pyrrolidinone derivative lacks claimed histamine H
AID353209	In vivo histamine H3 receptor potency in po dosed Swiss mouse assessed as N'-methylhistamine level	2009	Bioorganic & medicinal chemistry letters, Apr-15, Volume: 19, Issue:8	Fluorinated non-imidazole histamine H3 receptor antagonists.
AID1829881	Binding affinity in Nluc-hH3R assessed in HEK293 cells by NanoBRET binding assay	2021	Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15	A Versatile Sub-Nanomolar Fluorescent Ligand Enables NanoBRET Binding Studies and Single-Molecule Microscopy at the Histamine H
AID1690425	Antagonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as decrease in cAMP accumulation by measuring increase in forskolin level in presence of histamine by HitHunter-cAMP assay	2020	European journal of medicinal chemistry, Apr-01, Volume: 191	Novel pyrrolidinone derivative lacks claimed histamine H
AID516504	Displacement of [125I]iodoproxyfan human histamine H3 receptor	2010	Bioorganic & medicinal chemistry letters, Oct-01, Volume: 20, Issue:19	Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.
AID1729009	Binding affinity to human H3R	2021	European journal of medicinal chemistry, Mar-05, Volume: 213	Structural modifications in the distal, regulatory region of histamine H
AID599205	Antagonist activity at human histamine H3 receptor expressed in SK-N-MC cells assessed as inhibition of forskolin stimulated cAMP accumulation after 6 hrs	2009	European journal of medicinal chemistry, Nov, Volume: 44, Issue:11	Heterocyclic replacement of the central phenyl core of diamine-based histamine H3 receptor antagonists.
AID1578229	Inhibition of equine serum BChE using butyrylthiocholine iodide as substrate preincubated with enzyme for 5 mins prior to substrate addition measured after 5 mins by Ellman's method	2020	European journal of medicinal chemistry, Jan-01, Volume: 185	Search for new multi-target compounds against Alzheimer's disease among histamine H
AID1833215	Displacement of [3H]Nalpha-methylhistamine from recombinant human histamine H3 receptor expressed in HEK293 cells incubated for 90 mins by competition binding assay	2021	Bioorganic & medicinal chemistry, 11-15, Volume: 50	Histamine H
AID1125547	Displacement of [3H]pyrilamine from human H1 receptor expressed in CHO cell membrane after 120 mins by liquid scintillation counting analysis	2014	European journal of medicinal chemistry, Apr-22, Volume: 77	Non-imidazole histamine H3 receptor ligands incorporating antiepileptic moieties.
AID1346107	Human H3 receptor (Histamine receptors)	2015	Pharmacological reviews, Jul, Volume: 67, Issue:3	International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
AID1346055	Human H4 receptor (Histamine receptors)	2015	Pharmacological reviews, Jul, Volume: 67, Issue:3	International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
AID1346095	Human H2 receptor (Histamine receptors)	2015	Pharmacological reviews, Jul, Volume: 67, Issue:3	International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
AID1346037	Human H1 receptor (Histamine receptors)	2015	Pharmacological reviews, Jul, Volume: 67, Issue:3	International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.
AID1346107	Human H3 receptor (Histamine receptors)	2009	Bioorganic & medicinal chemistry, Apr-15, Volume: 17, Issue:8	Diether derivatives of homo- or substituted piperidines as non-imidazole histamine H3 receptor ligands.
[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	0 (0.00)	18.2507
2000's	9 (9.68)	29.6817
2010's	44 (47.31)	24.3611
2020's	40 (43.01)	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	14 (14.43%)	5.53%
Reviews	24 (24.74%)	6.00%
Case Studies	5 (5.15%)	4.05%
Observational	3 (3.09%)	0.25%
Other	51 (52.58%)	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
adenine [no description available]	4.61	1	1	6-aminopurines; purine nucleobase	Daphnia magna metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
ammonium hydroxide azane : Saturated acyclic nitrogen hydrides having the general formula NnHn+2.	4.61	1	1	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
carbamates [no description available]	5.72	6	0	amino-acid anion
methane Methane: The simplest saturated hydrocarbon. It is a colorless, flammable gas, slightly soluble in water. It is one of the chief constituents of natural gas and is formed in the decomposition of organic matter. (Grant & Hackh's Chemical Dictionary, 5th ed). methane : A one-carbon compound in which the carbon is attached by single bonds to four hydrogen atoms. It is a colourless, odourless, non-toxic but flammable gas (b.p. -161degreeC).	4.61	1	1	alkane; gas molecular entity; mononuclear parent hydride; one-carbon compound	bacterial metabolite; fossil fuel; greenhouse gas
citric acid, anhydrous Citric Acid: A key intermediate in metabolism. It is an acid compound found in citrus fruits. The salts of citric acid (citrates) can be used as anticoagulants due to their calcium chelating ability.. citric acid : A tricarboxylic acid that is propane-1,2,3-tricarboxylic acid bearing a hydroxy substituent at position 2. It is an important metabolite in the pathway of all aerobic organisms.	4.61	1	1	tricarboxylic acid	antimicrobial agent; chelator; food acidity regulator; fundamental metabolite
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.	2.31	1	0	catechols; dihydroxyphenylacetic acid	human metabolite
glycerol Moon: The natural satellite of the planet Earth. It includes the lunar cycles or phases, the lunar month, lunar landscapes, geography, and soil.	4.61	1	1	alditol; triol	algal metabolite; detergent; Escherichia coli metabolite; geroprotector; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; solvent
histamine [no description available]	5.92	6	1	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
hydrogen Hydrogen: The first chemical element in the periodic table with atomic symbol H, and atomic number 1. Protium (atomic weight 1) is by far the most common hydrogen isotope. Hydrogen also exists as the stable isotope DEUTERIUM (atomic weight 2) and the radioactive isotope TRITIUM (atomic weight 3). Hydrogen forms into a diatomic molecule at room temperature and appears as a highly flammable colorless and odorless gas.. dihydrogen : An elemental molecule consisting of two hydrogens joined by a single bond.	4.61	1	1	elemental hydrogen; elemental molecule; gas molecular entity	antioxidant; electron donor; food packaging gas; fuel; human metabolite
nitrates Nitrates: Inorganic or organic salts and esters of nitric acid. These compounds contain the NO3- radical.	4.61	1	1	monovalent inorganic anion; nitrogen oxoanion; reactive nitrogen species
nitrites Nitrites: Salts of nitrous acid or compounds containing the group NO2-. The inorganic nitrites of the type MNO2 (where M=metal) are all insoluble, except the alkali nitrites. The organic nitrites may be isomeric, but not identical with the corresponding nitro compounds. (Grant & Hackh's Chemical Dictionary, 5th ed)	4.61	1	1	monovalent inorganic anion; nitrogen oxoanion; reactive nitrogen species	human metabolite
propylene glycol Propylene Glycol: A clear, colorless, viscous organic solvent and diluent used in pharmaceutical preparations.. propane-1,2-diol : The simplest member of the class of propane-1,2-diols, consisting of propane in which a hydrogen at position 1 and a hydrogen at position 2 are substituted by hydroxy groups. A colourless, viscous, hygroscopic, low-melting (-59degreeC) and high-boiling (188degreeC) liquid with low toxicity, it is used as a solvent, emulsifying agent, and antifreeze.	4.61	1	1	glycol; propane-1,2-diols	allergen; human xenobiotic metabolite; mouse metabolite; protic solvent
sulfur dioxide Sulfur Dioxide: A highly toxic, colorless, nonflammable gas. It is used as a pharmaceutical aid and antioxidant. It is also an environmental air pollutant.	4.61	1	1	sulfur oxide	Escherichia coli metabolite; food bleaching agent; refrigerant
phenytoin [no description available]	2.53	2	0	imidazolidine-2,4-dione	anticonvulsant; drug allergen; sodium channel blocker; teratogenic agent
tacrine Tacrine: A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.. tacrine : A member of the class of acridines that is 1,2,3,4-tetrahydroacridine substituted by an amino group at position 9. It is used in the treatment of Alzheimer's disease.	2.25	1	0	acridines; aromatic amine	EC 3.1.1.7 (acetylcholinesterase) inhibitor
antazoline Antazoline: An antagonist of histamine H1 receptors.. antazoline : A member of the class of imidazolines that is 2-aminomethyl-2-imidazoline in which the exocyclic amino hydrogens are replaced by benzyl and phenyl groups. Antazoline is only found in individuals that have taken the drug.	2.17	1	0	aromatic amine; imidazolines; tertiary amino compound	cholinergic antagonist; H1-receptor antagonist; xenobiotic
betahistine Betahistine: A histamine analog and H1 receptor agonist that serves as a vasodilator. It is used in MENIERE DISEASE and in vascular headaches but may exacerbate bronchial asthma and peptic ulcers.. betahistine : An aminoalkylpyridine that is pyridine substituted by a 2-(methylamino)ethyl group at position 2. It acts as a histamine agonist and a vasodilator, and is thought to improve the microcirculation of the labyrinth, resulting in reduced endolymphatic pressure. It is used (generally as the hydrochloride or mesylate salt) to reduce the symptoms of vertigo, tinnitus, and hearing loss associated with Meniere's disease.	2.05	1	0	aminoalkylpyridine; secondary amino compound	H1-receptor agonist; vasodilator agent
clobenpropit clobenpropit: histamine H3 receptor antagonist. clobenpropit : An imidothiocarbamic ester that consists of isothiourea bearing S-3-(imidazol-4-yl)propyl and N-4-chlorobenzyl substituents. An extremely potent histamine H3 antagonist/inverse agonist (pA2 = 9.93). Also displays partial agonist activity at H4 receptors; induces eosinophil shape change with an EC50 of 3 nM.	3.07	3	0	imidazoles; imidothiocarbamic ester; organochlorine compound	H3-receptor antagonist; H4-receptor agonist
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.	7.31	1	0	primary amine
diphenhydramine Diphenhydramine: A histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations. It has some undesired antimuscarinic and sedative effects.. diphenhydramine : An ether that is the benzhydryl ether of 2-(dimethylamino)ethanol. It is a H1-receptor antagonist used as a antipruritic and antitussive drug.. antitussive : An agent that suppresses cough. Antitussives have a central or a peripheral action on the cough reflex, or a combination of both. Compare with expectorants, which are considered to increase the volume of secretions in the respiratory tract, so facilitating their removal by ciliary action and coughing, and mucolytics, which decrease the viscosity of mucus, facilitating its removal by ciliary action and expectoration.	3.31	1	0	ether; tertiary amino compound	anti-allergic agent; antidyskinesia agent; antiemetic; antiparkinson drug; antipruritic drug; antitussive; H1-receptor antagonist; local anaesthetic; muscarinic antagonist; oneirogen; sedative
donepezil Donepezil: An indan and piperidine derivative that acts as a selective and reversible inhibitor of ACETYLCHOLINESTERASE. Donepezil is highly selective for the central nervous system and is used in the management of mild to moderate DEMENTIA in ALZHEIMER DISEASE.. donepezil : A racemate comprising equimolar amounts of (R)- and (S)-donepezil. A centrally acting reversible acetylcholinesterase inhibitor, its main therapeutic use is in the treatment of Alzheimer's disease where it is used to increase cortical acetylcholine.. 2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxyindan-1-one : A member of the class of indanones that is 5,6-dimethoxyindan-1-one which is substituted at position 2 by an (N-benzylpiperidin-4-yl)methyl group.	2.58	2	0	aromatic ether; indanones; piperidines; racemate	EC 3.1.1.7 (acetylcholinesterase) inhibitor; EC 3.1.1.8 (cholinesterase) inhibitor; nootropic agent
estazolam Estazolam: A benzodiazepine with anticonvulsant, hypnotic, and muscle relaxant properties. It has been shown in some cases to be more potent than DIAZEPAM or NITRAZEPAM.. estazolam : A triazolo[4,3-a][1,4]benzodiazepine having a phenyl group at position 6 and a chloro substituent at position 8. A short-acting benzodiazepine with general properties similar to diazepam, it is given by mouth as a hypnotic in the short-term management of insomnia.	3.31	1	0	triazoles; triazolobenzodiazepine	anticonvulsant; anxiolytic drug; GABA modulator
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.	4.22	2	0	ethyl ester; imidazobenzodiazepine; organofluorine compound	antidote to benzodiazepine poisoning; GABA antagonist
fluoxetine 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.. 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.. 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.	3.31	1	0	(trifluoromethyl)benzenes; aromatic ether; secondary amino compound
gabapentin Gabapentin: A cyclohexane-gamma-aminobutyric acid derivative that is used for the treatment of PARTIAL SEIZURES; NEURALGIA; and RESTLESS LEGS SYNDROME.. gabapentin : A gamma-amino acid that is cyclohexane substituted at position 1 by aminomethyl and carboxymethyl groups. Used for treatment of neuropathic pain and restless legs syndrome.	3.31	1	0	gamma-amino acid	anticonvulsant; calcium channel blocker; environmental contaminant; xenobiotic
haloperidol Haloperidol: A phenyl-piperidinyl-butyrophenone that is used primarily to treat SCHIZOPHRENIA and other PSYCHOSES. It is also used in schizoaffective disorder, DELUSIONAL DISORDERS, ballism, and TOURETTE SYNDROME (a drug of choice) and occasionally as adjunctive therapy in INTELLECTUAL DISABILITY and the chorea of HUNTINGTON DISEASE. It is a potent antiemetic and is used in the treatment of intractable HICCUPS. (From AMA Drug Evaluations Annual, 1994, p279). haloperidol : A compound composed of a central piperidine structure with hydroxy and p-chlorophenyl substituents at position 4 and an N-linked p-fluorobutyrophenone moiety.	2.05	1	0	aromatic ketone; hydroxypiperidine; monochlorobenzenes; organofluorine compound; tertiary alcohol	antidyskinesia agent; antiemetic; dopaminergic antagonist; first generation antipsychotic; serotonergic antagonist
tele-methylhistamine tele-methylhistamine: histamine methyltransferase antagonist. N(tele)-methylhistamine : A primary amino compound that is the N(tele)-methyl derivative of histamine.	2.03	1	0	imidazoles; primary amino compound	human metabolite; mouse metabolite
imetit imetit: structure given in first source. imetit : An imidothiocarbamic ester that consists of isothiourea in which the thiol hydrogen is substituted by a 2-(imidazol-4-yl)ethyl group. An extremely potent, high affinity agonist at H3 and H4 receptors (Ki values are 0.3 and 2.7 nM respectively). Induces shape change in eosinophils with an EC50 of 25 nM. Centrally active following systemic administration.	2.69	2	0	imidazoles; imidothiocarbamic ester	H3-receptor agonist; H4-receptor agonist
isoflurane Isoflurane: A stable, non-explosive inhalation anesthetic, relatively free from significant side effects.	4.61	1	1	organofluorine compound	inhalation anaesthetic
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.	4.61	1	1	cyclohexanones; monochlorobenzenes; secondary amino compound	analgesic; environmental contaminant; intravenous anaesthetic; neurotoxin; NMDA receptor antagonist; xenobiotic
mazindol Mazindol: Tricyclic anorexigenic agent unrelated to and less toxic than AMPHETAMINE, but with some similar side effects. It inhibits uptake of catecholamines and blocks the binding of cocaine to the dopamine uptake transporter.	4.22	2	0	organic molecular entity
memantine [no description available]	4.61	1	1	adamantanes; primary aliphatic amine	antidepressant; antiparkinson drug; dopaminergic agent; neuroprotective agent; NMDA receptor antagonist
methadone Methadone: A synthetic opioid that is used as the hydrochloride. It is an opioid analgesic that is primarily a mu-opioid agonist. It has actions and uses similar to those of MORPHINE. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1082-3). methadone : A racemate comprising equimolar amounts of dextromethadone and levomethadone. It is a opioid analgesic which is used as a painkiller and as a substitute for heroin in the treatment of heroin addiction.. 6-(dimethylamino)-4,4-diphenylheptan-3-one : A ketone that is heptan-3-one substituted by a dimethylamino group at position 6 and two phenyl groups at position 4.	4.61	1	1	benzenes; diarylmethane; ketone; tertiary amino compound
methylphenidate Methylphenidate: A central nervous system stimulant used most commonly in the treatment of ATTENTION DEFICIT DISORDER in children and for NARCOLEPSY. Its mechanisms appear to be similar to those of DEXTROAMPHETAMINE. The d-isomer of this drug is referred to as DEXMETHYLPHENIDATE HYDROCHLORIDE.. methylphenidate : A racemate comprising equimolar amounts of the two threo isomers of methyl phenyl(piperidin-2-yl)acetate. A central stimulant and indirect-acting sympathomimetic, is used (generally as the hydrochloride salt) in the treatment of hyperactivity disorders in children and for the treatment of narcolepsy.. methyl phenyl(piperidin-2-yl)acetate : A amino acid ester that is methyl phenylacetate in which one of the hydrogens alpha to the carbonyl group is replaced by a piperidin-2-yl group.	3.31	1	0	beta-amino acid ester; methyl ester; piperidines
modafinil Modafinil: A benzhydryl acetamide compound, central nervous system stimulant, and CYP3A4 inducing agent that is used in the treatment of NARCOLEPSY and SLEEP WAKE DISORDERS.. modafinil : A racemate comprising equimolar amounts of armodafinil and (S)-modafinil. A central nervous system stimulant, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. The optical enantiomers of modafinil have similar pharmacological actions in animals.. 2-[(diphenylmethyl)sulfinyl]acetamide : A sulfoxide that is dimethylsulfoxide in which two hydrogens attached to one of the methyl groups are replaced by phenyl groups, while one hydrogen attached to the other methyl group is replaced by a carbamoyl (aminocarbonyl) group.	9.88	13	3	monocarboxylic acid amide; sulfoxide
mosapramine mosapramine: structure given in first source. mosapramine : A racemate comprising equimolar amounts of (R)- and (S)-mosapramine. It is a second-generation antipsychotic used for the treatment of schizophrenia.. 1'-[3-(3-chloro-10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)propyl]hexahydro-2H-spiro[imidazo[1,2-a]pyridine-3,4'-piperidin]-2-one : A dibenzoazepine that is 10,11-dihydro-5H-dibenzo[b,f]azepine which is substituted by chlorine at position 3 and in which the hydrogen attached to the nitrogen is replaced by a 3-(2-oxohexahydro-2H-spiro[imidazo[1,2-a]pyridine-3,4'-piperidin]-1'-yl)propyl group.	3.31	1	0	azaspiro compound; dibenzoazepine; organochlorine compound; tertiary amino compound
norfluoxetine norfluoxetine: metabolite of fluoxetine; RN given refers to parent cpd without isomeric designation	3.31	1	0	(trifluoromethyl)benzenes
pyrilamine Pyrilamine: A histamine H1 antagonist. It has mild hypnotic properties and some local anesthetic action and is used for allergies (including skin eruptions) both parenterally and locally. It is a common ingredient of cold remedies.. mepyramine : An ethylenediamine derivative that is ethylenediamine in which one of the amino nitrogens is substituted by two methyl groups and the remaining amino nitrogen is substituted by a 4-methoxybenzyl and a pyridin-2-yl group.	2.13	1	0	aromatic ether; ethylenediamine derivative	H1-receptor antagonist
quetiapine [no description available]	3.31	1	0	dibenzothiazepine; N-alkylpiperazine; N-arylpiperazine	adrenergic antagonist; dopaminergic antagonist; histamine antagonist; second generation antipsychotic; serotonergic antagonist
trazodone Trazodone: A serotonin uptake inhibitor that is used as an antidepressive agent. It has been shown to be effective in patients with major depressive disorders and other subsets of depressive disorders. It is generally more useful in depressive disorders associated with insomnia and anxiety. This drug does not aggravate psychotic symptoms in patients with schizophrenia or schizoaffective disorders. (From AMA Drug Evaluations Annual, 1994, p309). trazodone : An N-arylpiperazine in which one nitrogen is substituted by a 3-chlorophenyl group, while the other is substituted by a 3-(3-oxo[1,2,4]triazolo[4,3-a]pyridin-2(3H)-yl)propyl group.	3.35	1	0	monochlorobenzenes; N-alkylpiperazine; N-arylpiperazine; triazolopyridine	adrenergic antagonist; antidepressant; anxiolytic drug; H1-receptor antagonist; sedative; serotonin uptake inhibitor
venlafaxine venlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-methoxyphenyl group.	3.31	1	0	cyclohexanols; monomethoxybenzene; tertiary alcohol; tertiary amino compound	adrenergic uptake inhibitor; analgesic; antidepressant; dopamine uptake inhibitor; environmental contaminant; serotonin uptake inhibitor; xenobiotic
zaleplon 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. 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.	3.31	1	0	nitrile; pyrazolopyrimidine	anticonvulsant; anxiolytic drug; central nervous system depressant; sedative
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.	4.86	3	0	imidazopyridine	central nervous system depressant; GABA agonist; sedative
corticosterone [no description available]	7.25	1	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
dextroamphetamine Dextroamphetamine: The d-form of AMPHETAMINE. It is a central nervous system stimulant and a sympathomimetic. It has also been used in the treatment of narcolepsy and of attention deficit disorders and hyperactivity in children. Dextroamphetamine has multiple mechanisms of action including blocking uptake of adrenergics and dopamine, stimulating release of monamines, and inhibiting monoamine oxidase. It is also a drug of abuse and a psychotomimetic.. (S)-amphetamine : A 1-phenylpropan-2-amine that has S configuration.	3.31	1	0	1-phenylpropan-2-amine	adrenergic agent; adrenergic uptake inhibitor; dopamine uptake inhibitor; dopaminergic agent; neurotoxin; sympathomimetic agent
sucrose Saccharum: A plant genus of the family POACEAE widely cultivated in the tropics for the sweet cane that is processed into sugar.	2.17	1	0	glycosyl glycoside	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; sweetening agent
apomorphine Apomorphine: A derivative of morphine that is a dopamine D2 agonist. It is a powerful emetic and has been used for that effect in acute poisoning. It has also been used in the diagnosis and treatment of parkinsonism, but its adverse effects limit its use.	2.05	1	0	aporphine alkaloid	alpha-adrenergic drug; antidyskinesia agent; antiparkinson drug; dopamine agonist; emetic; serotonergic drug
phenylalanine Phenylalanine: An essential aromatic amino acid that is a precursor of MELANIN; DOPAMINE; noradrenalin (NOREPINEPHRINE), and THYROXINE.. L-phenylalanine : The L-enantiomer of phenylalanine.. phenylalanine : An aromatic amino acid that is alanine in which one of the methyl hydrogens is substituted by a phenyl group.	5.72	6	0	amino acid zwitterion; erythrose 4-phosphate/phosphoenolpyruvate family amino acid; L-alpha-amino acid; phenylalanine; proteinogenic amino acid	algal metabolite; EC 3.1.3.1 (alkaline phosphatase) inhibitor; Escherichia coli metabolite; human xenobiotic metabolite; micronutrient; mouse metabolite; nutraceutical; plant metabolite; Saccharomyces cerevisiae metabolite
histidine Histidine: An essential amino acid that is required for the production of HISTAMINE.. L-histidine : The L-enantiomer of the amino acid histidine.. histidine : An alpha-amino acid that is propanoic acid bearing an amino substituent at position 2 and a 1H-imidazol-4-yl group at position 3.	4.61	1	1	amino acid zwitterion; histidine; L-alpha-amino acid; polar amino acid zwitterion; proteinogenic amino acid	algal metabolite; Escherichia coli metabolite; human metabolite; micronutrient; mouse metabolite; nutraceutical; Saccharomyces cerevisiae metabolite
ethylene Plastipore: high density polyethylene sponge biocompatible material; used as posts in dental bridges	4.61	1	1	alkene; gas molecular entity	plant hormone; refrigerant
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.	2.05	1	0	benzenes; piperidines	anaesthetic; neurotoxin; NMDA receptor antagonist; psychotropic drug
quinoxalines quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.	4.61	1	1	mancude organic heterobicyclic parent; naphthyridine; ortho-fused heteroarene
caprolactam Caprolactam: Cyclic amide of caproic acid used in manufacture of synthetic fibers of the polyamide type. Can cause local irritation.. epsilon-caprolactam : A member of the class of caprolactams that is azepane substituted by an oxo group at position 2.	4.61	1	1	caprolactams	human blood serum metabolite
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	2.13	1	0	pyrrole; secondary amine
thiophenes Thiophenes: A monocyclic heteroarene furan in which the oxygen atom is replaced by a sulfur.. thiophenes : Compounds containing at least one thiophene ring.	4.61	1	1	mancude organic heteromonocyclic parent; monocyclic heteroarene; thiophenes; volatile organic compound	non-polar solvent
isopropyl myristate isopropyl myristate: used for microemulsions; structure	4.61	1	1	fatty acid ester
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.	2.13	1	0	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines
benzoxazoles 1,3-benzoxazole : A benzoxazole in which the benzene ring is fused to a 1,3-oxazole ring across positions 4 and 5.. benzoxazole : Compounds based on a fused 1,2- or 1,3-oxazole and benzene bicyclic ring skeleton.	4.61	1	1	1,3-benzoxazoles; mancude organic heterobicyclic parent
thiazoles [no description available]	4.61	1	1	1,3-thiazoles; mancude organic heteromonocyclic parent; monocyclic heteroarene
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.	3.47	1	1	dicarboxylic acid; L-proline derivative; non-proteinogenic L-alpha-amino acid; pyrrolidinecarboxylic acid	antinematodal drug; excitatory amino acid agonist
methamphetamine Methamphetamine: A central nervous system stimulant and sympathomimetic with actions and uses similar to DEXTROAMPHETAMINE. The smokable form is a drug of abuse and is referred to as crank, crystal, crystal meth, ice, and speed.. methamphetamine : A member of the class of amphetamines in which the amino group of (S)-amphetamine carries a methyl substituent.	2.05	1	0	amphetamines; secondary amine	central nervous system stimulant; environmental contaminant; neurotoxin; psychotropic drug; xenobiotic
muscone muscone: structure in first source	4.61	1	1
deoxycytidine [no description available]	4.61	1	1	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
1,2-epoxyhexane [no description available]	4.61	1	1
n-methylaspartate N-Methylaspartate: An amino acid that, as the D-isomer, is the defining agonist for the NMDA receptor subtype of glutamate receptors (RECEPTORS, NMDA).. N-methyl-D-aspartic acid : An aspartic acid derivative having an N-methyl substituent and D-configuration.	2.08	1	0	amino dicarboxylic acid; D-alpha-amino acid; D-aspartic acid derivative; secondary amino compound	neurotransmitter agent
silver Silver: An element with the atomic symbol Ag, atomic number 47, and atomic weight 107.87. It is a soft metal that is used medically in surgical instruments, dental prostheses, and alloys. Long-continued use of silver salts can lead to a form of poisoning known as ARGYRIA.	4.61	1	1	copper group element atom; elemental silver	Escherichia coli metabolite
thulium Thulium: An element of the rare earth family of metals. It has the atomic symbol Tm, atomic number 69, and atomic weight 168.93.	4.61	1	1	f-block element atom; lanthanoid atom
titanium Titanium: A dark-gray, metallic element of widespread distribution but occurring in small amounts with atomic number, 22, atomic weight, 47.867 and symbol, Ti; specific gravity, 4.5; used for fixation of fractures.	4.61	1	1	titanium group element atom
uranium Uranium: A radioactive element of the actinide series of metals. It has an atomic symbol U, atomic number 92, and atomic weight 238.03. U-235 is used as the fissionable fuel in nuclear weapons and as fuel in nuclear power reactors.	4.61	1	1	actinoid atom; f-block element atom; monoatomic uranium
galactose aldohexose : A hexose with a (potential) aldehyde group at one end.	4.61	1	1
ozone Ozone: The unstable triatomic form of oxygen, O3. It is a powerful oxidant that is produced for various chemical and industrial uses. Its production is also catalyzed in the ATMOSPHERE by ULTRAVIOLET RAY irradiation of oxygen or other ozone precursors such as VOLATILE ORGANIC COMPOUNDS and NITROGEN OXIDES. About 90% of the ozone in the atmosphere exists in the stratosphere (STRATOSPHERIC OZONE).. ozone : An elemental molecule with formula O3. An explosive, pale blue gas (b.p. -112degreeC) that has a characteristic, pungent odour, it is continuously produced in the upper atmosphere by the action of solar ultraviolet radiation on atmospheric oxygen. It is an antimicrobial agent used in the production of bottled water, as well as in the treatment of meat, poultry and other foodstuffs.	4.61	1	1	elemental molecule; gas molecular entity; reactive oxygen species; triatomic oxygen	antiseptic drug; disinfectant; electrophilic reagent; greenhouse gas; mutagen; oxidising agent; tracer
l-amphetamine (R)-amphetamine : A 1-phenylpropan-2-amine that has R configuration.	3.31	1	0	1-phenylpropan-2-amine
paclitaxel Taxus: Genus of coniferous yew trees or shrubs, several species of which have medicinal uses. Notable is the Pacific yew, Taxus brevifolia, which is used to make the anti-neoplastic drug taxol (PACLITAXEL).	4.61	1	1	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
Arbaclofen [no description available]	3.31	1	0	organonitrogen compound; organooxygen compound
alpidem [no description available]	3.31	1	0	imidazoles
gemcitabine gemcitabine : A 2'-deoxycytidine having geminal fluoro substituents in the 2'-position. An inhibitor of ribonucleotide reductase, gemcitabine is used in the treatment of various carcinomas, particularly non-small cell lung cancer, pancreatic cancer, bladder cancer and breast cancer.	4.61	1	1	organofluorine compound; pyrimidine 2'-deoxyribonucleoside	antimetabolite; antineoplastic agent; antiviral drug; DNA synthesis inhibitor; EC 1.17.4.1 (ribonucleoside-diphosphate reductase) inhibitor; environmental contaminant; immunosuppressive agent; photosensitizing agent; prodrug; radiosensitizing agent; xenobiotic
venlafaxine hydrochloride Venlafaxine Hydrochloride: A cyclohexanol and phenylethylamine derivative that functions as a SEROTONIN AND NORADRENALINE REUPTAKE INHIBITOR (SNRI) and is used as an ANTIDEPRESSIVE AGENT.	3.25	1	0	hydrochloride
baicalin [no description available]	4.61	1	1	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
1h-imidazo(4,5-b)pyridine 1H-imidazo(4,5-b)pyridine: structure given in first source. 4-azabenzimidazole : The [4,5-b]-fused isomer of imidazopyridine.	3.31	1	0	imidazopyridine
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.	3.35	1	0	1,2,3-triazole
dapoxetine [no description available]	4.61	1	1	naphthalenes
voriconazole Voriconazole: A triazole antifungal agent that specifically inhibits STEROL 14-ALPHA-DEMETHYLASE and CYTOCHROME P-450 CYP3A.. voriconazole : A triazole-based antifungal agent used for the treatment of esophageal candidiasis, invasive pulmonary aspergillosis, and serious fungal infections caused by Scedosporium apiospermum and Fusarium spp. It is an inhibitor of cytochrome P450 2C9 (CYP2C9) and CYP3A4.	4.61	1	1	conazole antifungal drug; difluorobenzene; pyrimidines; tertiary alcohol; triazole antifungal drug	P450 inhibitor
imidazo(1,2-a)pyridine imidazo(1,2-a)pyridine: structure	3.31	1	0
clarithromycin Clarithromycin: A semisynthetic macrolide antibiotic derived from ERYTHROMYCIN that is active against a variety of microorganisms. It can inhibit PROTEIN SYNTHESIS in BACTERIA by reversibly binding to the 50S ribosomal subunits. This inhibits the translocation of aminoacyl transfer-RNA and prevents peptide chain elongation.. clarithromycin : The 6-O-methyl ether of erythromycin A, clarithromycin is a macrolide antibiotic used in the treatment of respiratory-tract, skin and soft-tissue infections. It is also used to eradicate Helicobacter pylori in the treatment of peptic ulcer disease. It prevents bacteria from growing by interfering with their protein synthesis.	4.22	2	0	macrolide antibiotic	antibacterial drug; environmental contaminant; protein synthesis inhibitor; xenobiotic
nicotine (S)-nicotine : A 3-(1-methylpyrrolidin-2-yl)pyridine in which the chiral centre has S-configuration. The naturally occurring and most active enantiomer of nicotine, isolated from Nicotiana tabacum.	4.61	1	1	3-(1-methylpyrrolidin-2-yl)pyridine	anxiolytic drug; biomarker; immunomodulator; mitogen; neurotoxin; nicotinic acetylcholine receptor agonist; peripheral nervous system drug; phytogenic insecticide; plant metabolite; psychotropic drug; teratogenic agent; xenobiotic
sk&f 95282 zolantidine: structure given in first source	2.13	1	0	piperidines
lopinavir [no description available]	4.61	1	1	amphetamines; dicarboxylic acid diamide	anticoronaviral agent; antiviral drug; HIV protease inhibitor
sr141716 [no description available]	2.31	1	0	amidopiperidine; carbohydrazide; dichlorobenzene; monochlorobenzenes; pyrazoles	anti-obesity agent; appetite depressant; CB1 receptor antagonist
1,n(6)-ethenoadenine 1,N(6)-ethenoadenine: biologically active fluorescent derivatives of this cpd potentially valuable in studies concerning interactions between adenine cpds & various enzymes for which they serve as substrates or co-factors; structure	4.61	1	1	imidazo[2,1-i]purine	mutagen
thiamethoxam Thiamethoxam: A nitro-oxazine and thiazole derivative that is used as a broad spectrum neonicotinoid insecticide.. thiamethoxam : An oxadiazane that is tetrahydro-N-nitro-4H-1,3,5-oxadiazin-4-imine bearing (2-chloro-1,3-thiazol-5-yl)methyl and methyl substituents at positions 3 and 5 respectively.	4.61	1	1	1,3-thiazoles; 2-nitroguanidine derivative; organochlorine compound; oxadiazane	antifeedant; carcinogenic agent; environmental contaminant; neonicotinoid insectide; xenobiotic
peroxynitrous acid Peroxynitrous Acid: A potent oxidant synthesized by the cell during its normal metabolism. Peroxynitrite is formed from the reaction of two free radicals, NITRIC OXIDE and the superoxide anion (SUPEROXIDES).	4.61	1	1	nitrogen oxoacid
imatinib mesylate imatinib methanesulfonate : A methanesulfonate (mesylate) salt that is the monomesylate salt of imatinib. Used for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.	4.61	1	1	methanesulfonate salt	anticoronaviral agent; antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor
gefitinib [no description available]	4.61	1	1	aromatic ether; monochlorobenzenes; monofluorobenzenes; morpholines; quinazolines; secondary amino compound; tertiary amino compound	antineoplastic agent; epidermal growth factor receptor antagonist
desvenlafaxine O-desmethylvenlafaxine : A tertiary amino compound that is N,N-dimethylethanamine substituted at position 1 by a 1-hydroxycyclohexyl and 4-hydroxyphenyl group. It is a metabolite of the drug venlafaxine.	3.31	1	0	cyclohexanols; phenols; tertiary amino compound	antidepressant; drug metabolite; marine xenobiotic metabolite
iodoproxyfan iodoproxyfan: structure given in first source	2.03	1	0
calcium borate calcium borate: RN given refers to cpd with MF CaB4O7	4.61	1	1
docetaxel anhydrous Docetaxel: A semisynthetic analog of PACLITAXEL used in the treatment of locally advanced or metastatic BREAST NEOPLASMS and NON-SMALL CELL LUNG CANCER.. docetaxel anhydrous : A tetracyclic diterpenoid that is paclitaxel with the N-benzyloxycarbonyl group replaced by N-tert-butoxycarbonyl, and the acetoxy group at position 10 replaced by a hydroxy group.	4.61	1	1	secondary alpha-hydroxy ketone; tetracyclic diterpenoid	antimalarial; antineoplastic agent; photosensitizing agent
alpha-methylhistamine (R)-alpha-methylhistamine : An aralkylamino compound that is histamine bearing a methyl substituent at the alpha-position (the R-enantiomer).	2.83	3	0	aralkylamino compound; imidazoles	H3-receptor agonist
atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.	2.17	1	0
ramelteon ramelteon: melatonin MT1/MT2 receptor agonist	3.31	1	0	indanes
benzofurans Benzofurans: Compounds that contain a BENZENE ring fused to a furan ring.	2.52	2	0
interferon-gamma aplysamine-1: from sponge Aplysia sp.; structure in first source	2.05	1	0
ritonavir Ritonavir: An HIV protease inhibitor that works by interfering with the reproductive cycle of HIV. It also inhibits CYTOCHROME P-450 CYP3A.. ritonavir : An L-valine derivative that is L-valinamide in which alpha-amino group has been acylated by a [(2-isopropyl-1,3-thiazol-4-yl)methyl]methylcarbamoyl group and in which a hydrogen of the carboxamide amino group has been replaced by a (2R,4S,5S)-4-hydroxy-1,6-diphenyl-5-{[(1,3-thiazol-5-ylmethoxy)carbonyl]amino}hexan-2-yl group. A CYP3A inhibitor and antiretroviral drug from the protease inhibitor class used to treat HIV infection and AIDS, it is often used as a fixed-dose combination with another protease inhibitor, lopinavir. Also used in combination with dasabuvir sodium hydrate, ombitasvir and paritaprevir (under the trade name Viekira Pak) for treatment of chronic hepatitis C virus genotype 1 infection as well as cirrhosis of the liver.	4.61	1	1	1,3-thiazoles; carbamate ester; carboxamide; L-valine derivative; ureas	antiviral drug; environmental contaminant; HIV protease inhibitor; xenobiotic
permanganate [no description available]	4.61	1	1	manganese oxoacid
carboplatin [no description available]	4.61	1	1
conessine conessine : A steroid alkaloid that is con-5-enine substituted by a N,N-dimethylamino group at position 3. It has been isolated from the plant species of the family Apocynaceae.	3.57	2	0	steroid alkaloid; tertiary amino compound	antibacterial agent; antimalarial; H3-receptor antagonist; plant metabolite
tretinoin Tretinoin: An important regulator of GENE EXPRESSION during growth and development, and in NEOPLASMS. Tretinoin, also known as retinoic acid and derived from maternal VITAMIN A, is essential for normal GROWTH; and EMBRYONIC DEVELOPMENT. An excess of tretinoin can be teratogenic. It is used in the treatment of PSORIASIS; ACNE VULGARIS; and several other SKIN DISEASES. It has also been approved for use in promyelocytic leukemia (LEUKEMIA, PROMYELOCYTIC, ACUTE).. retinoic acid : A retinoid consisting of 3,7-dimethylnona-2,4,6,8-tetraenoic acid substituted at position 9 by a 2,6,6-trimethylcyclohex-1-en-1-yl group (geometry of the four exocyclic double bonds is not specified).. all-trans-retinoic acid : A retinoic acid in which all four exocyclic double bonds have E- (trans-) geometry.	4.61	1	1	retinoic acid; vitamin A	anti-inflammatory agent; antineoplastic agent; antioxidant; AP-1 antagonist; human metabolite; keratolytic drug; retinoic acid receptor agonist; retinoid X receptor agonist; signalling molecule
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.	2.57	2	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
2,3-bis(bromomethyl)quinoxaline-1,4-dioxide conoidin A: inhibits the peroxiredoxin TgPrx11; structure in first source	4.61	1	1
doxepin hydrochloride [no description available]	3.31	1	0
eszopiclone Eszopiclone: A pyridine, pyrazine, and piperazine derivative that is used as a HYPNOTIC AND SEDATIVE in the treatment of INSOMNIA.. 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.	3.31	1	0	zopiclone	central nervous system depressant; sedative
jnj-5207852 [no description available]	3.36	6	0
nitrogen dioxide Nitrogen Dioxide: Nitrogen oxide (NO2). A highly poisonous gas. Exposure produces inflammation of lungs that may only cause slight pain or pass unnoticed, but resulting edema several days later may cause death. (From Merck, 11th ed) It is a major atmospheric pollutant that is able to absorb UV light that does not reach the earth's surface.	4.61	1	1	nitrogen oxide
thioperamide thioperamide: structure given in first source; histamine H3 receptor antagonist	3.05	4	0	primary aliphatic amine
prucalopride prucalopride: a 5-HT4 agonist enterokinetic compound	2.25	1	0	benzamides
cholecalciferol 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.. 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.	4.61	1	1	D3 vitamins; hydroxy seco-steroid; seco-cholestane; secondary alcohol; steroid hormone	geroprotector; human metabolite
baicalein [no description available]	4.61	1	1	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
menaquinone 6 menaquinone 6: RN given refers to (all-E)-isomer	4.61	1	1
sirolimus Sirolimus: A macrolide compound obtained from Streptomyces hygroscopicus that acts by selectively blocking the transcriptional activation of cytokines thereby inhibiting cytokine production. It is bioactive only when bound to IMMUNOPHILINS. Sirolimus is a potent immunosuppressant and possesses both antifungal and antineoplastic properties.. sirolimus : A macrolide lactam isolated from Streptomyces hygroscopicus consisting of a 29-membered ring containing 4 trans double bonds, three of which are conjugated. It is an antibiotic, immunosupressive and antineoplastic agent.	4.61	1	1	antibiotic antifungal drug; cyclic acetal; cyclic ketone; ether; macrolide lactam; organic heterotricyclic compound; secondary alcohol	antibacterial drug; anticoronaviral agent; antineoplastic agent; bacterial metabolite; geroprotector; immunosuppressive agent; mTOR inhibitor
menaquinone 7 menaquinone-7 : A menaquinone whose side-chain contains seven isoprene units in an all-trans-configutation.	4.61	1	1	menaquinone	bone density conservation agent; cofactor; Escherichia coli metabolite; human blood serum metabolite; Mycoplasma genitalium metabolite
istradefylline [no description available]	3.76	2	0	oxopurine
lead Lead: A soft, grayish metal with poisonous salts; atomic number 82, atomic weight 207.2, symbol Pb.	4.61	1	1	carbon group element atom; elemental lead; metal atom	neurotoxin
arsenic Arsenic: A shiny gray element with atomic symbol As, atomic number 33, and atomic weight 75. It occurs throughout the universe, mostly in the form of metallic arsenides. Most forms are toxic. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), arsenic and certain arsenic compounds have been listed as known carcinogens. (From Merck Index, 11th ed)	4.61	1	1	metalloid atom; pnictogen	micronutrient
phosphorus Phosphorus: A non-metal element that has the atomic symbol P, atomic number 15, and atomic weight 31. It is an essential element that takes part in a broad variety of biochemical reactions.	4.61	1	1	monoatomic phosphorus; nonmetal atom; pnictogen	macronutrient
dizocilpine maleate Dizocilpine Maleate: A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.. dizocilpine maleate : A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid.	2.78	3	0	maleate salt; tetracyclic antidepressant	anaesthetic; anticonvulsant; neuroprotective agent; nicotinic antagonist; NMDA receptor antagonist
proxyfan [no description available]	2.04	1	0	benzyl ether
ciproxifan [no description available]	4.32	5	0	aromatic ketone
axitinib [no description available]	4.61	1	1	aryl sulfide; benzamides; indazoles; pyridines	antineoplastic agent; tyrosine kinase inhibitor; vascular endothelial growth factor receptor antagonist
cb 34 CB 34: ligand for peripheral benzodiazepine receptors; structure in first source	3.31	1	0
(2S)-1-(1H-imidazol-5-yl)-2-propanamine [no description available]	2.31	1	0	aralkylamine
sb 334867-a 1-(2-methylbenzoxazol-6-yl)-3-(1,5)naphthyridin-4-yl urea: selective OX1 receptor antagonist	3.31	1	0	naphthyridine derivative
armodafinil armodafinil : A 2-[(diphenylmethyl)sulfinyl]acetamide that has R configuration at the sulfur atom. Like its racemate, modafinil, it is used for the treatment of sleeping disorders such as narcolepsy, obstructive sleep apnoea, and shift-work sleep disorder. Peak concentration in the blood later occurs later following administration than with modafinil, so it is thought that armodafinil may be more effective than modafinil in treating people with excessive daytime sleepiness.	3.31	1	0	2-[(diphenylmethyl)sulfinyl]acetamide	central nervous system stimulant; eugeroic
nnc 38-1049 NNC 38-1049: selective histamine H3 receptor antagonist; structure in first source	2.52	2	0
dibutyl phthalate 6-((3-cyclobutyl-2,3,4,5-tetrahydro-1H-3-benzazepin-7-yl)oxy)-N-methyl-3-pyridinecarboxamide: GSK-189254 is the HCl salt; an H3 receptor antagonist; putative cognitive enhancer; structure in first source	2.73	3	0
benzonitrile, 4-(2-(2-((2r)-2-methyl-1-pyrrolidinyl)ethyl)-5-benzofuranyl)- [no description available]	2.96	4	0
sorbitan monooleate [no description available]	4.61	1	1	fatty acid ester
jnj 10181457 [no description available]	2.05	1	0
tasimelteon tasimelteon : A member of the class of 1-benzofurans that is propionamide in which one of the amide hydrogens is replaced by a [(1R,2R)-2-(2,3-dihydro-1-benzofuran-4-yl)cyclopropyl]methyl group. A melatonin receptor agonist used for the treatment of non-24-hour sleep-wake disorder.	3.31	1	0	1-benzofurans; cyclopropanes; monocarboxylic acid amide	melatonin receptor agonist
mk-0249 MK-0249: a histamine-3 receptor inverse agonist; structure in first source	3.61	2	0
scopolamine hydrobromide [no description available]	2.03	1	0
mdv 3100 [no description available]	3.35	1	0	(trifluoromethyl)benzenes; benzamides; imidazolidinone; monofluorobenzenes; nitrile; thiocarbonyl compound	androgen antagonist; antineoplastic agent
glucagon Glucagon: A 29-amino acid pancreatic peptide derived from proglucagon which is also the precursor of intestinal GLUCAGON-LIKE PEPTIDES. Glucagon is secreted by PANCREATIC ALPHA CELLS and plays an important role in regulation of BLOOD GLUCOSE concentration, ketone metabolism, and several other biochemical and physiological processes. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1511). glucagon : A 29-amino acid peptide hormone consisting of His, Ser, Gln, Gly, Thr, Phe, Thr, Ser, Asp, Tyr, Ser, Lys, Tyr, Leu, Asp, Ser, Arg, Arg, Ala, Gln, Asp, Phe, Val, Gln, Trp, Leu, Met, Asn and Thr residues joined in sequence.	4.61	1	1	peptide hormone
msh, 4-nle-7-phe-alpha- [no description available]	3.35	1	0	polypeptide	dermatologic drug
cellulose DEAE-Cellulose: Cellulose derivative used in chromatography, as ion-exchange material, and for various industrial applications.	4.61	1	1	glycoside
fedratinib fedratinib: a selective small-molecule inhibitor of JAK2	3.35	1	0	sulfonamide
chitosan [no description available]	4.61	1	1
sodium oxybate Sodium Oxybate: The sodium salt of 4-hydroxybutyric acid. It is used for both induction and maintenance of ANESTHESIA.	5.7	5	0
pf-3893787 PF-3893787: structure in first source	3.21	1	0
apalutamide [no description available]	3.35	1	0
suvorexant suvorexant: an orexin receptor antagonist; structure in first source. suvorexant : An aromatic amide obtained by formal condensation of the carboxy group of 5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid with the secondary amino group of 5-chloro-2-[(5R)-5-methyl-1,4-diazepan-1-yl]-1,3-benzoxazole. An orexin receptor antagonist used for the management of insomnia.	4.24	2	0	1,3-benzoxazoles; aromatic amide; diazepine; organochlorine compound; triazoles	central nervous system depressant; orexin receptor antagonist
pexidartinib pexidartinib: inhibits both CSF1R and c-kit receptor tyrosine kinase; structure in first source. pexidartinib : A pyrrolopyridine that is 5-chloro-1H-pyrrolo[2,3-b]pyridine which is substituted by a [6-({[6-(trifluoromethyl)pyridin-3-yl]methyl}amino)pyridin-3-yl]methyl group at position 3. It is a potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, KIT, and FLT3 (IC50 of 20 nM, 10 nM and 160 nM, respectively). Approved by the FDA for the treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT).	3.35	1	0	aminopyridine; organochlorine compound; organofluorine compound; pyrrolopyridine; secondary amino compound	antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
glycolipids [no description available]	4.61	1	1
piperidines Piperidines: A family of hexahydropyridines.	15.75	68	14
interleukin-8 Interleukin-8: A member of the CXC chemokine family that plays a role in the regulation of the acute inflammatory response. It is secreted by variety of cell types and induces CHEMOTAXIS of NEUTROPHILS and other inflammatory cells.	4.61	1	1
5-(4-amino-1-propan-2-yl-3-pyrazolo[3,4-d]pyrimidinyl)-1,3-benzoxazol-2-amine sapanisertib: an mTOR inhibitor	4.61	1	1	benzoxazole
heme Heme: The color-furnishing portion of hemoglobin. It is found free in tissues and as the prosthetic group in many hemeproteins.. ferroheme : Any iron(II)--porphyrin coordination complex.. ferroheme b : Heme b in which the iron has oxidation state +2.. heme : A heme is any tetrapyrrolic chelate of iron.	4.61	1	1
omadacycline omadacycline: demonstrated in vitro activity against a broad range of Gram-positive and select Gram-negative pathogens; structure in first source	2.25	1	0	tetracyclines
catalpol catalpol: component of dihuang; RN given refers to (1aS-(1aalpha,1bbeta,2beta,5abeta,6beta,6aalpha))-isomer; RN for cpd without isomeric designation not avail 12/92	4.61	1	1
olanzapine Olanzapine: A benzodiazepine derivative that binds SEROTONIN RECEPTORS; MUSCARINIC RECEPTORS; HISTAMINE H1 RECEPTORS; ADRENERGIC ALPHA-1 RECEPTORS; and DOPAMINE RECEPTORS. It is an antipsychotic agent used in the treatment of SCHIZOPHRENIA; BIPOLAR DISORDER; and MAJOR DEPRESSIVE DISORDER; it may also reduce nausea and vomiting in patients undergoing chemotherapy.. olanzapine : A benzodiazepine that is 10H-thieno[2,3-b][1,5]benzodiazepine substituted by a methyl group at position 2 and a 4-methylpiperazin-1-yl group at position 4.	7.13	1	0	benzodiazepine; N-arylpiperazine; N-methylpiperazine	antiemetic; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; serotonin uptake inhibitor
acetylcellulose acetylcellulose: coating compound. cellulose acetate : A glucan derivative obtained through the esterification of cellulose by acetic anhydride or acetic acid, resulting in the substitution of some of the hydroxy groups of cellulose by acetyl groups. It is used in a variety of applications including base material for photographic film, clothing, membrane filters, coatings, food packaging, and as a frame material for eyeglasses.	4.61	1	1

Condition	Indicated	Relationship Strength	Studies	Trials
Obesity A status with BODY WEIGHT that is grossly above the recommended standards, usually due to accumulation of excess FATS in the body. The standards may vary with age, sex, genetic or cultural background. In the BODY MASS INDEX, a BMI greater than 30.0 kg/m2 is considered obese, and a BMI greater than 40.0 kg/m2 is considered morbidly obese (MORBID OBESITY).	0	9.92	11	9
Absence Seizure [description not available]	0	2.66	2	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	2.66	2	0
Long Sleeper Syndrome [description not available]	0	3.97	2	0
Sleep Wake Disorders Abnormal sleep-wake schedule or pattern associated with the CIRCADIAN RHYTHM which affect the length, timing, and/or rigidity of the sleep-wake cycle relative to the day-night cycle.	0	3.97	2	0
Degenerative Diseases, Central Nervous System [description not available]	0	3.12	1	0
Behavior Disorders [description not available]	0	3.12	1	0
Mental Disorders Psychiatric illness or diseases manifested by breakdowns in the adaptational process expressed primarily as abnormalities of thought, feeling, and behavior producing either distress or impairment of function.	0	3.12	1	0
Neurodegenerative Diseases Hereditary and sporadic conditions which are characterized by progressive nervous system dysfunction. These disorders are often associated with atrophy of the affected central or peripheral nervous system structures.	0	3.12	1	0
Acute Confusional Senile Dementia [description not available]	0	7.92	6	4
Alzheimer Disease A degenerative disease of the BRAIN characterized by the insidious onset of DEMENTIA. Impairment of MEMORY, judgment, attention span, and problem solving skills are followed by severe APRAXIAS and a global loss of cognitive abilities. The condition primarily occurs after age 60, and is marked pathologically by severe cortical atrophy and the triad of SENILE PLAQUES; NEUROFIBRILLARY TANGLES; and NEUROPIL THREADS. (From Adams et al., Principles of Neurology, 6th ed, pp1049-57)	0	7.92	6	4
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	5.18	3	1
Gelineau Syndrome [description not available]	0	15.01	42	15
Cataleptic Attacks [description not available]	0	13.66	25	12
Narcolepsy A condition characterized by recurrent episodes of daytime somnolence and lapses in consciousness (microsomnias) that may be associated with automatic behaviors and AMNESIA. CATAPLEXY; SLEEP PARALYSIS, and hypnagogic HALLUCINATIONS frequently accompany narcolepsy. The pathophysiology of this disorder includes sleep-onset rapid eye movement (REM) sleep, which normally follows stage III or IV sleep. (From Neurology 1998 Feb;50(2 Suppl 1):S2-S7)	1	19.7	84	30
Autism Spectrum Disorder Wide continuum of associated cognitive and neurobehavioral disorders, including, but not limited to, three core-defining features: impairments in socialization, impairments in verbal and nonverbal communication, and restricted and repetitive patterns of behaviors. (from DSM-V)	0	2.41	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	16.25	88	83
Hyperactivity, Motor [description not available]	0	2.41	1	0
Apnea, Obstructive Sleep [description not available]	0	7.93	7	1
Lassitude [description not available]	0	3.33	1	0
Daytime Sleepiness [description not available]	0	11.46	16	6
Fatigue The state of weariness following a period of exertion, mental or physical, characterized by a decreased capacity for work and reduced efficiency to respond to stimuli.	0	8.33	1	0
Disorders of Excessive Somnolence Disorders characterized by hypersomnolence during normal waking hours that may impair cognitive functioning. Subtypes include primary hypersomnia disorders (e.g., IDIOPATHIC HYPERSOMNOLENCE; NARCOLEPSY; and KLEINE-LEVIN SYNDROME) and secondary hypersomnia disorders where excessive somnolence can be attributed to a known cause (e.g., drug affect, MENTAL DISORDERS, and SLEEP APNEA SYNDROME). (From J Neurol Sci 1998 Jan 8;153(2):192-202; Thorpy, Principles and Practice of Sleep Medicine, 2nd ed, p320)	0	11.46	16	6
Sleep Apnea, Obstructive A disorder characterized by recurrent apneas during sleep despite persistent respiratory efforts. It is due to upper airway obstruction. The respiratory pauses may induce HYPERCAPNIA or HYPOXIA. Cardiac arrhythmias and elevation of systemic and pulmonary arterial pressures may occur. Frequent partial arousals occur throughout sleep, resulting in relative SLEEP DEPRIVATION and daytime tiredness. Associated conditions include OBESITY; ACROMEGALY; MYXEDEMA; micrognathia; MYOTONIC DYSTROPHY; adenotonsilar dystrophy; and NEUROMUSCULAR DISEASES. (From Adams et al., Principles of Neurology, 6th ed, p395)	0	7.93	7	1
Aura [description not available]	0	2.41	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	7.41	1	0
Panic Attacks [description not available]	0	7.6	1	0
Panic Disorder A type of anxiety disorder characterized by unexpected panic attacks that last minutes or, rarely, hours. Panic attacks begin with intense apprehension, fear or terror and, often, a feeling of impending doom. Symptoms experienced during a panic attack include dyspnea or sensations of being smothered; dizziness, loss of balance or faintness; choking sensations; palpitations or accelerated heart rate; shakiness; sweating; nausea or other form of abdominal distress; depersonalization or derealization; paresthesias; hot flashes or chills; chest discomfort or pain; fear of dying and fear of not being in control of oneself or going crazy. Agoraphobia may also develop. Similar to other anxiety disorders, it may be inherited as an autosomal dominant trait.	0	2.6	1	0
Chronic Insomnia [description not available]	0	5.91	4	1
Sleep Initiation and Maintenance Disorders Disorders characterized by impairment of the ability to initiate or maintain sleep. This may occur as a primary disorder or in association with another medical or psychiatric condition.	0	5.91	4	1
Adverse Drug Event [description not available]	0	2.6	1	0
Drug-Related Side Effects and Adverse Reactions Disorders that result from the intended use of PHARMACEUTICAL PREPARATIONS. Included in this heading are a broad variety of chemically-induced adverse conditions due to toxicity, DRUG INTERACTIONS, and metabolic effects of pharmaceuticals.	0	2.6	1	0
Injuries, Spinal Cord [description not available]	0	2.6	1	0
Spinal Cord Injuries Penetrating and non-penetrating injuries to the spinal cord resulting from traumatic external forces (e.g., WOUNDS, GUNSHOT; WHIPLASH INJURIES; etc.).	0	2.6	1	0
Alcohol Abuse [description not available]	0	2.21	1	0
Labhart-Willi Syndrome [description not available]	0	2.21	1	0
Alcoholism A primary, chronic disease with genetic, psychosocial, and environmental factors influencing its development and manifestations. The disease is often progressive and fatal. It is characterized by impaired control over drinking, preoccupation with the drug alcohol, use of alcohol despite adverse consequences, and distortions in thinking, most notably denial. Each of these symptoms may be continuous or periodic. (Morse & Flavin for the Joint Commission of the National Council on Alcoholism and Drug Dependence and the American Society of Addiction Medicine to Study the Definition and Criteria for the Diagnosis of Alcoholism: in JAMA 1992;268:1012-4)	1	4.21	1	0
Anorexia Nervosa An eating disorder that is characterized by the lack or loss of APPETITE, known as ANOREXIA. Other features include excess fear of becoming OVERWEIGHT; BODY IMAGE disturbance; significant WEIGHT LOSS; refusal to maintain minimal normal weight; and AMENORRHEA. This disorder occurs most frequently in adolescent females. (APA, Thesaurus of Psychological Index Terms, 1994)	0	7.21	1	0
Prader-Willi Syndrome An autosomal dominant disorder caused by deletion of the proximal long arm of the paternal chromosome 15 (15q11-q13) or by inheritance of both of the pair of chromosomes 15 from the mother (UNIPARENTAL DISOMY) which are imprinted (GENETIC IMPRINTING) and hence silenced. Clinical manifestations include MENTAL RETARDATION; MUSCULAR HYPOTONIA; HYPERPHAGIA; OBESITY; short stature; HYPOGONADISM; STRABISMUS; and HYPERSOMNOLENCE. (Menkes, Textbook of Child Neurology, 5th ed, p229)	1	4.21	1	0
Bilateral Headache [description not available]	0	2.21	1	0
Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.	0	2.21	1	0
Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.	0	7.88	3	0
Headache The symptom of PAIN in the cranial region. It may be an isolated benign occurrence or manifestation of a wide variety of HEADACHE DISORDERS.	0	2.21	1	0
Idiopathic Parkinson Disease [description not available]	0	2.25	1	0
Parkinson Disease A progressive, degenerative neurologic disease characterized by a TREMOR that is maximal at rest, retropulsion (i.e. a tendency to fall backwards), rigidity, stooped posture, slowness of voluntary movements, and a masklike facial expression. Pathologic features include loss of melanin containing neurons in the substantia nigra and other pigmented nuclei of the brainstem. LEWY BODIES are present in the substantia nigra and locus coeruleus but may also be found in a related condition (LEWY BODY DISEASE, DIFFUSE) characterized by dementia in combination with varying degrees of parkinsonism. (Adams et al., Principles of Neurology, 6th ed, p1059, pp1067-75)	1	4.25	1	0
Disease Exacerbation [description not available]	0	14.65	49	49
Birth Weight The mass or quantity of heaviness of an individual at BIRTH. It is expressed by units of pounds or kilograms.	0	4.43	1	1
Recrudescence [description not available]	0	4.43	1	1
Diffuse Parenchymal Lung Disease [description not available]	0	4.43	1	1
Hibernation, Myocardial [description not available]	0	4.43	1	1
Tuberculosis, Drug-Resistant [description not available]	0	4.43	1	1
Infections, Coronavirus [description not available]	0	9.74	9	9
Chronic Hepatitis B [description not available]	0	4.43	1	1
Anterior Cerebral Circulation Infarction [description not available]	0	4.43	1	1
Apoplexy [description not available]	0	4.43	1	1
Diffuse Lymphocytic Lymphoma, Poorly-Differentiated [description not available]	0	4.43	1	1
Airflow Obstruction, Chronic [description not available]	0	4.43	1	1
Ductal Carcinoma [description not available]	0	4.43	1	1
Gastrointestinal Stromal Neoplasm [description not available]	0	4.43	1	1
Complications of Diabetes Mellitus [description not available]	0	4.43	1	1
Overweight A status with BODY WEIGHT that is above certain standards. In the scale of BODY MASS INDEX, overweight is defined as having a BMI of 25.0-29.9 kg/m2. Overweight may or may not be due to increases in body fat (ADIPOSE TISSUE), hence overweight does not equal over fat.	0	4.43	1	1
Atherogenesis [description not available]	0	7.55	4	4
Bone Fractures [description not available]	0	4.43	1	1
Chronic Kidney Diseases [description not available]	0	7.55	4	4
Primary Graft Dysfunction A form of ischemia-reperfusion injury occurring in the early period following transplantation. Significant pathophysiological changes in MITOCHONDRIA are the main cause of the dysfunction. It is most often seen in the transplanted lung, liver, or kidney and can lead to GRAFT REJECTION.	0	4.43	1	1
Lung Injury, Acute [description not available]	0	4.43	1	1
Airway Remodeling The structural changes in the number, mass, size and/or composition of the airway tissues.	0	4.43	1	1
Atheroma [description not available]	0	4.43	1	1
Lower Urinary Tract Symptom [description not available]	0	4.43	1	1
Carcinogenesis The origin, production or development of cancer through genotypic and phenotypic changes which upset the normal balance between cell proliferation and cell death. Carcinogenesis generally requires a constellation of steps, which may occur quickly or over a period of many years.	0	9.74	9	9
Adolescent Obesity [description not available]	0	4.43	1	1
Allergic Rhinitis [description not available]	0	4.43	1	1
Thyroid Cancer, Anaplastic [description not available]	0	4.43	1	1
Encephalopathy, Traumatic [description not available]	0	4.43	1	1
Familial Nonmedullary Thyroid Cancer [description not available]	0	4.43	1	1
Esophageal Squamous Cell Carcinoma A carcinoma that originates usually from cells on the surface of the middle and lower third of the ESOPHAGUS. Tumor cells exhibit typical squamous morphology and form large polypoid lesions. Mutations in RNF6, LZTS1, TGFBR2, DEC1, and WWOX1 genes are associated with this cancer.	0	4.43	1	1
2019 Novel Coronavirus Disease [description not available]	0	9.74	9	9
Adenocarcinoma, Basal Cell [description not available]	0	4.43	1	1
Anoxemia [description not available]	0	4.43	1	1
Rheumatoid Arthritis [description not available]	0	4.43	1	1
Asthma, Bronchial [description not available]	0	4.43	1	1
Amaurosis [description not available]	0	4.43	1	1
Bone Loss, Osteoclastic [description not available]	0	4.43	1	1
Benign Neoplasms, Brain [description not available]	0	4.43	1	1
Breast Cancer [description not available]	0	9.74	9	9
Carcinoma, Ehrlich Tumor A transplantable, poorly differentiated malignant tumor which appeared originally as a spontaneous breast carcinoma in a mouse. It grows in both solid and ascitic forms.	0	4.43	1	1
Carcinoma, Non-Small Cell Lung [description not available]	0	4.43	1	1
Adenocarcinoma Of Kidney [description not available]	0	7.55	4	4
Cell Transformation, Neoplastic Cell changes manifested by escape from control mechanisms, increased growth potential, alterations in the cell surface, karyotypic abnormalities, morphological and biochemical deviations from the norm, and other attributes conferring the ability to invade, metastasize, and kill.	0	4.43	1	1
Clostridioides difficile Infection [description not available]	0	4.43	1	1
Alloxan Diabetes [description not available]	0	4.43	1	1
Autoimmune Diabetes [description not available]	0	4.43	1	1
Diabetes Mellitus, Adult-Onset [description not available]	0	4.43	1	1
Anasarca [description not available]	0	4.43	1	1
Cutis Elastica [description not available]	0	4.43	1	1
E coli Infections [description not available]	0	4.43	1	1
Cancer of Esophagus [description not available]	0	4.43	1	1
Exanthem [description not available]	0	4.43	1	1
Glial Cell Tumors [description not available]	0	4.43	1	1
Cardiac Failure [description not available]	0	11.38	16	16
Extravascular Hemolysis [description not available]	0	4.43	1	1
Bleeding [description not available]	0	4.43	1	1
Hepatitis B Virus Infection [description not available]	0	7.55	4	4
Hepatocellular Carcinoma [description not available]	0	7.55	4	4
Fasting Hypoglycemia HYPOGLYCEMIA expressed in the postabsorptive state, after prolonged FASTING, or an overnight fast.	0	4.43	1	1
Innate Inflammatory Response [description not available]	0	11.38	16	16
Hypermobility, Joint [description not available]	0	4.43	1	1
Chronic Kidney Failure [description not available]	0	4.43	1	1
Cancer of Kidney [description not available]	0	7.55	4	4
Cirrhosis, Liver [description not available]	0	4.43	1	1
Cancer of Liver [description not available]	0	7.55	4	4
Cancer of Lung [description not available]	0	4.43	1	1
B16 Melanoma [description not available]	0	4.43	1	1
Muscle Disorders [description not available]	0	4.43	1	1
Metastase [description not available]	0	7.55	4	4
Benign Neoplasms [description not available]	0	7.55	4	4
Morbid Obesity [description not available]	0	4.43	1	1
Age-Related Osteoporosis [description not available]	0	7.55	4	4
Cancer of Ovary [description not available]	0	4.43	1	1
Cancer of Pancreas [description not available]	0	9.74	9	9
Experimental Lung Inflammation Inflammation of any part, segment or lobe, of the lung parenchyma.	0	4.43	1	1
Prediabetes [description not available]	0	4.43	1	1
Acute Respiratory Distress Syndrome [description not available]	0	4.43	1	1
Acute Hypercapnic Respiratory Failure [description not available]	0	4.43	1	1
Cancer of Salivary Gland [description not available]	0	4.43	1	1
Hemorrhagic Shock [description not available]	0	4.43	1	1
Cancer of Skin [description not available]	0	4.43	1	1
Blood Clot [description not available]	0	4.43	1	1
Cancer of the Thyroid [description not available]	0	4.43	1	1
Pulmonary Consumption [description not available]	0	4.43	1	1
Deficiency, Vitamin D [description not available]	0	4.43	1	1
Injuries Used with anatomic headings, animals, and sports for wounds and injuries. Excludes cell damage, for which pathology is used.	0	4.43	1	1
Injury, Ischemia-Reperfusion [description not available]	0	4.43	1	1
HIV Coinfection [description not available]	0	4.43	1	1
Bone Loss, Perimenopausal [description not available]	0	4.43	1	1
Bacterial Infections, Gram-Negative [description not available]	0	7.55	4	4
Carcinoma, Ductal, Pancreatic [description not available]	0	4.43	1	1
Hangman Fracture [description not available]	0	4.43	1	1
Idiopathic Interstitial Pneumonia [description not available]	0	4.43	1	1
Eye Infections, Fungal Infection by a variety of fungi, usually through four possible mechanisms: superficial infection producing conjunctivitis, keratitis, or lacrimal obstruction; extension of infection from neighboring structures - skin, paranasal sinuses, nasopharynx; direct introduction during surgery or accidental penetrating trauma; or via the blood or lymphatic routes in patients with underlying mycoses.	0	4.43	1	1
Local Neoplasm Recurrence [description not available]	0	9.74	9	9
Invasiveness, Neoplasm [description not available]	0	4.43	1	1
Cell Transformation, Viral An inheritable change in cells manifested by changes in cell division and growth and alterations in cell surface properties. It is induced by infection with a transforming virus.	0	4.43	1	1
Delayed Effects, Prenatal Exposure [description not available]	0	4.43	1	1
Brain Injuries, Traumatic A form of acquired brain injury which occurs when a sudden trauma causes damage to the brain.	0	4.43	1	1
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	0	4.43	1	1
Aging The gradual irreversible changes in structure and function of an organism that occur as a result of the passage of time.	0	4.43	1	1
Albuminuria The presence of albumin in the urine, an indicator of KIDNEY DISEASES.	0	4.43	1	1
Hypoxia Sub-optimal OXYGEN levels in the ambient air of living organisms.	0	4.43	1	1
Arthritis, Rheumatoid A chronic systemic disease, primarily of the joints, marked by inflammatory changes in the synovial membranes and articular structures, widespread fibrinoid degeneration of the collagen fibers in mesenchymal tissues, and by atrophy and rarefaction of bony structures. Etiology is unknown, but autoimmune mechanisms have been implicated.	0	4.43	1	1
Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).	0	4.43	1	1
Blindness The inability to see or the loss or absence of perception of visual stimuli. This condition may be the result of EYE DISEASES; OPTIC NERVE DISEASES; OPTIC CHIASM diseases; or BRAIN DISEASES affecting the VISUAL PATHWAYS or OCCIPITAL LOBE.	0	4.43	1	1
Brain Neoplasms Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.	0	4.43	1	1
Breast Neoplasms Tumors or cancer of the human BREAST.	0	9.74	9	9
Carcinoma, Non-Small-Cell Lung A heterogeneous aggregate of at least three distinct histological types of lung cancer, including SQUAMOUS CELL CARCINOMA; ADENOCARCINOMA; and LARGE CELL CARCINOMA. They are dealt with collectively because of their shared treatment strategy.	0	4.43	1	1
Carcinoma, Renal Cell A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.	0	7.55	4	4
Cardiovascular Diseases Pathological conditions involving the CARDIOVASCULAR SYSTEM including the HEART; the BLOOD VESSELS; or the PERICARDIUM.	0	7.55	4	4
Clostridium Infections Infections with bacteria of the genus CLOSTRIDIUM and closely related CLOSTRIDIOIDES species.	0	4.43	1	1
Colitis Inflammation of the COLON section of the large intestine (INTESTINE, LARGE), usually with symptoms such as DIARRHEA (often with blood and mucus), ABDOMINAL PAIN, and FEVER.	0	4.43	1	1
Connective Tissue Diseases A heterogeneous group of disorders, some hereditary, others acquired, characterized by abnormal structure or function of one or more of the elements of connective tissue, i.e., collagen, elastin, or the mucopolysaccharides.	0	4.43	1	1
Diabetes Mellitus A heterogeneous group of disorders characterized by HYPERGLYCEMIA and GLUCOSE INTOLERANCE.	0	4.43	1	1
Diabetes Mellitus, Type 1 A subtype of DIABETES MELLITUS that is characterized by INSULIN deficiency. It is manifested by the sudden onset of severe HYPERGLYCEMIA, rapid progression to DIABETIC KETOACIDOSIS, and DEATH unless treated with insulin. The disease may occur at any age, but is most common in childhood or adolescence.	0	4.43	1	1
Diabetes Mellitus, Type 2 A subclass of DIABETES MELLITUS that is not INSULIN-responsive or dependent (NIDDM). It is characterized initially by INSULIN RESISTANCE and HYPERINSULINEMIA; and eventually by GLUCOSE INTOLERANCE; HYPERGLYCEMIA; and overt diabetes. Type II diabetes mellitus is no longer considered a disease exclusively found in adults. Patients seldom develop KETOSIS but often exhibit OBESITY.	0	4.43	1	1
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	0	4.43	1	1
Ehlers-Danlos Syndrome A heterogeneous group of autosomally inherited COLLAGEN DISEASES caused by defects in the synthesis or structure of FIBRILLAR COLLAGEN. There are numerous subtypes: classical, hypermobility, vascular, and others. Common clinical features include hyperextensible skin and joints, skin fragility and reduced wound healing capability.	0	4.43	1	1
Escherichia coli Infections Infections with bacteria of the species ESCHERICHIA COLI.	0	4.43	1	1
Esophageal Neoplasms Tumors or cancer of the ESOPHAGUS.	0	4.43	1	1
Exanthema Diseases in which skin eruptions or rashes are a prominent manifestation. Classically, six such diseases were described with similar rashes; they were numbered in the order in which they were reported. Only the fourth (Duke's disease), fifth (ERYTHEMA INFECTIOSUM), and sixth (EXANTHEMA SUBITUM) numeric designations survive as occasional synonyms in current terminology.	0	4.43	1	1
Glioma Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)	0	4.43	1	1
Heart Failure A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.	0	11.38	16	16
Hemolysis The destruction of ERYTHROCYTES by many different causal agents such as antibodies, bacteria, chemicals, temperature, and changes in tonicity.	0	4.43	1	1
Hemorrhage Bleeding or escape of blood from a vessel.	0	4.43	1	1
Hepatitis B INFLAMMATION of the LIVER in humans caused by a member of the ORTHOHEPADNAVIRUS genus, HEPATITIS B VIRUS. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.	0	7.55	4	4
Carcinoma, Hepatocellular A primary malignant neoplasm of epithelial liver cells. It ranges from a well-differentiated tumor with EPITHELIAL CELLS indistinguishable from normal HEPATOCYTES to a poorly differentiated neoplasm. The cells may be uniform or markedly pleomorphic, or form GIANT CELLS. Several classification schemes have been suggested.	0	7.55	4	4
Hypoglycemia A syndrome of abnormally low BLOOD GLUCOSE level. Clinical hypoglycemia has diverse etiologies. Severe hypoglycemia eventually lead to glucose deprivation of the CENTRAL NERVOUS SYSTEM resulting in HUNGER; SWEATING; PARESTHESIA; impaired mental function; SEIZURES; COMA; and even DEATH.	0	4.43	1	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	0	11.38	16	16
Kidney Failure, Chronic The end-stage of CHRONIC RENAL INSUFFICIENCY. It is characterized by the severe irreversible kidney damage (as measured by the level of PROTEINURIA) and the reduction in GLOMERULAR FILTRATION RATE to less than 15 ml per min (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002). These patients generally require HEMODIALYSIS or KIDNEY TRANSPLANTATION.	0	4.43	1	1
Kidney Neoplasms Tumors or cancers of the KIDNEY.	0	7.55	4	4
Liver Cirrhosis Liver disease in which the normal microcirculation, the gross vascular anatomy, and the hepatic architecture have been variably destroyed and altered with fibrous septa surrounding regenerated or regenerating parenchymal nodules.	0	4.43	1	1
Liver Neoplasms Tumors or cancer of the LIVER.	0	7.55	4	4
Lung Neoplasms Tumors or cancer of the LUNG.	0	4.43	1	1
Muscular Diseases Acquired, familial, and congenital disorders of SKELETAL MUSCLE and SMOOTH MUSCLE.	0	4.43	1	1
Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.	0	4.43	1	1
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	0	7.55	4	4
Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms.	0	7.55	4	4
Neuroblastoma A common neoplasm of early childhood arising from neural crest cells in the sympathetic nervous system, and characterized by diverse clinical behavior, ranging from spontaneous remission to rapid metastatic progression and death. This tumor is the most common intraabdominal malignancy of childhood, but it may also arise from thorax, neck, or rarely occur in the central nervous system. Histologic features include uniform round cells with hyperchromatic nuclei arranged in nests and separated by fibrovascular septa. Neuroblastomas may be associated with the opsoclonus-myoclonus syndrome. (From DeVita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2099-2101; Curr Opin Oncol 1998 Jan;10(1):43-51)	0	4.43	1	1
Obesity, Morbid The condition of weighing two, three, or more times the ideal weight, so called because it is associated with many serious and life-threatening disorders. In the BODY MASS INDEX, morbid obesity is defined as having a BMI greater than 40.0 kg/m2.	0	4.43	1	1
Osteoporosis Reduction of bone mass without alteration in the composition of bone, leading to fractures. Primary osteoporosis can be of two major types: postmenopausal osteoporosis (OSTEOPOROSIS, POSTMENOPAUSAL) and age-related or senile osteoporosis.	0	7.55	4	4
Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.	0	4.43	1	1
Pancreatic Neoplasms Tumors or cancer of the PANCREAS. Depending on the types of ISLET CELLS present in the tumors, various hormones can be secreted: GLUCAGON from PANCREATIC ALPHA CELLS; INSULIN from PANCREATIC BETA CELLS; and SOMATOSTATIN from the SOMATOSTATIN-SECRETING CELLS. Most are malignant except the insulin-producing tumors (INSULINOMA).	0	9.74	9	9
Pneumonia Infection of the lung often accompanied by inflammation.	0	4.43	1	1
Pneumonia, Viral Inflammation of the lung parenchyma that is caused by a viral infection.	0	9.74	9	9
Prediabetic State The time period before the development of symptomatic diabetes. For example, certain risk factors can be observed in subjects who subsequently develop INSULIN RESISTANCE as in type 2 diabetes (DIABETES MELLITUS, TYPE 2).	0	4.43	1	1
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	0	11.38	16	16
Respiratory Distress Syndrome A syndrome characterized by progressive life-threatening RESPIRATORY INSUFFICIENCY in the absence of known LUNG DISEASES, usually following a systemic insult such as surgery or major TRAUMA.	0	4.43	1	1
Respiratory Insufficiency Failure to adequately provide oxygen to cells of the body and to remove excess carbon dioxide from them. (Stedman, 25th ed)	0	4.43	1	1
Salivary Gland Neoplasms Tumors or cancer of the SALIVARY GLANDS.	0	4.43	1	1
Skin Neoplasms Tumors or cancer of the SKIN.	0	4.43	1	1
Thrombosis Formation and development of a thrombus or blood clot in the blood vessel.	0	4.43	1	1
Thyroid Neoplasms Tumors or cancer of the THYROID GLAND.	0	4.43	1	1
Tuberculosis, Pulmonary MYCOBACTERIUM infections of the lung.	0	4.43	1	1
Uveitis Inflammation of part or all of the uvea, the middle (vascular) tunic of the eye, and commonly involving the other tunics (sclera and cornea, and the retina). (Dorland, 27th ed)	0	4.43	1	1
Vitamin D Deficiency A nutritional condition produced by a deficiency of VITAMIN D in the diet, insufficient production of vitamin D in the skin, inadequate absorption of vitamin D from the diet, or abnormal conversion of vitamin D to its bioactive metabolites. It is manifested clinically as RICKETS in children and OSTEOMALACIA in adults. (From Cecil Textbook of Medicine, 19th ed, p1406)	0	4.43	1	1
Wounds and Injuries Damage inflicted on the body as the direct or indirect result of an external force, with or without disruption of structural continuity.	0	4.43	1	1
Reperfusion Injury Adverse functional, metabolic, or structural changes in tissues that result from the restoration of blood flow to the tissue (REPERFUSION) following ISCHEMIA.	0	4.43	1	1
HIV Infections Includes the spectrum of human immunodeficiency virus infections that range from asymptomatic seropositivity, thru AIDS-related complex (ARC), to acquired immunodeficiency syndrome (AIDS).	0	4.43	1	1
Osteoporosis, Postmenopausal Metabolic disorder associated with fractures of the femoral neck, vertebrae, and distal forearm. It occurs commonly in women within 15-20 years after menopause, and is caused by factors associated with menopause including estrogen deficiency.	0	4.43	1	1
Spinal Fractures Broken bones in the vertebral column.	0	4.43	1	1
Gram-Negative Bacterial Infections Infections caused by bacteria that show up as pink (negative) when treated by the gram-staining method.	0	7.55	4	4
Lung Diseases, Interstitial A diverse group of lung diseases that affect the lung parenchyma. They are characterized by an initial inflammation of PULMONARY ALVEOLI that extends to the interstitium and beyond leading to diffuse PULMONARY FIBROSIS. Interstitial lung diseases are classified by their etiology (known or unknown causes), and radiological-pathological features.	0	4.43	1	1
Tuberculosis, Multidrug-Resistant Tuberculosis resistant to chemotherapy with two or more ANTITUBERCULAR AGENTS, including at least ISONIAZID and RIFAMPICIN. The problem of resistance is particularly troublesome in tuberculous OPPORTUNISTIC INFECTIONS associated with HIV INFECTIONS. It requires the use of second line drugs which are more toxic than the first line regimens. TB with isolates that have developed further resistance to at least three of the six classes of second line drugs is defined as EXTENSIVELY DRUG-RESISTANT TUBERCULOSIS.	0	4.43	1	1
Coronavirus Infections Virus diseases caused by the CORONAVIRUS genus. Some specifics include transmissible enteritis of turkeys (ENTERITIS, TRANSMISSIBLE, OF TURKEYS); FELINE INFECTIOUS PERITONITIS; and transmissible gastroenteritis of swine (GASTROENTERITIS, TRANSMISSIBLE, OF SWINE).	0	9.74	9	9
Hepatitis B, Chronic INFLAMMATION of the LIVER in humans caused by HEPATITIS B VIRUS lasting six months or more. It is primarily transmitted by parenteral exposure, such as transfusion of contaminated blood or blood products, but can also be transmitted via sexual or intimate personal contact.	0	4.43	1	1
Brain Infarction Tissue NECROSIS in any area of the brain, including the CEREBRAL HEMISPHERES, the CEREBELLUM, and the BRAIN STEM. Brain infarction is the result of a cascade of events initiated by inadequate blood flow through the brain that is followed by HYPOXIA and HYPOGLYCEMIA in brain tissue. Damage may be temporary, permanent, selective or pan-necrosis.	0	4.43	1	1
Stroke A group of pathological conditions characterized by sudden, non-convulsive loss of neurological function due to BRAIN ISCHEMIA or INTRACRANIAL HEMORRHAGES. Stroke is classified by the type of tissue NECROSIS, such as the anatomic location, vasculature involved, etiology, age of the affected individual, and hemorrhagic vs. non-hemorrhagic nature. (From Adams et al., Principles of Neurology, 6th ed, pp777-810)	0	4.43	1	1
Lymphoma, Mantle-Cell A form of non-Hodgkin lymphoma having a usually diffuse pattern with both small and medium lymphocytes and small cleaved cells. It accounts for about 5% of adult non-Hodgkin lymphomas in the United States and Europe. The majority of mantle-cell lymphomas are associated with a t(11;14) translocation resulting in overexpression of the CYCLIN D1 gene (GENES, BCL-1).	0	4.43	1	1
Carcinoma, Pancreatic Ductal Carcinoma that arises from the PANCREATIC DUCTS. It accounts for the majority of cancers derived from the PANCREAS.	0	4.43	1	1
Pulmonary Disease, Chronic Obstructive A disease of chronic diffuse irreversible airflow obstruction. Subcategories of COPD include CHRONIC BRONCHITIS and PULMONARY EMPHYSEMA.	0	4.43	1	1
Carcinoma, Ductal Malignant neoplasms involving the ductal systems of any of a number of organs, such as the MAMMARY GLANDS, the PANCREAS, the PROSTATE, or the LACRIMAL GLAND.	0	4.43	1	1
Gastrointestinal Stromal Tumors All tumors in the GASTROINTESTINAL TRACT arising from mesenchymal cells (MESODERM) except those of smooth muscle cells (LEIOMYOMA) or Schwann cells (SCHWANNOMA).	0	4.43	1	1
Atherosclerosis A thickening and loss of elasticity of the walls of ARTERIES that occurs with formation of ATHEROSCLEROTIC PLAQUES within the ARTERIAL INTIMA.	0	7.55	4	4
Fractures, Bone Breaks in bones.	0	4.43	1	1
Renal Insufficiency, Chronic Conditions in which the KIDNEYS perform below the normal level for more than three months. Chronic kidney insufficiency is classified by five stages according to the decline in GLOMERULAR FILTRATION RATE and the degree of kidney damage (as measured by the level of PROTEINURIA). The most severe form is the end-stage renal disease (CHRONIC KIDNEY FAILURE). (Kidney Foundation: Kidney Disease Outcome Quality Initiative, 2002)	0	7.55	4	4
Acute Lung Injury A condition of lung damage that is characterized by bilateral pulmonary infiltrates (PULMONARY EDEMA) rich in NEUTROPHILS, and in the absence of clinical HEART FAILURE. This can represent a spectrum of pulmonary lesions, endothelial and epithelial, due to numerous factors (physical, chemical, or biological).	0	4.43	1	1
Rhinitis, Allergic An inflammation of the NASAL MUCOSA triggered by ALLERGENS.	0	4.43	1	1
Thyroid Carcinoma, Anaplastic An aggressive THYROID GLAND malignancy which generally occurs in IODINE-deficient areas in people with previous thyroid pathology such as GOITER. It is associated with CELL DEDIFFERENTIATION of THYROID CARCINOMA (e.g., FOLLICULAR THYROID CARCINOMA; PAPILLARY THYROID CANCER). Typical initial presentation is a rapidly growing neck mass which upon metastasis is associated with DYSPHAGIA; NECK PAIN; bone pain; DYSPNEA; and NEUROLOGIC DEFICITS.	0	4.43	1	1
Amentia [description not available]	0	3.17	1	0
Dementia An acquired organic mental disorder with loss of intellectual abilities of sufficient severity to interfere with social or occupational functioning. The dysfunction is multifaceted and involves memory, behavior, personality, judgment, attention, spatial relations, language, abstract thought, and other executive functions. The intellectual decline is usually progressive, and initially spares the level of consciousness.	0	3.17	1	0
Arrhythmia [description not available]	0	7.15	1	0
Arrhythmias, Cardiac Any disturbances of the normal rhythmic beating of the heart or MYOCARDIAL CONTRACTION. Cardiac arrhythmias can be classified by the abnormalities in HEART RATE, disorders of electrical impulse generation, or impulse conduction.	0	2.15	1	0
Sleepiness Compelling urge to sleep.	0	3.09	1	0
Hypersomnolence, CNS, Idiopathic [description not available]	0	3.46	2	0
Idiopathic Hypersomnia A sleep disorder of central nervous system origin characterized by prolonged nocturnal sleep and periods of daytime drowsiness. Affected individuals experience difficulty with awakening in the morning and may have associated sleep drunkenness, automatic behaviors, and memory disturbances. This condition differs from narcolepsy in that daytime sleep periods are longer, there is no association with CATAPLEXY, and the multiple sleep latency onset test does not record sleep-onset rapid eye movement sleep. (From Chokroverty, Sleep Disorders Medicine, 1994, pp319-20; Psychiatry Clin Neurosci 1998 Apr:52(2):125-129)	1	5.46	2	0
Audiogenic Epilepsy [description not available]	0	3.47	1	1
Epilepsy, Reflex A subtype of epilepsy characterized by seizures that are consistently provoked by a certain specific stimulus. Auditory, visual, and somatosensory stimuli as well as the acts of writing, reading, eating, and decision making are examples of events or activities that may induce seizure activity in affected individuals. (From Neurol Clin 1994 Feb;12(1):57-8)	0	3.47	1	1
Age-Related Memory Disorders [description not available]	0	2.13	1	0
Memory Disorders Disturbances in registering an impression, in the retention of an acquired impression, or in the recall of an impression. Memory impairments are associated with DEMENTIA; CRANIOCEREBRAL TRAUMA; ENCEPHALITIS; ALCOHOLISM (see also ALCOHOL AMNESTIC DISORDER); SCHIZOPHRENIA; and other conditions.	0	2.13	1	0
Electrocardiogram QT Prolonged [description not available]	0	3.51	1	1
Long QT Syndrome A condition that is characterized by episodes of fainting (SYNCOPE) and varying degree of ventricular arrhythmia as indicated by the prolonged QT interval. The inherited forms are caused by mutation of genes encoding cardiac ion channel proteins. The two major forms are ROMANO-WARD SYNDROME and JERVELL-LANGE NIELSEN SYNDROME.	0	3.51	1	1
Nervous System Disorders [description not available]	0	3.06	1	0
Nervous System Diseases Diseases of the central and peripheral nervous system. This includes disorders of the brain, spinal cord, cranial nerves, peripheral nerves, nerve roots, autonomic nervous system, neuromuscular junction, and muscle.	0	3.06	1	0
Chronic Motor and Vocal Tic Disorder [description not available]	0	2.07	1	0
Tourette Syndrome A neuropsychological disorder related to alterations in DOPAMINE metabolism and neurotransmission involving frontal-subcortical neuronal circuits. Both multiple motor and one or more vocal tics need to be present with TICS occurring many times a day, nearly daily, over a period of more than one year. The onset is before age 18 and the disturbance is not due to direct physiological effects of a substance or another medical condition. The disturbance causes marked distress or significant impairment in social, occupational, or other important areas of functioning. (From DSM-IV, 1994; Neurol Clin 1997 May;15(2):357-79)	0	2.07	1	0
Hypothermia, Accidental [description not available]	0	2.07	1	0
Ache [description not available]	0	2.07	1	0
Hypothermia Lower than normal body temperature, especially in warm-blooded animals.	0	2.07	1	0
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	0	7.07	1	0
Dementia Praecox [description not available]	0	2.03	1	0
Schizophrenia A severe emotional disorder of psychotic depth characteristically marked by a retreat from reality with delusion formation, HALLUCINATIONS, emotional disharmony, and regressive behavior.	1	4.03	1	0

pitolisant

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Dosage Studied

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Protein Targets (10)

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Research Demand Index: 82.62

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pitolisant

Description

Cross-References

Synonyms (53)

Research Excerpts

Overview

Treatment

Toxicity

Pharmacokinetics

Dosage Studied

Drug Classes (1)

Protein Targets (10)

Potency Measurements

Inhibition Measurements

Activation Measurements

Other Measurements

Biological Processes (39)

Molecular Functions (16)

Ceullar Components (10)

Bioassays (65)

Research

Studies (93)

Market Indicators

Research Demand Index: 82.62

Study Types

Related Drugs (160)

Related Conditions (249)