Page last updated: 2024-12-11

rmp 7

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

RMP 7: a synthetic bradykinin analog; selectively increases uptake of molecular tracers in RG2 glial tumors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	6918284
CHEMBL ID	2105864
SCHEMBL ID	411837
MeSH ID	M0237580

Synonyms (31)

Synonym
gtpl672
[hyp3,thi5,4-me-tyr8psi(ch2-nh)arg9]bradykinin
labradimil
rmp-7
cereport
lobradimil
159768-75-9
(2s)-2-[[(2s)-2-[[(2s)-1-[(2s)-2-[[(2s)-2-[[2-[[(2s,4r)-1-[(2s)-1-[(2s)-2-amino-5-(diaminomethylideneamino)pentanoyl]pyrrolidine-2-carbonyl]-4-hydroxypyrrolidine-2-carbonyl]amino]acetyl]amino]-3-thiophen-2-ylpropanoyl]amino]-3-hydroxypropanoyl]pyrrolidine
rmp 7
CHEMBL2105864
l-prolinamide, l-arginyl-l-prolyl-trans-4-hydroxy-l-prolyl-3-(2-thienyl)-l-alanylglycyl-l-seryl-n-(2-((4-((aminoiminomethyl)amino)-1-carboxybutyl)amino)-1-((4-methoxyphenyl)methyl)ethyl)-, (s-(r,r))-
labradimil [usan:inn]
2mk663c346 ,
bradykinin, 3-(trans-4-hydroxy-l-proline)-5-(3-(2-thienyl)-l-alanine)-8-de-l-phenylalanine-9-(n2-(2-amino-3-(4-methoxyphenyl)propyl)-l-arginine)-, (s)-
n2-((s)-2-(l-arginyl-l-prolyl-trans-4-hydroxy-l-prolylglycyl-3-(2-thienyl)-l-alanyl-l-seryl-l-prolinamido)-3-(p-methoxyphenyl)propyl)-l-arginine
(s-(r,r))-l-arginyl-l-prolyl-trans-4-hydroxy-l-prolyl-3-(2-thienyl)-l-alanylglycyl-l-seryl-n-(2-((4-((aminoiminomethyl)amino)-1-carboxybutyl)amino)-1-((4-methoxyphenyl)methyl)ethyl)-l-prolinamide
n(sup 2)-((s)-2-(l-arginyl-l-prolyl-trans-4-hydroxy-l-prolyglycyl-3-(2-thienyl)-l-alanyl-l-seryl-l-prolinamido)-3-(p-methoxyphenyl)propyl)-l-arginine
(s-(r,r))-l-arginyl-l-prolyl-trans-4-hydroxy-l-prolylglycyl-3-(2-thienyl)-l-alanyl-l-seryl-n-(2-((4-(aminoiminomethyl)amino)-1-carboxybutyl)amino)-1-((4-methoxyphenyl)methyl)ethyl)-l-prolinamide
l-arginine, l-arginyl-l-prolyl-(4r)-4-hydroxy-l-prolyl-3-(2-thienyl)-l-alanylglycyl-l-seryl-l-prolyl-o-methyl-l-tyrosyl-psi(ch2-nh)-
drg-0182
unii-2mk663c346
SCHEMBL411837
173220-35-4
labradimil [inn]
labradimil [usan]
n(sup 2)2-((s)-2-(l-arginyl-l-prolyl-trans-4-hydroxy-l-prolyglycyl-3-(2-thienyl)-l-alanyl-l-seryl-l-prolinamido)-3-(p-methoxyphenyl)propyl)-l-arginine
DB06549
Q27078449
HY-105155
CS-0025139
AKOS040748717

Research Excerpts

Toxicity

Excerpt	Reference	Relevance
" The safer and effective administration of lower doses of CsA combined with enhanced BBB permeability using Cereport, offers a novel way of producing protective effects in the CNS without the toxic liabilities of high-dose CsA."	( Bradykinin receptor agonist facilitates low-dose cyclosporine-A protection against 6-hydroxydopamine neurotoxicity. Bartus, RT; Borlongan, CV; Emerich, DF; Hoffer, BJ, 2002)	0.31

Pharmacokinetics

Excerpt	Reference	Relevance
" Pharmacokinetic parameters for carboplatin were compared with respect to the dose of Cereport and with historical controls."	( Pharmacokinetics of carboplatin administered in combination with the bradykinin agonist Cereport (RMP-7) for the treatment of brain tumours. Bleehen, N; Boddy, AV; Calvert, AH; Ford, J; Lind, MJ; Thomas, HD, 2000)	0.31
"Carboplatin pharmacokinetic studies were performed on 21 of 25 children with primary brain tumors who received carboplatin and lobradimil on two consecutive days every 28 days in a phase I dose-escalation trial of lobradimil."	( Pharmacokinetics of carboplatin administered with lobradimil to pediatric patients with brain tumors. Aikin, A; Balis, FM; Egorin, M; Gervais, A; Warren, K, 2004)	0.32
" The degree to which the measured carboplatin AUC exceeded the target AUC appeared to be greater at higher doses of lobradimil, suggesting that the failure of the adaptive dosing method was related to an unexpected pharmacokinetic drug interaction."	( Pharmacokinetics of carboplatin administered with lobradimil to pediatric patients with brain tumors. Aikin, A; Balis, FM; Egorin, M; Gervais, A; Warren, K, 2004)	0.32

Compound-Compound Interactions

Excerpt	Reference	Relevance
" In order to investigate the pharmacokinetics of carboplatin in combination with Cereport, we performed pharmacological studies in conjunction with early clinical trials."	( Pharmacokinetics of carboplatin administered in combination with the bradykinin agonist Cereport (RMP-7) for the treatment of brain tumours. Bleehen, N; Boddy, AV; Calvert, AH; Ford, J; Lind, MJ; Thomas, HD, 2000)	0.31
"Cereport combined with carboplatin was well-tolerated, with mild haematological toxicities consistent with the target area under the concentration time curve (AUC) of 7 mg/ml x min."	( Pharmacokinetics of carboplatin administered in combination with the bradykinin agonist Cereport (RMP-7) for the treatment of brain tumours. Bleehen, N; Boddy, AV; Calvert, AH; Ford, J; Lind, MJ; Thomas, HD, 2000)	0.31
"To determine the pharmacokinetics of adaptively dosed carboplatin when administered in combination with the bradykinin agonist, lobradimil (RMP-7, Cereport), to pediatric patients with brain tumors."	( Pharmacokinetics of carboplatin administered with lobradimil to pediatric patients with brain tumors. Aikin, A; Balis, FM; Egorin, M; Gervais, A; Warren, K, 2004)	0.32

Bioavailability

Excerpt	Reference	Relevance
" Tight junction (TJ) modulation offers an approach to increase bioavailability of pharmaceutical compounds."	( Recent progress in tight junction modulation for improving bioavailability. Baumann, K; Reichl, S; Saaber, D; Wollenhaupt, S, 2014)	0.4

Dosage Studied

Excerpt	Relevance	Reference
" dosing regimens included pre-treatment with RMP-7 (0."	( Intravenous infusion of RMP-7 increases ocular uptake of ganciclovir. Bartus, RT; Elliot, PJ; Mackic, JB; Zlokovic, BV, 1997)	0.3
" For each subject, one of the alternating dosing sequences (above) was repeated four times during a single dosing session which lasted approximately 40 minutes."	( Intra-arterial administration of carboplatin and the blood brain barrier permeabilizing agent, RMP-7: a toxicologic evaluation in swine. Bartus, RT; Black, KL; Gobin, YP; Kim, NN; LeBel, CP; Riley, MG; Watson, VE, 1998)	0.3
" A high dosage (100 mg of GCV/kg/day) eradicated all HSV-tk- and HSV-tk+ tumors."	( Intravenous RMP-7 increases delivery of ganciclovir into rat brain tumors and enhances the effects of herpes simplex virus thymidine kinase gene therapy. Anderson, WF; Bartus, R; Gordon, EM; Gray, B; Jovanovic, S; Kittaka, M; LeMay, DR; McComb, JG; Stins, MF; Tabrizi, P; Weiss, MH; Zlokovic, BV, 1998)	0.3
" Carboplatin dosing was by target area under the curve (AUC) according to the Calvert protocol."	( A phase I study of intravenous RMP-7 with carboplatin in patients with progression of malignant glioma. Barton, T; Bleehen, NM; Ford, J; Osborn, C, 1998)	0.3
" Collectively, these data provide the first systematic evaluation of dosing parameters involving receptor-mediated changes in BBTB permeability and provide new information regarding the pharmacodynamics and potential clinical use of Cereport."	( Enhanced delivery of carboplatin into brain tumours with intravenous Cereport (RMP-7): dramatic differences and insight gained from dosing parameters. Agostino, M; Bartus, RT; Dean, R; Emerich, DF; Hasler, B; Kim, BS; Pink, M; Snodgrass, P; Xiong, H, 1999)	0.3
" Neurological impairment, performance status and steroid use were measured prior to dosing at each cycle and tumour volume by 3-D MRI at the end of cycles 2, 4, 6, 9 and 12."	( Phase II studies of RMP-7 and carboplatin in the treatment of recurrent high grade glioma. RMP-7 European Study Group. Barton, T; Grant, R; Gregor, A; Hadley, DM; Lind, M; Newman, H; Osborn, C, 1999)	0.3
" However, immunosuppressant side effects (including nephrotoxicity and hepatotoxicity) are associated with such CsA dosing regimens."	( Bradykinin receptor agonist facilitates low-dose cyclosporine-A protection against 6-hydroxydopamine neurotoxicity. Bartus, RT; Borlongan, CV; Emerich, DF; Hoffer, BJ, 2002)	0.31
"To determine the pharmacokinetics of adaptively dosed carboplatin when administered in combination with the bradykinin agonist, lobradimil (RMP-7, Cereport), to pediatric patients with brain tumors."	( Pharmacokinetics of carboplatin administered with lobradimil to pediatric patients with brain tumors. Aikin, A; Balis, FM; Egorin, M; Gervais, A; Warren, K, 2004)	0.32
" The adaptive dosing formula was: carboplatin dose (mg/m2)=target AUC (mg."	( Pharmacokinetics of carboplatin administered with lobradimil to pediatric patients with brain tumors. Aikin, A; Balis, FM; Egorin, M; Gervais, A; Warren, K, 2004)	0.32
"Adaptive dosing of carboplatin based on GFR overestimated the dose required to achieve the target carboplatin AUC in pediatric patients with brain tumors treated with concurrent lobradimil."	( Pharmacokinetics of carboplatin administered with lobradimil to pediatric patients with brain tumors. Aikin, A; Balis, FM; Egorin, M; Gervais, A; Warren, K, 2004)	0.32

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
B2 bradykinin receptor	Homo sapiens (human)	Ki	0.0190	0.0000	0.7057	7.6740	AID43286
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (16)

Process	via Protein(s)	Taxonomy
smooth muscle contraction	B2 bradykinin receptor	Homo sapiens (human)
inflammatory response	B2 bradykinin receptor	Homo sapiens (human)
cell surface receptor signaling pathway	B2 bradykinin receptor	Homo sapiens (human)
cell surface receptor protein tyrosine kinase signaling pathway	B2 bradykinin receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	B2 bradykinin receptor	Homo sapiens (human)
blood circulation	B2 bradykinin receptor	Homo sapiens (human)
response to salt stress	B2 bradykinin receptor	Homo sapiens (human)
regulation of vasoconstriction	B2 bradykinin receptor	Homo sapiens (human)
negative regulation of peptidyl-serine phosphorylation	B2 bradykinin receptor	Homo sapiens (human)
vasoconstriction	B2 bradykinin receptor	Homo sapiens (human)
vasodilation	B2 bradykinin receptor	Homo sapiens (human)
regulation of vascular permeability	B2 bradykinin receptor	Homo sapiens (human)
arachidonic acid secretion	B2 bradykinin receptor	Homo sapiens (human)
negative regulation of intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediator	B2 bradykinin receptor	Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to osmotic stress by p53 class mediator	B2 bradykinin receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	B2 bradykinin receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (6)

Process	via Protein(s)	Taxonomy
protease binding	B2 bradykinin receptor	Homo sapiens (human)
phosphatidylinositol phospholipase C activity	B2 bradykinin receptor	Homo sapiens (human)
bradykinin receptor activity	B2 bradykinin receptor	Homo sapiens (human)
protein binding	B2 bradykinin receptor	Homo sapiens (human)
type 1 angiotensin receptor binding	B2 bradykinin receptor	Homo sapiens (human)
protein heterodimerization activity	B2 bradykinin receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Process	via Protein(s)	Taxonomy
endosome	B2 bradykinin receptor	Homo sapiens (human)
Golgi apparatus	B2 bradykinin receptor	Homo sapiens (human)
plasma membrane	B2 bradykinin receptor	Homo sapiens (human)
intracellular membrane-bounded organelle	B2 bradykinin receptor	Homo sapiens (human)
plasma membrane	B2 bradykinin receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5)

Assay ID	Title	Year	Journal	Article
AID1347008	Rat B2 receptor (Bradykinin receptors)	1999	Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20	Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.
AID1347008	Rat B2 receptor (Bradykinin receptors)	1994	The Journal of pharmacology and experimental therapeutics, Oct, Volume: 271, Issue:1	The bradykinin analog RMP-7 increases intracellular free calcium levels in rat brain microvascular endothelial cells.
AID92692	Agonistic activity on human umbilical vein(HUV) in presence of inhibitors	1999	Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20	Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.
AID43286	Binding affinity against human cloned Bradykinin receptor B2 expressed in CHO cells using [3H]-bradykinin as radioligand	1999	Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20	Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.
AID92588	Agonistic activity on human umbilical vein(HUV) in absence of inhibitors	1999	Journal of medicinal chemistry, Oct-07, Volume: 42, Issue:20	Design and synthesis of potent bradykinin agonists containing a benzothiazepine moiety.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (65)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	33 (50.77)	18.2507
2000's	28 (43.08)	29.6817
2010's	4 (6.15)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.41

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

Metric	This Compound (vs All)
Research Demand Index	17.41 (24.57)
Research Supply Index	4.39 (2.92)
Research Growth Index	4.18 (4.65)
Search Engine Demand Index	15.26 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (17.41)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	12 (17.65%)	5.53%
Reviews	3 (4.41%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	53 (77.94%)	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
histamine [no description available]	1.99	1	0	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
carmustine Carmustine: A cell-cycle phase nonspecific alkylating antineoplastic agent. It is used in the treatment of brain tumors and various other malignant neoplasms. (From Martindale, The Extra Pharmacopoeia, 30th ed, p462) This substance may reasonably be anticipated to be a carcinogen according to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985). (From Merck Index, 11th ed). carmustine : A member of the class of N-nitrosoureas that is 1,3-bis(2-chloroethyl)urea in which one of the nitrogens is substituted by a nitroso group.	2.4	2	0	N-nitrosoureas; organochlorine compound	alkylating agent; antineoplastic agent
loperamide Loperamide: One of the long-acting synthetic ANTIDIARRHEALS; it is not significantly absorbed from the gut, and has no effect on the adrenergic system or central nervous system, but may antagonize histamine and interfere with acetylcholine release locally.. loperamide : A synthetic piperidine derivative, effective against diarrhoea resulting from gastroenteritis or inflammatory bowel disease.	1.99	1	0	monocarboxylic acid amide; monochlorobenzenes; piperidines; tertiary alcohol	anticoronaviral agent; antidiarrhoeal drug; mu-opioid receptor agonist
losartan Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.. losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position	2.01	1	0	biphenylyltetrazole; imidazoles	angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist
oxidopamine Oxidopamine: A neurotransmitter analogue that depletes noradrenergic stores in nerve endings and induces a reduction of dopamine levels in the brain. Its mechanism of action is related to the production of cytolytic free-radicals.. oxidopamine : A benzenetriol that is phenethylamine in which the hydrogens at positions 2, 4, and 5 on the phenyl ring are replaced by hydroxy groups. It occurs naturally in human urine, but is also produced as a metabolite of the drug DOPA (used for the treatment of Parkinson's disease).	2.01	1	0	benzenetriol; catecholamine; primary amino compound	drug metabolite; human metabolite; neurotoxin
rolipram [no description available]	2	1	0	pyrrolidin-2-ones	antidepressant; EC 3.1.4.* (phosphoric diester hydrolase) inhibitor
delavirdine Delavirdine: A potent, non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1.. delavirdine : The amide resulting from the formal condensation of 5-[(methylsulfonyl)amino]-1H-indole-2-carboxylic acid and 4-amino group of 1-[3-(isopropylamino)pyridin-2-yl]piperazine, delavirdine is a non-nucleoside reverse transcriptase inhibitor with activity specific for HIV-1. Viral resistance emerges rapidly when delavirdine is used alone, so it is therefore used (as the methanesulfonic acid salt) with other antiretrovirals for combination therapy of HIV infection.	2.07	1	0	aminopyridine; indolecarboxamide; N-acylpiperazine; sulfonamide	antiviral drug; HIV-1 reverse transcriptase inhibitor
sucrose Saccharum: A plant genus of the family POACEAE widely cultivated in the tropics for the sweet cane that is processed into sugar.	1.98	1	0	glycosyl glycoside	algal metabolite; Escherichia coli metabolite; human metabolite; mouse metabolite; osmolyte; Saccharomyces cerevisiae metabolite; sweetening agent
edetic acid Edetic Acid: A chelating agent that sequesters a variety of polyvalent cations such as CALCIUM. It is used in pharmaceutical manufacturing and as a food additive.	3.38	1	1	ethylenediamine derivative; polyamino carboxylic acid; tetracarboxylic acid	anticoagulant; antidote; chelator; copper chelator; geroprotector
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.	2.69	3	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
mannitol [no description available]	2.01	1	0	mannitol	allergen; antiglaucoma drug; compatible osmolytes; Escherichia coli metabolite; food anticaking agent; food bulking agent; food humectant; food stabiliser; food thickening agent; hapten; metabolite; osmotic diuretic; sweetening agent
evans blue Evans Blue: An azo dye used in blood volume and cardiac output measurement by the dye dilution method. It is very soluble, strongly bound to plasma albumin, and disappears very slowly.. Evans blue : An organic sodium salt that is the tetrasodium salt of 6,6'-{(3,3'-dimethyl[1,1'-biphenyl]-4,4'-diyl)bis[diazene-2,1-diyl]}bis(4-amino-5-hydroxynaphthalene-1,3-disulfonate). It is sometimes used as a counterstain, especially in fluorescent methods to suppress background autofluorescence.	2.01	1	0	organic sodium salt	fluorochrome; histological dye; sodium channel blocker; teratogenic agent
deoxycytidine [no description available]	2	1	0	pyrimidine 2'-deoxyribonucleoside	Escherichia coli metabolite; human metabolite; mouse metabolite; Saccharomyces cerevisiae metabolite
stavudine Stavudine: A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV.. stavudine : A nucleoside analogue obtained by formal dehydration across positions 2 and 3 of thymidine. An inhibitor of HIV-1 reverse transcriptase	2.07	1	0	dihydrofuran; nucleoside analogue; organic molecular entity	antimetabolite; antiviral agent; EC 2.7.7.49 (RNA-directed DNA polymerase) inhibitor
lanthanum [no description available]	1.98	1	0	f-block element atom; lanthanoid atom; scandium group element atom
platinum Platinum: A heavy, soft, whitish metal, resembling tin, with atomic number 78, atomic weight 195.084, symbol Pt. It is used in manufacturing equipment for laboratory and industrial use. It occurs as a black powder (platinum black) and as a spongy substance (spongy platinum) and may have been known in Pliny's time as alutiae.	2	1	0	elemental platinum; nickel group element atom; platinum group metal atom
transferrin Transferrin: An iron-binding beta1-globulin that is synthesized in the LIVER and secreted into the blood. It plays a central role in the transport of IRON throughout the circulation. A variety of transferrin isoforms exist in humans, including some that are considered markers for specific disease states.	2.1	1	0
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).	2	1	0	taxane diterpenoid; tetracyclic diterpenoid	antineoplastic agent; human metabolite; metabolite; microtubule-stabilising agent
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.	2	1	0	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
ammonium peroxydisulfate ammonium persulfate : An inorganic ammonium salt in which two of the terminal hydroxy groups of peroxydisulfuric acid are deprotonated and associated with ammonium ions as counter-cations.	2.07	1	0
1,2-distearoylphosphatidylethanolamine 1,2-distearoylphosphatidylethanolamine: RN given refers to cpd without isomeric designation. 1,2-distearoylphosphatidylethanolamine : A phosphatidylethanolamine in which the phosphatidyl acyl group at C-1 and C-2 is stearoyl.	2.42	2	0	phosphatidylethanolamine zwitterion; phosphatidylethanolamine	human metabolite
4-boronophenylalanine 4-boronophenylalanine: neutron absorbing (10)B-cpd used in thermal neutron capturetherapy of malignant melanoma; RN given refers to (L)-isomer; structure given in first source	2.69	3	0
biotin vitamin B7 : Any member of a group of vitamers that belong to the chemical structural class called biotins that exhibit biological activity against vitamin B7 deficiency. Vitamin B7 deficiency is very rare in individuals who take a normal balanced diet. Foods rich in biotin are egg yolk, liver, cereals, vegetables (spinach, mushrooms) and rice. Symptoms associated with vitamin B7 deficiency include thinning hair, scaly skin rashes around eyes, nose and mouth, and brittle nails. The vitamers include biotin and its ionized and salt forms.	1.99	1	0	biotins; vitamin B7	coenzyme; cofactor; Escherichia coli metabolite; fundamental metabolite; human metabolite; mouse metabolite; nutraceutical; prosthetic group; Saccharomyces cerevisiae metabolite
carboplatin [no description available]	10.77	29	14
bradykinin [no description available]	13.8	67	14	oligopeptide	human blood serum metabolite; vasodilator agent
nitroarginine Nitroarginine: An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6). N(gamma)-nitro-L-arginine : An L-arginine derivative that is L-arginine in which the terminal nitrogen of the guanidyl group is replaced by a nitro group.	2.01	1	0	guanidines; L-arginine derivative; N-nitro compound; non-proteinogenic L-alpha-amino acid
saquinavir Saquinavir: An HIV protease inhibitor which acts as an analog of an HIV protease cleavage site. It is a highly specific inhibitor of HIV-1 and HIV-2 proteases, and also inhibits CYTOCHROME P-450 CYP3A.. saquinavir : An aspartic acid derivative obtained by formal condensation of the primary amino group of (2S,3R)-4-[(3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl]-3-hydroxy-1-phenylbutan-2-ylamine with the carboxy group of N(2)(-quinolin-2-ylcarbonyl)-L-asparagine. An inhibitor of HIV-1 protease.	2.07	1	0	L-asparagine derivative; quinolines	antiviral drug; HIV protease inhibitor
quercetin [no description available]	2.15	1	0	7-hydroxyflavonol; pentahydroxyflavone	antibacterial agent; antineoplastic agent; antioxidant; Aurora kinase inhibitor; chelator; EC 1.10.99.2 [ribosyldihydronicotinamide dehydrogenase (quinone)] inhibitor; geroprotector; phytoestrogen; plant metabolite; protein kinase inhibitor; radical scavenger
amphotericin b Amphotericin B: Macrolide antifungal antibiotic produced by Streptomyces nodosus obtained from soil of the Orinoco river region of Venezuela.. amphotericin B : A macrolide antibiotic used to treat potentially life-threatening fungal infections.	2.42	2	0	antibiotic antifungal drug; macrolide antibiotic; polyene antibiotic	antiamoebic agent; antiprotozoal drug; bacterial metabolite
enalaprilat anhydrous Enalaprilat: The active metabolite of ENALAPRIL and one of the potent, intravenously administered, ANGIOTENSIN-CONVERTING ENZYME INHIBITORS. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.. enalaprilat dihydrate : The dihydrate form of enalaprilat, an angiotensin-converting enzyme (ACE) inhibitor that is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is administered by intravenous injection.. enalaprilat (anhydrous) : Enalapril in which the ethyl ester group has been hydrolysed to the corresponding carboxylic acid. Enalaprilat is an angiotensin-converting enzyme (ACE) inhibitor and is used (often in the form of its prodrug, enalapril) in the treatment of hypertension and heart failure, for reduction of proteinuria and renal disease in patients with nephropathies, and for the prevention of stroke, myocardial infarction, and cardiac death in high-risk patients. Unlike enalapril, enalaprilat is not absorbed by mouth but is given by intravenous injection, usually as the dihydrate.	2.01	1	0	dicarboxylic acid; dipeptide	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
ammonium sulfate Ammonium Sulfate: Sulfuric acid diammonium salt. It is used in CHEMICAL FRACTIONATION of proteins.. ammonium sulfate : An inorganic sulfate salt obtained by reaction of sulfuric acid with two equivalents of ammonia. A high-melting (decomposes above 280degreeC) white solid which is very soluble in water (70.6 g/100 g water at 0degreeC; 103.8 g/100 g water at 100degreeC), it is widely used as a fertilizer for alkaline soils.	2.07	1	0	ammonium salt; inorganic sulfate salt	fertilizer
icatibant [no description available]	2	1	0	oligopeptide	beta-adrenergic antagonist; bradykinin receptor antagonist; peptidomimetic
indocyanine green Indocyanine Green: A tricarbocyanine dye that is used diagnostically in liver function tests and to determine blood volume and cardiac output.	2.01	1	0	1,1-diunsubstituted alkanesulfonate; benzoindole; cyanine dye
icatibant icatibant: a potent bradykinin (B2) receptor antagonist; WIN 65365 is an L-Tic(7) stereoisomer. icatibant : A ten-membered synthetic oligopeptide consisting of D-Arg, Arg, Pro, Hyp, Gly, Thi, Ser, D-Tic, Oic, and Arg residues joined in sequrence. A bradykinin receptor antagonist used as its acetate salt for the treatment of acute attacks of hereditary angioedema in adult patients.	2	1	0
cyclosporine Cyclosporine: A cyclic undecapeptide from an extract of soil fungi. It is a powerful immunosupressant with a specific action on T-lymphocytes. It is used for the prophylaxis of graft rejection in organ and tissue transplantation. (From Martindale, The Extra Pharmacopoeia, 30th ed).	2.01	1	0
lactoferrin Lactoferrin: An iron-binding protein that was originally characterized as a milk protein. It is widely distributed in secretory fluids and is found in the neutrophilic granules of LEUKOCYTES. The N-terminal part of lactoferrin possesses a serine protease which functions to inactivate the TYPE III SECRETION SYSTEM used by bacteria to export virulence proteins for host cell invasion.	2.15	1	0
acyclovir Acyclovir: A GUANOSINE analog that acts as an antimetabolite. Viruses are especially susceptible. Used especially against herpes.. acyclovir : An oxopurine that is guanine substituted by a (2-hydroxyethoxy)methyl substituent at position 9. Used in the treatment of viral infections.	2	1	0	2-aminopurines; oxopurine	antimetabolite; antiviral drug
ganciclovir [no description available]	2.68	3	0	2-aminopurines; oxopurine	antiinfective agent; antiviral drug
zaprinast zaprinast: anaphylaxis inhibitor; structure	2	1	0	triazolopyrimidines

Condition	Indicated	Relationship Strength	Studies	Trials
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	0	2.4	2	0
Acute Confusional Senile Dementia [description not available]	0	2.52	2	0
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	2.52	2	0
HIV Coinfection [description not available]	0	2.07	1	0
HIV Human immunodeficiency virus. A non-taxonomic and historical term referring to any of two species, specifically HIV-1 and/or HIV-2. Prior to 1986, this was called human T-lymphotropic virus type III/lymphadenopathy-associated virus (HTLV-III/LAV). From 1986-1990, it was an official species called HIV. Since 1991, HIV was no longer considered an official species name; the two species were designated HIV-1 and HIV-2.	0	2.07	1	0
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	2.07	1	0
Anaplastic Astrocytoma [description not available]	0	4.64	3	2
Benign Neoplasms, Brain [description not available]	0	9.77	30	9
Astrocytoma, Grade IV [description not available]	0	10.17	12	12
Astrocytoma Neoplasms of the brain and spinal cord derived from glial cells which vary from histologically benign forms to highly anaplastic and malignant tumors. Fibrillary astrocytomas are the most common type and may be classified in order of increasing malignancy (grades I through IV). In the first two decades of life, astrocytomas tend to originate in the cerebellar hemispheres; in adults, they most frequently arise in the cerebrum and frequently undergo malignant transformation. (From Devita et al., Cancer: Principles and Practice of Oncology, 5th ed, pp2013-7; Holland et al., Cancer Medicine, 3d ed, p1082)	0	4.64	3	2
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	9.77	30	9
Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.	0	10.17	12	12
Autosomal Dominant Juvenile Parkinson Disease [description not available]	0	2.01	1	0
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	0	2.41	2	0
Idiopathic Parkinson Disease [description not available]	0	2.01	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)	0	2.01	1	0
Parkinsonian Disorders A group of disorders which feature impaired motor control characterized by bradykinesia, MUSCLE RIGIDITY; TREMOR; and postural instability. Parkinsonian diseases are generally divided into primary parkinsonism (see PARKINSON DISEASE), secondary parkinsonism (see PARKINSON DISEASE, SECONDARY) and inherited forms. These conditions are associated with dysfunction of dopaminergic or closely related motor integration neuronal pathways in the BASAL GANGLIA.	0	2.01	1	0
Glial Cell Tumors [description not available]	0	12.47	34	15
Local Neoplasm Recurrence [description not available]	0	10.24	13	12
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)	1	14.47	34	15
Fungal Meningitis [description not available]	0	2.02	1	0
Brain Stem Neoplasms, Primary [description not available]	0	5.29	2	2
Brain Stem Neoplasms Benign and malignant intra-axial tumors of the MESENCEPHALON; PONS; or MEDULLA OBLONGATA of the BRAIN STEM. Primary and metastatic neoplasms may occur in this location. Clinical features include ATAXIA, cranial neuropathies (see CRANIAL NERVE DISEASES), NAUSEA, hemiparesis (see HEMIPLEGIA), and quadriparesis. Primary brain stem neoplasms are more frequent in children. Histologic subtypes include GLIOMA; HEMANGIOBLASTOMA; GANGLIOGLIOMA; and EPENDYMOMA.	0	5.29	2	2
Blood Pressure, Low [description not available]	0	5.39	5	1
Hypotension Abnormally low BLOOD PRESSURE that can result in inadequate blood flow to the brain and other vital organs. Common symptom is DIZZINESS but greater negative impacts on the body occur when there is prolonged depravation of oxygen and nutrients.	0	5.39	5	1
Sensitivity and Specificity Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)	0	1.99	1	0
Brain Swelling [description not available]	0	1.99	1	0
Experimental Radiation Injuries [description not available]	0	1.99	1	0
Brain Edema Increased intracellular or extracellular fluid in brain tissue. Cytotoxic brain edema (swelling due to increased intracellular fluid) is indicative of a disturbance in cell metabolism, and is commonly associated with hypoxic or ischemic injuries (see HYPOXIA, BRAIN). An increase in extracellular fluid may be caused by increased brain capillary permeability (vasogenic edema), an osmotic gradient, local blockages in interstitial fluid pathways, or by obstruction of CSF flow (e.g., obstructive HYDROCEPHALUS). (From Childs Nerv Syst 1992 Sep; 8(6):301-6)	0	1.99	1	0
Experimental Neoplasms [description not available]	0	2.69	3	0
Blood Diseases [description not available]	0	3.38	1	1
Hematologic Diseases Disorders of the blood and blood forming tissues.	0	3.38	1	1
Nervous System Disorders [description not available]	0	2	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	2	1	0
Angiogenesis, Pathologic [description not available]	0	2	1	0
Disease Exacerbation [description not available]	0	3.39	1	1
Experimental Hepatoma [description not available]	0	2	1	0
Cancer of Lung [description not available]	0	2	1	0
Experimental Mammary Neoplasms [description not available]	0	2	1	0
Lung Neoplasms Tumors or cancer of the LUNG.	0	2	1	0
Central Nervous System Neoplasm [description not available]	0	2.92	1	0
Central Nervous System Neoplasms Benign and malignant neoplastic processes that arise from or secondarily involve the brain, spinal cord, or meninges.	1	4.92	1	0
Adenocarcinoma, Basal Cell [description not available]	0	2	1	0
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	0	2	1	0
Acute Necrotizing Encephalitis, Herpetic [description not available]	0	2	1	0
Encephalitis, Herpes Simplex An acute (or rarely chronic) inflammatory process of the brain caused by SIMPLEXVIRUS infections which may be fatal. The majority of infections are caused by human herpesvirus 1 (HERPESVIRUS 1, HUMAN) and less often by human herpesvirus 2 (HERPESVIRUS 2, HUMAN). Clinical manifestations include FEVER; HEADACHE; SEIZURES; HALLUCINATIONS; behavioral alterations; APHASIA; hemiparesis; and COMA. Pathologically, the condition is marked by a hemorrhagic necrosis involving the medial and inferior TEMPORAL LOBE and orbital regions of the FRONTAL LOBE. (From Adams et al., Principles of Neurology, 6th ed, pp751-4)	0	2	1	0
Body Weight The mass or quantity of heaviness of an individual. It is expressed by units of pounds or kilograms.	0	2	1	0
Bilateral Headache [description not available]	0	4.31	1	1
Absence Seizure [description not available]	0	4.31	1	1
Thrombopenia [description not available]	0	4.31	1	1
Flushing A transient reddening of the face that may be due to fever, certain drugs, exertion, or stress.	0	4.31	1	1
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	4.31	1	1
Neutropenia A decrease in the number of NEUTROPHILS found in the blood.	0	4.31	1	1
Seizures Clinical or subclinical disturbances of cortical function due to a sudden, abnormal, excessive, and disorganized discharge of brain cells. Clinical manifestations include abnormal motor, sensory and psychic phenomena. Recurrent seizures are usually referred to as EPILEPSY or seizure disorder.	0	4.31	1	1
Thrombocytopenia A subnormal level of BLOOD PLATELETS.	0	4.31	1	1
Malignant Melanoma [description not available]	0	2.01	1	0
Melanoma A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)	0	2.01	1	0
Cardiomyopathy, Congestive [description not available]	0	2.01	1	0
Cardiomyopathy, Dilated A form of CARDIAC MUSCLE disease that is characterized by ventricular dilation, VENTRICULAR DYSFUNCTION, and HEART FAILURE. Risk factors include SMOKING; ALCOHOL DRINKING; HYPERTENSION; INFECTION; PREGNANCY; and mutations in the LMNA gene encoding LAMIN TYPE A, a NUCLEAR LAMINA protein.	0	2.01	1	0

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