bms 248360 profile

ID Source	ID
PubMed CID	9895957
CHEMBL ID	11706
SCHEMBL ID	4764273
MeSH ID	M0438856

Synonym
L021638
4''-(2-butyl-4-oxo-1,3-diaza-spiro[4.4]non-1-en-3-ylmethyl)-2''-(3,3-dimethyl-2-oxo-pyrrolidin-1-ylmethyl)-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide
bdbm50117910
4''''-(2-butyl-4-oxo-1,3-diaza-spiro[4.4]non-1-en-3-ylmethyl)-2''''-(3,3-dimethyl-2-oxo-pyrrolidin-1-ylmethyl)-biphenyl-2-sulfonic acid (3,4-dimethyl-isoxazol-5-yl)-amide
bms-248360
CHEMBL11706 ,
254737-87-6
unii-eep77n970y
eep77n970y ,
(1,1'-biphenyl)-2-sulfonamide, 4'-((2-butyl-4-oxo-1,3-diazaspiro(4.4)non-1-en-3-yl)methyl)-n-(3,4-dimethyl-5-isoxazolyl)-2'-((3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl)-
SCHEMBL4764273
bms-248360, >=98% (hplc)
CS-0064693
HY-114953
Q27277140
2-[4-[(2-butyl-4-oxo-1,3-diazaspiro[4.4]non-1-en-3-yl)methyl]-2-[(3,3-dimethyl-2-oxopyrrolidin-1-yl)methyl]phenyl]-n-(3,4-dimethyl-1,2-oxazol-5-yl)benzenesulfonamide
AKOS040741387

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Type-1A angiotensin II receptor	Rattus norvegicus (Norway rat)	Ki	0.0060	0.0002	0.1025	1.7000	AID37981
Endothelin-1 receptor	Homo sapiens (human)	Ki	0.0019	0.0000	0.4300	10.0000	AID254289; AID671506; AID68479; AID68482
Type-1B angiotensin II receptor	Rattus norvegicus (Norway rat)	Ki	0.0060	0.0002	0.0521	1.1000	AID37706; AID37981
Type-1 angiotensin II receptor	Homo sapiens (human)	Ki	0.0100	0.0002	0.1837	4.7000	AID254304; AID39788; AID671505
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
mitotic cell cycle	Endothelin-1 receptor	Homo sapiens (human)
branching involved in blood vessel morphogenesis	Endothelin-1 receptor	Homo sapiens (human)
response to hypoxia	Endothelin-1 receptor	Homo sapiens (human)
in utero embryonic development	Endothelin-1 receptor	Homo sapiens (human)
blood vessel remodeling	Endothelin-1 receptor	Homo sapiens (human)
response to amphetamine	Endothelin-1 receptor	Homo sapiens (human)
regulation of heart rate	Endothelin-1 receptor	Homo sapiens (human)
glomerular filtration	Endothelin-1 receptor	Homo sapiens (human)
cardiac chamber formation	Endothelin-1 receptor	Homo sapiens (human)
left ventricular cardiac muscle tissue morphogenesis	Endothelin-1 receptor	Homo sapiens (human)
atrial cardiac muscle tissue development	Endothelin-1 receptor	Homo sapiens (human)
cardiac neural crest cell migration involved in outflow tract morphogenesis	Endothelin-1 receptor	Homo sapiens (human)
noradrenergic neuron differentiation	Endothelin-1 receptor	Homo sapiens (human)
intracellular calcium ion homeostasis	Endothelin-1 receptor	Homo sapiens (human)
smooth muscle contraction	Endothelin-1 receptor	Homo sapiens (human)
mitochondrion organization	Endothelin-1 receptor	Homo sapiens (human)
signal transduction	Endothelin-1 receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Endothelin-1 receptor	Homo sapiens (human)
activation of adenylate cyclase activity	Endothelin-1 receptor	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Endothelin-1 receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Endothelin-1 receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Endothelin-1 receptor	Homo sapiens (human)
respiratory gaseous exchange by respiratory system	Endothelin-1 receptor	Homo sapiens (human)
regulation of blood pressure	Endothelin-1 receptor	Homo sapiens (human)
cell population proliferation	Endothelin-1 receptor	Homo sapiens (human)
response to wounding	Endothelin-1 receptor	Homo sapiens (human)
gene expression	Endothelin-1 receptor	Homo sapiens (human)
protein kinase A signaling	Endothelin-1 receptor	Homo sapiens (human)
regulation of glucose transmembrane transport	Endothelin-1 receptor	Homo sapiens (human)
neural crest cell fate commitment	Endothelin-1 receptor	Homo sapiens (human)
artery smooth muscle contraction	Endothelin-1 receptor	Homo sapiens (human)
neuron remodeling	Endothelin-1 receptor	Homo sapiens (human)
heparin metabolic process	Endothelin-1 receptor	Homo sapiens (human)
thyroid gland development	Endothelin-1 receptor	Homo sapiens (human)
cellular response to oxidative stress	Endothelin-1 receptor	Homo sapiens (human)
embryonic heart tube development	Endothelin-1 receptor	Homo sapiens (human)
aorta development	Endothelin-1 receptor	Homo sapiens (human)
vasoconstriction	Endothelin-1 receptor	Homo sapiens (human)
norepinephrine metabolic process	Endothelin-1 receptor	Homo sapiens (human)
middle ear morphogenesis	Endothelin-1 receptor	Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transduction	Endothelin-1 receptor	Homo sapiens (human)
cellular response to human chorionic gonadotropin stimulus	Endothelin-1 receptor	Homo sapiens (human)
enteric nervous system development	Endothelin-1 receptor	Homo sapiens (human)
sympathetic nervous system development	Endothelin-1 receptor	Homo sapiens (human)
axon extension	Endothelin-1 receptor	Homo sapiens (human)
embryonic skeletal system development	Endothelin-1 receptor	Homo sapiens (human)
neuromuscular process	Endothelin-1 receptor	Homo sapiens (human)
sodium ion homeostasis	Endothelin-1 receptor	Homo sapiens (human)
canonical Wnt signaling pathway	Endothelin-1 receptor	Homo sapiens (human)
face development	Endothelin-1 receptor	Homo sapiens (human)
axonogenesis involved in innervation	Endothelin-1 receptor	Homo sapiens (human)
establishment of endothelial barrier	Endothelin-1 receptor	Homo sapiens (human)
pharyngeal arch artery morphogenesis	Endothelin-1 receptor	Homo sapiens (human)
renal sodium ion absorption	Endothelin-1 receptor	Homo sapiens (human)
calcium ion transmembrane transport	Endothelin-1 receptor	Homo sapiens (human)
cellular response to follicle-stimulating hormone stimulus	Endothelin-1 receptor	Homo sapiens (human)
cellular response to luteinizing hormone stimulus	Endothelin-1 receptor	Homo sapiens (human)
protein transmembrane transport	Endothelin-1 receptor	Homo sapiens (human)
glomerular endothelium development	Endothelin-1 receptor	Homo sapiens (human)
podocyte differentiation	Endothelin-1 receptor	Homo sapiens (human)
endothelin receptor signaling pathway involved in heart process	Endothelin-1 receptor	Homo sapiens (human)
renal albumin absorption	Endothelin-1 receptor	Homo sapiens (human)
vascular associated smooth muscle cell development	Endothelin-1 receptor	Homo sapiens (human)
mesenchymal cell apoptotic process	Endothelin-1 receptor	Homo sapiens (human)
sympathetic neuron axon guidance	Endothelin-1 receptor	Homo sapiens (human)
semaphorin-plexin signaling pathway involved in axon guidance	Endothelin-1 receptor	Homo sapiens (human)
podocyte apoptotic process	Endothelin-1 receptor	Homo sapiens (human)
meiotic cell cycle process involved in oocyte maturation	Endothelin-1 receptor	Homo sapiens (human)
cranial skeletal system development	Endothelin-1 receptor	Homo sapiens (human)
response to acetylcholine	Endothelin-1 receptor	Homo sapiens (human)
regulation of protein localization to cell leading edge	Endothelin-1 receptor	Homo sapiens (human)
positive regulation of cation channel activity	Endothelin-1 receptor	Homo sapiens (human)
endothelin receptor signaling pathway	Endothelin-1 receptor	Homo sapiens (human)
developmental pigmentation	Endothelin-1 receptor	Homo sapiens (human)
regulation of cell growth	Type-1 angiotensin II receptor	Homo sapiens (human)
kidney development	Type-1 angiotensin II receptor	Homo sapiens (human)
renin-angiotensin regulation of aldosterone production	Type-1 angiotensin II receptor	Homo sapiens (human)
maintenance of blood vessel diameter homeostasis by renin-angiotensin	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of systemic arterial blood pressure by renin-angiotensin	Type-1 angiotensin II receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Type-1 angiotensin II receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Type-1 angiotensin II receptor	Homo sapiens (human)
Rho protein signal transduction	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of macrophage derived foam cell differentiation	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of vasoconstriction	Type-1 angiotensin II receptor	Homo sapiens (human)
calcium-mediated signaling	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of phospholipase A2 activity	Type-1 angiotensin II receptor	Homo sapiens (human)
low-density lipoprotein particle remodeling	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of renal sodium excretion	Type-1 angiotensin II receptor	Homo sapiens (human)
angiotensin-activated signaling pathway	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of cell population proliferation	Type-1 angiotensin II receptor	Homo sapiens (human)
symbiont entry into host cell	Type-1 angiotensin II receptor	Homo sapiens (human)
regulation of inflammatory response	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of inflammatory response	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of protein metabolic process	Type-1 angiotensin II receptor	Homo sapiens (human)
cell chemotaxis	Type-1 angiotensin II receptor	Homo sapiens (human)
phospholipase C-activating angiotensin-activated signaling pathway	Type-1 angiotensin II receptor	Homo sapiens (human)
blood vessel diameter maintenance	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of blood vessel endothelial cell proliferation involved in sprouting angiogenesis	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of CoA-transferase activity	Type-1 angiotensin II receptor	Homo sapiens (human)
positive regulation of reactive oxygen species metabolic process	Type-1 angiotensin II receptor	Homo sapiens (human)
inflammatory response	Type-1 angiotensin II receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

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

Process	via Protein(s)	Taxonomy
plasma membrane	Endothelin-1 receptor	Homo sapiens (human)
plasma membrane	Endothelin-1 receptor	Homo sapiens (human)
plasma membrane	Type-1 angiotensin II receptor	Homo sapiens (human)
membrane	Type-1 angiotensin II receptor	Homo sapiens (human)
plasma membrane	Type-1 angiotensin II receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (29)

Assay ID	Title	Year	Journal	Article
AID30945	half life was determined in rat at a dose of 10 (umol/kg) following intravenous administration (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID178543	Compound was tested for its activity in Ang II pressor test following intravenous administration	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID68479	Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1	2003	Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6	Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.
AID171981	Maximum blood pressure decrease in rats	2003	Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6	Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.
AID29532	A dose of 10(umol/kg) was administered orally to rat and Tmax value was determined (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID249997	Permeability in Caco-2 cell monolayer	2005	Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1	Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.
AID68482	Compound was evaluated for its binding affinity towards human Endothelin A receptor	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID28062	A dose of 10 (umol/kg) was administered pre orally to rat and plasma concentration was reported (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID39788	Compound was evaluated for its binding affinity towards human Angiotensin II receptor, type 1	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID26954	A dose of 10(umol/kg) was administered orally to rat and % bioavailability was determined	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID250063	Endothelin pressor effect in rats after oral dose of 30 uM/kg	2005	Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1	Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.
AID178546	Compound was tested for its activity in bET-1 pressor test following intravenous administration	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID25978	Pharmacokinetic parameter Area under curve reported following peroral administration at a dose of 10 (umol/kg) (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID671506	Binding affinity at endothelin receptor subtype A	2012	Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15	Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.
AID254304	Inhibitory concentration against angiotensin II receptor, type 1	2005	Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21	Designed multiple ligands. An emerging drug discovery paradigm.
AID25977	Pharmacokinetic parameter Area under curve reported following intravenous administration at a dose of 10 (umol/kg) (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID671505	Binding affinity at type 1 angiotensin 2 receptor	2012	Bioorganic & medicinal chemistry, Aug-01, Volume: 20, Issue:15	Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.
AID178547	Compound was tested for its activity in bET-1 pressor test following oral administration	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID250249	Angiotensin II pressor effect in rats after oral dose of 30 uM/kg	2005	Journal of medicinal chemistry, Jan-13, Volume: 48, Issue:1	Dual angiotensin II and endothelin A receptor antagonists: synthesis of 2'-substituted N-3-isoxazolyl biphenylsulfonamides with improved potency and pharmacokinetics.
AID178545	Compound was tested for its activity in Ang II pressor test following oral administration	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID30946	half life was determined in rat at a dose of 10 (umol/kg) following peroral administration (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID27784	Pharmacokinetic parameter MRT value determined in rat at a dose of 10(umol/kg) following peroral administration (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID27881	Pharmacokinetic parameter Plasma clearance determined after intravenous administration at a dose of 10 (umol/kg) (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID169933	Compound at peroral dose 30 uM/kg was tested in vivo for the inhibition of angiotensin II (A II) pressor effect in rat	2003	Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6	Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.
AID254289	Inhibitory concentration against endothelin receptor type A	2005	Journal of medicinal chemistry, Oct-20, Volume: 48, Issue:21	Designed multiple ligands. An emerging drug discovery paradigm.
AID37706	Compound was evaluated for its binding affinity towards rat Angiotensin II receptor, type 1	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID30141	Pharmacokinetic parameter Volume of distribution was determined in rat following i.v. administration of a dose of 10 (umol/kg) (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
AID37981	Binding affinity towards Angiotensin II receptor, type 1 in rat aortic smooth muscle cells using 0.2 nM [125I]-labeled Sar-Ile-angiotensin II	2003	Bioorganic & medicinal chemistry letters, Mar-24, Volume: 13, Issue:6	Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.
AID27785	Pharmacokinetic parameter MRT value was determined in rat at a dose of 10(umol/kg) following intravenous administration (mean+/-SD)	2002	Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18	Discovery of N-isoxazolyl biphenylsulfonamides as potent dual angiotensin II and endothelin A receptor antagonists.
[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	4 (80.00)	29.6817
2010's	1 (20.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (20.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	4 (80.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
1-(1-naphthyl)piperazine 1-(1-naphthyl)piperazine: serotonin agonist; structure given in first source	3.12	1	N-arylpiperazine
celecoxib [no description available]	3.12	1	organofluorine compound; pyrazoles; sulfonamide; toluenes	cyclooxygenase 2 inhibitor; geroprotector; non-narcotic analgesic; non-steroidal anti-inflammatory drug
cetirizine Cetirizine: A potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Unlike many traditional antihistamines, it does not cause drowsiness or anticholinergic side effects.. cetirizine : A member of the class of piperazines that is piperazine in which the hydrogens attached to nitrogen are replaced by a (4-chlorophenyl)(phenyl)methyl and a 2-(carboxymethoxy)ethyl group respectively.	3.12	1	ether; monocarboxylic acid; monochlorobenzenes; piperazines	anti-allergic agent; environmental contaminant; H1-receptor antagonist; xenobiotic
cyproheptadine Cyproheptadine: A serotonin antagonist and a histamine H1 blocker used as antipruritic, appetite stimulant, antiallergic, and for the post-gastrectomy dumping syndrome, etc.. cyproheptadine : The product resulting from the formal oxidative coupling of position 5 of 5H-dibenzo[a,d]cycloheptene with position 4 of 1-methylpiperidine resulting in the formation of a double bond between the two fragments. It is a sedating antihistamine with antimuscarinic and calcium-channel blocking actions. It is used (particularly as the hydrochloride sesquihydrate) for the relief of allergic conditions including rhinitis, conjunctivitis due to inhalant allergens and foods, urticaria and angioedema, and in pruritic skin disorders. Unlike other antihistamines, it is also a seratonin receptor antagonist, making it useful in conditions such as vascular headache and anorexia.	3.12	1	piperidines; tertiary amine	anti-allergic agent; antipruritic drug; gastrointestinal drug; H1-receptor antagonist; serotonergic antagonist
fentanyl Fentanyl: A potent narcotic analgesic, abuse of which leads to habituation or addiction. It is primarily a mu-opioid agonist. Fentanyl is also used as an adjunct to general anesthetics, and as an anesthetic for induction and maintenance. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1078). fentanyl : A monocarboxylic acid amide resulting from the formal condensation of the aryl amino group of N-phenyl-1-(2-phenylethyl)piperidin-4-amine with propanoic acid.	3.12	1	anilide; monocarboxylic acid amide; piperidines	adjuvant; anaesthesia adjuvant; anaesthetic; intravenous anaesthetic; mu-opioid receptor agonist; opioid analgesic
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.	3.12	1	(trifluoromethyl)benzenes; aromatic ether; secondary amino compound
avapro Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease.. irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.	4.03	4	azaspiro compound; biphenylyltetrazole	angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic
loratadine Loratadine: A second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.. loratadine : A benzocycloheptapyridine that is 6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine substituted by a chloro group at position 8 and a 1-(ethoxycarbonyl)piperidin-4-ylidene group at position 11. It is a H1-receptor antagonist commonly employed in the treatment of allergic disorders.	3.12	1	benzocycloheptapyridine; ethyl ester; N-acylpiperidine; organochlorine compound; tertiary carboxamide	anti-allergic agent; cholinergic antagonist; geroprotector; H1-receptor antagonist
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	2.07	1	biphenylyltetrazole; imidazoles	angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist
pindolol Pindolol: A moderately lipophilic beta blocker (ADRENERGIC BETA-ANTAGONISTS). It is non-cardioselective and has intrinsic sympathomimetic actions, but little membrane-stabilizing activity. (From Martindale, The Extra Pharmocopoeia, 30th ed, p638). pindolol : A member of the class of indols which is the 2-hydroxy-3-(isopropylamino)propyl ether derivative of 1H-indol-4-ol.	3.12	1	indoles; secondary amine	antiglaucoma drug; antihypertensive agent; beta-adrenergic antagonist; serotonergic antagonist; vasodilator agent
roxatidine acetate roxatidine acetate: structure given in first source	3.12	1	piperidines
imatinib [no description available]	3.12	1	aromatic amine; benzamides; N-methylpiperazine; pyridines; pyrimidines	antineoplastic agent; apoptosis inducer; tyrosine kinase inhibitor
captopril Captopril: A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.. captopril : A L-proline derivative in which L-proline is substituted on nitrogen with a (2S)-2-methyl-3-sulfanylpropanoyl group. It is used as an anti-hypertensive ACE inhibitor drug.	3.12	1	alkanethiol; L-proline derivative; N-acylpyrrolidine; pyrrolidinemonocarboxylic acid	antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor
sulotroban sulotroban: thromboxane receptor antagonist	3.12	1
sch 37370 N-acetyldesloratadine: dual antagonist of platelet-activating factor and histamine	3.12	1
duloxetine [no description available]	3.12	1	duloxetine
ziprasidone ziprasidone: a benzisothiazoylpiperazine derivative; has combined dopamine and serotonin receptor antagonist activity; structurally related to tiospirone. ziprasidone : A piperazine compound having 1,2-benzothiazol-3-yl- and 2-(6-chloro-1,3-dihydro-2-oxindol-5-yl)ethyl substituents attached to the nitrogen atoms.	3.12	1	1,2-benzisothiazole; indolones; organochlorine compound; piperazines	antipsychotic agent; dopaminergic antagonist; histamine antagonist; muscarinic antagonist; psychotropic drug; serotonergic antagonist
prifelone prifelone: structure given in first source	3.12	1	aromatic ketone
bosentan anhydrous Bosentan: A sulfonamide and pyrimidine derivative that acts as a dual endothelin receptor antagonist used to manage PULMONARY HYPERTENSION and SYSTEMIC SCLEROSIS.	2.07	1	primary alcohol; pyrimidines; sulfonamide	antihypertensive agent; endothelin receptor antagonist
sq 28603 SQ 28603: a selective neutral endopeptidase inhibitor	3.12	1
rupatadine rupatadine: structure given in first source; RN given refers to trihydrochloride	3.12	1	benzocycloheptapyridine
ml-3000 [no description available]	3.12	1
mk 767 5-((2,4-dioxo-5-thiazolidinyl)methyl)-2-methoxy-N-((4-(trifluoromethyl)phenyl)methyl)benzamide: an antihyperlipidemic agent that also functions as an insulin sensitizer, PPARalpha agonist, and PPARgamma agonist; structure in first source	3.12	1
bms 207940 N-((2'-(((4,5-dimethyl-3-isoxazolyl)amino)sulfonyl)-4-(2-oxazolyl)(1,1'-biphenyl)-2-yl)methyl)-N,3,3-trimethylbutanamide: an ET(A) receptor antagonist; structure in first source	3.12	1
e 3040 E 3040: a dual inhibitor of 5-lipoxygenase and thromboxane A2 synthetase; structure given in first source	3.12	1	benzothiazoles; organic hydroxy compound; pyridines; secondary amino compound	anti-inflammatory drug; EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor; uricosuric drug
tropisetron Tropisetron: An indole derivative and 5-HT3 RECEPTOR antagonist that is used for the prevention of nausea and vomiting.. tropisetron : An indolyl carboxylate ester obtained by formal condensation of the carboxy group of indole-3-carboxylic acid with the hydroxy group of tropine.	3.12	1	indolyl carboxylic acid
l 365260 L 365260: a CCK-B antagonist; structure given in first source; potent & selective CCK-B & gastrin receptor ligand; L 365260 and L 365346 are (R)- and (S)-stereoisomers, respectively	3.12	1	benzodiazepine
bosutinib 4-((2,4-dichloro-5-methoxyphenyl)amino)-6-methoxy-7-(3-(4-methyl-1-piperazinyl)propoxy)-3-quinolinecarbonitrile: a Src kinase inhibitor; structure in first source	3.12	1	aminoquinoline; aromatic ether; dichlorobenzene; N-methylpiperazine; nitrile; tertiary amino compound	antineoplastic agent; tyrosine kinase inhibitor
6-(4-(2-(((4-chlorophenyl)sulfonyl)amino)ethyl)phenyl)-6-(3-pyridyl)hex-5-enoic acid 6-(4-(2-(((4-chlorophenyl)sulfonyl)amino)ethyl)phenyl)-6-(3-pyridyl)hex-5-enoic acid: combined thromboxane A2 receptor & thromboxane synthesis inhibitor; structure given in first source; RN given refers to (E)-isomer	3.12	1
bms 193884 [no description available]	2.42	2
sb-649915 SB-649915: potent 5-HT1A and 5-HT1B autoreceptor antagonist and 5-HT re-uptake inhibitor	3.12	1
milnacipran [no description available]	3.12	1	acetamides
clozapine Clozapine: A tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. Agranulocytosis is a major adverse effect associated with administration of this agent.. clozapine : A benzodiazepine that is 5H-dibenzo[b,e][1,4]diazepine substituted by a chloro group at position 8 and a 4-methylpiperazin-1-yl group at position 11. It is a second generation antipsychotic used in the treatment of psychiatric disorders like schizophrenia.	3.12	1	benzodiazepine; N-arylpiperazine; N-methylpiperazine; organochlorine compound	adrenergic antagonist; dopaminergic antagonist; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor; environmental contaminant; GABA antagonist; histamine antagonist; muscarinic antagonist; second generation antipsychotic; serotonergic antagonist; xenobiotic

Condition	Relationship Strength	Studies
Blood Pressure, High [description not available]	2.02	1
Hypertension Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.	2.02	1
Diseases, Metabolic [description not available]	2.94	1
Metabolic Diseases Generic term for diseases caused by an abnormal metabolic process. It can be congenital due to inherited enzyme abnormality (METABOLISM, INBORN ERRORS) or acquired due to disease of an endocrine organ or failure of a metabolically important organ such as the liver. (Stedman, 26th ed)	2.94	1

bms 248360

Cross-References

Synonyms (17)

Protein Targets (4)

Inhibition Measurements

Biological Processes (99)

Molecular Functions (7)

Ceullar Components (2)

Bioassays (29)

Research

Studies (5)

Market Indicators

Research Demand Index: 12.50

Study Types

bms 248360

Cross-References

Synonyms (17)

Protein Targets (4)

Inhibition Measurements

Biological Processes (99)

Molecular Functions (7)

Ceullar Components (2)

Bioassays (29)

Research

Studies (5)

Market Indicators

Research Demand Index: 12.50

Study Types

Related Drugs (33)

Related Conditions (4)