cyclazosin profile

cyclazosin: an alpha(1D)-adrenoceptor antagonist; structure given in first source; RN given for (cis)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cyclazosin : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of furoic acid with the secondary amino group of 6,7-dimethoxy-2-[(4aR,8aS)-octahydroquinoxalin-1-yl]quinazolin-4-amine. [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]

ID Source	ID
PubMed CID	132266
CHEMBL ID	423294
CHEBI ID	63937
MeSH ID	M0214993

Synonym
quinoxaline, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-furanylcarbonyl)decahydro-, cis-
cis-1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-furanylcarbonyl)decahydroquinoxaline
[(4ar,8as)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2,3,4a,5,6,7,8,8a-octahydroquinoxalin-1-yl]-furan-2-ylmethanone
(+)-cyclazosin
gtpl486
cyclazosin
CHEMBL423294
chebi:63937 ,
139953-73-4
(4-(4-amino-6,7-dimethoxyquinazolin-2-yl)octahydroquinoxalin-1-yl)furan-2-ylmethanone hydrochloride
[(4ar,8as)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2,3,4a,5,6,7,8,8a-octahydroquinoxalin-1-yl]-(furan-2-yl)methanone
bdbm50403649
[(4ar,8as)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)octahydroquinoxalin-1(2h)-yl](2-furyl)methanone
J981.319E ,
Q27076939
[(4~{a}~{r},8~{a}~{s})-4-(4-azanyl-6,7-dimethoxy-quinazolin-2-yl)-2,3,4~{a},5,6,7,8,8~{a}-octahydroquinoxalin-1-yl]-(furan-2-yl)methanone
T0B ,
DTXSID701112809
quinoxaline, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(2-furanylcarbonyl)decahydro-, (4ar,8as)-rel-
cyclazosin, (+)-
(((4ar)-4-(4-amino-6,7-dimethoxyquinazoline-2-yl)-3,4,4a.beta.,5,6,7,8,8a.beta.-octahydroquinoxaline)-1(2h)-yl)(2-furanyl) ketone
[(4ar,8as)-4-(4-amino-6,7-dimethoxy-2-quinazolinyl)octahydro-1(2h)-quinoxalinyl]-2-furanylmethanone
methanone, [(4ar,8as)-4-(4-amino-6,7-dimethoxy-2-quinazolinyl)octahydro-1(2h)-quinoxalinyl]-2-furanyl-
((4ar,8as)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)octahydroquinoxalin-1(2h)-yl)(2-furyl)methanone
210542-51-1
2FH26454WF
(+)-2-((4as,8ar)-4-(2-furoyl)octahydroquinoxalin-1(2h)-yl)-6,7-dimethoxyquinazolin-4-amine

Excerpt	Reference	Relevance
"(+)-Cyclazosin is a quinazoline derivative pharmacologically characterized as alpha(1b)-adrenoceptor selective ligand in binding assays and alpha(1B)-selective antagonist in isolated tissues. "	( Absolute configuration of the alpha (1B)-adrenoceptor antagonist (+)-cyclazosin. Antolini, L; Giardinà, D; Grelli, M; Gulini, U; Melchiorre, C; Sagratini, G, 2004)	1.12

Role	Description
adenosine A2A receptor antagonist	An antagonist at the A2A receptor.
[role 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]

Class	Description
quinazolines	Any organic heterobicyclic compound based on a quinazoline skeleton and its substituted derivatives.
furans	Compounds containing at least one furan ring.
aromatic ether	Any ether in which the oxygen is attached to at least one aryl substituent.
quinoxaline derivative	Any naphthyridine derivative that is a derivative of quinoxaline (1,4-naphthyridine).
aromatic amide	An amide in which the amide linkage is bonded directly to an aromatic system.
monocarboxylic acid amide	A carboxamide derived from a monocarboxylic acid.
[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	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Alpha-1A adrenergic receptor	Oryctolagus cuniculus (rabbit)	Ki	0.0251	0.0000	0.0204	0.2512	AID36753
Beta-casein	Rattus norvegicus (Norway rat)	Ki	0.0001	0.0001	0.0006	0.0015	AID35168
Muscarinic acetylcholine receptor M4	Homo sapiens (human)	Ki	0.0123	0.0000	0.7951	9.1201	AID294001
5-hydroxytryptamine receptor 1A	Homo sapiens (human)	Ki	1.0000	0.0001	0.5326	10.0000	AID3920
Alpha-1B adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.0003	0.0001	0.9490	10.0000	AID422825
Alpha-1A adrenergic receptor	Bos taurus (cattle)	Ki	0.0024	0.0000	0.5072	3.7020	AID36464
5-hydroxytryptamine receptor 1A	Rattus norvegicus (Norway rat)	Ki	0.0002	0.0001	0.7396	10.0000	AID37186
Alpha-2B adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.0316	0.0000	0.9296	10.0000	AID35467
Alpha-2C adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.0316	0.0000	0.9708	10.0000	AID35467
Alpha-2A adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.0316	0.0000	0.9375	10.0000	AID35467
Alpha-1D adrenergic receptor	Rattus norvegicus (Norway rat)	Ki	0.0006	0.0000	0.5751	10.0000	AID35741
Alpha-1D adrenergic receptor	Homo sapiens (human)	Ki	0.0096	0.0000	0.3609	10.0000	AID1497049; AID294003; AID35467; AID422826
Alpha-1A adrenergic receptor	Homo sapiens (human)	Ki	0.0138	0.0000	0.2726	10.0000	AID1497047; AID294001; AID36753; AID422824
Alpha-1B adrenergic receptor	Homo sapiens (human)	Ki	0.0003	0.0000	0.4713	10.0000	AID1497048; AID1497059; AID294002; AID37186; AID37187; AID422825
D(2) dopamine receptor	Rattus norvegicus (Norway rat)	Ki	10.0000	0.0000	0.4375	10.0000	AID63806
[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)
Alpha-1D adrenergic receptor	Rattus norvegicus (Norway rat)	Kd	0.0537	0.0002	0.8962	7.5858	AID1497043
Alpha-1A adrenergic receptor	Rattus norvegicus (Norway rat)	Kd	0.0091	0.0002	0.5139	7.5858	AID1497041; AID422827
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
signal transduction	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
cell surface receptor signaling pathway	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathway	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
regulation of locomotion	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathway	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
chemical synaptic transmission	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
behavioral fear response	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
G protein-coupled receptor signaling pathway	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
serotonin receptor signaling pathway	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
gamma-aminobutyric acid signaling pathway	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
positive regulation of cell population proliferation	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of serotonin secretion	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of vasoconstriction	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
exploration behavior	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of dopamine metabolic process	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
serotonin metabolic process	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of hormone secretion	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of behavior	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
chemical synaptic transmission	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
regulation of vasoconstriction	Alpha-1A adrenergic receptor	Bos taurus (cattle)
positive regulation of MAPK cascade	Alpha-1A adrenergic receptor	Bos taurus (cattle)
regulation of cardiac muscle contraction	Alpha-1A adrenergic receptor	Bos taurus (cattle)
G protein-coupled receptor signaling pathway	Alpha-1D adrenergic receptor	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Alpha-1D adrenergic receptor	Homo sapiens (human)
positive regulation of cell population proliferation	Alpha-1D adrenergic receptor	Homo sapiens (human)
neuron-glial cell signaling	Alpha-1D adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-1D adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-1D adrenergic receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Alpha-1D adrenergic receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Alpha-1D adrenergic receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Alpha-1D adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-1D adrenergic receptor	Homo sapiens (human)
MAPK cascade	Alpha-1A adrenergic receptor	Homo sapiens (human)
negative regulation of heart rate involved in baroreceptor response to increased systemic arterial blood pressure	Alpha-1A adrenergic receptor	Homo sapiens (human)
norepinephrine-epinephrine vasoconstriction involved in regulation of systemic arterial blood pressure	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of heart rate by epinephrine-norepinephrine	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of the force of heart contraction by epinephrine-norepinephrine	Alpha-1A adrenergic receptor	Homo sapiens (human)
apoptotic process	Alpha-1A adrenergic receptor	Homo sapiens (human)
smooth muscle contraction	Alpha-1A adrenergic receptor	Homo sapiens (human)
signal transduction	Alpha-1A adrenergic receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Alpha-1A adrenergic receptor	Homo sapiens (human)
activation of phospholipase C activity	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Alpha-1A adrenergic receptor	Homo sapiens (human)
adult heart development	Alpha-1A adrenergic receptor	Homo sapiens (human)
negative regulation of cell population proliferation	Alpha-1A adrenergic receptor	Homo sapiens (human)
response to xenobiotic stimulus	Alpha-1A adrenergic receptor	Homo sapiens (human)
response to hormone	Alpha-1A adrenergic receptor	Homo sapiens (human)
negative regulation of autophagy	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of cardiac muscle hypertrophy	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of synaptic transmission, GABAergic	Alpha-1A adrenergic receptor	Homo sapiens (human)
intracellular signal transduction	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of action potential	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of vasoconstriction	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of smooth muscle contraction	Alpha-1A adrenergic receptor	Homo sapiens (human)
calcium ion transport into cytosol	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of cardiac muscle contraction	Alpha-1A adrenergic receptor	Homo sapiens (human)
cell growth involved in cardiac muscle cell development	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Alpha-1A adrenergic receptor	Homo sapiens (human)
positive regulation of protein kinase C signaling	Alpha-1A adrenergic receptor	Homo sapiens (human)
pilomotor reflex	Alpha-1A adrenergic receptor	Homo sapiens (human)
neuron-glial cell signaling	Alpha-1A adrenergic receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Alpha-1A adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-1A adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-1A adrenergic receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
regulation of vasoconstriction	Alpha-1B adrenergic receptor	Homo sapiens (human)
intracellular signal transduction	Alpha-1B adrenergic receptor	Homo sapiens (human)
positive regulation of MAPK cascade	Alpha-1B adrenergic receptor	Homo sapiens (human)
regulation of cardiac muscle contraction	Alpha-1B adrenergic receptor	Homo sapiens (human)
neuron-glial cell signaling	Alpha-1B adrenergic receptor	Homo sapiens (human)
adenylate cyclase-activating adrenergic receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
cell-cell signaling	Alpha-1B adrenergic receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Alpha-1B adrenergic receptor	Homo sapiens (human)
positive regulation of cytosolic calcium ion concentration	Alpha-1B adrenergic receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
G protein-coupled serotonin receptor activity	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
G protein-coupled acetylcholine receptor activity	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
G protein-coupled serotonin receptor activity	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
protein binding	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
receptor-receptor interaction	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
neurotransmitter receptor activity	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
serotonin binding	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
protein heterodimerization activity	Alpha-1A adrenergic receptor	Bos taurus (cattle)
protein binding	Alpha-1D adrenergic receptor	Homo sapiens (human)
identical protein binding	Alpha-1D adrenergic receptor	Homo sapiens (human)
alpha1-adrenergic receptor activity	Alpha-1D adrenergic receptor	Homo sapiens (human)
alpha1-adrenergic receptor activity	Alpha-1A adrenergic receptor	Homo sapiens (human)
protein binding	Alpha-1A adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Alpha-1A adrenergic receptor	Homo sapiens (human)
protein binding	Alpha-1B adrenergic receptor	Homo sapiens (human)
protein heterodimerization activity	Alpha-1B adrenergic receptor	Homo sapiens (human)
alpha1-adrenergic receptor activity	Alpha-1B adrenergic receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
plasma membrane	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
postsynaptic membrane	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
dendrite	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
plasma membrane	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
synapse	Muscarinic acetylcholine receptor M4	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
synapse	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
plasma membrane	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
dendrite	5-hydroxytryptamine receptor 1A	Homo sapiens (human)
nucleus	Alpha-1A adrenergic receptor	Bos taurus (cattle)
cytoplasm	Alpha-1A adrenergic receptor	Bos taurus (cattle)
plasma membrane	Alpha-1A adrenergic receptor	Bos taurus (cattle)
caveola	Alpha-1A adrenergic receptor	Bos taurus (cattle)
nuclear membrane	Alpha-1A adrenergic receptor	Bos taurus (cattle)
plasma membrane	Alpha-1D adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1D adrenergic receptor	Homo sapiens (human)
nucleus	Alpha-1A adrenergic receptor	Homo sapiens (human)
nucleoplasm	Alpha-1A adrenergic receptor	Homo sapiens (human)
cytoplasm	Alpha-1A adrenergic receptor	Homo sapiens (human)
cytosol	Alpha-1A adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1A adrenergic receptor	Homo sapiens (human)
caveola	Alpha-1A adrenergic receptor	Homo sapiens (human)
nuclear membrane	Alpha-1A adrenergic receptor	Homo sapiens (human)
intracellular membrane-bounded organelle	Alpha-1A adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1A adrenergic receptor	Homo sapiens (human)
nucleus	Alpha-1B adrenergic receptor	Homo sapiens (human)
cytoplasm	Alpha-1B adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1B adrenergic receptor	Homo sapiens (human)
caveola	Alpha-1B adrenergic receptor	Homo sapiens (human)
nuclear membrane	Alpha-1B adrenergic receptor	Homo sapiens (human)
plasma membrane	Alpha-1B adrenergic receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (58)

Assay ID	Title	Year	Journal	Article
AID294000	Selectivity ratio for rat adrenergic alpha-1A receptor over rat adrenergic Alpha-1D receptor	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID294002	Displacement of [3H]prazosin from human adrenergic alpha-1b receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID36464	Compound was tested for binding affinity against cloned Alpha-1A adrenergic receptor from bovine brain using radioligand ([3H]prazosin) binding assay	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID294006	Selectivity ratio of pKi for human adrenergic alpha-1a receptor to pKi for human adrenergic alpha1d receptor	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID63792	Antagonistic affinity against rat striatum Dopamine receptor D2	1998	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11	Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.
AID35467	Binding affinity was tested on cloned rat Alpha-1D adrenergic receptor	1997	Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9	Pharmacological options in the treatment of benign prostatic hyperplasia.
AID36006	Binding affinity against native Alpha-1 adrenergic receptor from rat cerebral cortex using radioligand [3H]-prazosin binding assay	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID293998	Selectivity ratio for rat adrenergic alpha-1A receptor over rat adrenergic Alpha-1B receptor	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID422825	Displacement of [3H]prazosin from human Alpha-1B adrenoceptor expressed in CHO cells	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
AID35502	Antagonistic affinity against native rat cortex Alpha-2 adrenergic receptor	1998	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11	Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.
AID1497042	Antagonist activity at alpha1B adrenergic receptor in Wistar rat spleen assessed as inhibition of phenylephrine-induced contraction incubated for 30 mins in presence of beta-adrenoceptor blocker propranolol hydrochloride
AID422827	Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
AID3920	Antagonistic affinity against cloned human 5-hydroxytryptamine 1A receptor	1998	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11	Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.
AID37186	Binding affinity was tested on cloned hamster Alpha-1B adrenergic receptor	1997	Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9	Pharmacological options in the treatment of benign prostatic hyperplasia.
AID293999	Selectivity ratio for rat adrenergic Alpha-1D receptor over rat adrenergic Alpha-1B receptor	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID422829	Antagonist activity at rat Alpha-1D adrenoceptor assessed as inhibition if norepenephrine-induced contraction of thoracic aorta	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
AID1497059	Binding affinity to human alpha1B adrenergic receptor
AID1497044	Selectivity ratio of compound effect for antagonism of alpha1B adrenergic receptor in Wistar rat spleen to compound effect for antagonism of alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens
AID1497051	Selectivity ratio of compound effect for displacement of [3H]prazosin from human alpha1B adrenergic receptor expressed in CHO cell membranes to compound effect for displacement of [3H]prazosin from human alpha1D adrenergic receptor expressed in CHO cell m
AID294003	Displacement of [3H]prazosin from human adrenergic alpha-1d receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID294004	Selectivity ratio of pKi for human adrenergic alpha-1a receptor to pKi for human adrenergic alpha-1b receptor	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID35168	Compound was tested for binding affinity against native Alpha-1B adrenergic receptor from rat liver using radioligand ([3H]prazosin) binding assay	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID1497041	Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocai
AID63806	Compound was tested for binding affinity against native Dopamine receptor D2 from rat striatum using radioligand [3H]-spiperone)	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID35151	Antagonistic affinity against Alpha-1B adrenergic receptor was determined in isolated spleen tissue from rat	1998	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11	Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.
AID1497048	Displacement of [3H]prazosin from human alpha1B adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
AID294001	Displacement of [3H]prazosin from human adrenergic alpha-1a receptor expressed in CHO cells	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID36753	Binding affinity was tested on human Alpha-1A adrenergic receptor	1997	Journal of medicinal chemistry, Apr-25, Volume: 40, Issue:9	Pharmacological options in the treatment of benign prostatic hyperplasia.
AID294005	Selectivity ratio of pKi for human adrenergic alpha-1d receptor to pKi for human adrenergic alpha-1b receptor	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID1497060	Selectivity ratio of compound effect for human alpha1B adrenergic receptor to compound effect for human alpha1A adrenergic receptor
AID239801	Binding affinity for alpha 1d adrenoceptor	2005	Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15	Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID37187	Compound was tested for binding affinity against cloned Alpha-1B adrenergic receptor from hamster smooth muscle using radioligand ([3H]prazosin) binding assay	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID293995	Antagonist activity against adrenergic alpha-1A receptor in rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contraction	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID422824	Displacement of [3H]prazosin from human alpha1A adrenoceptor expressed in CHO cells	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
AID1497052	Selectivity ratio of compound effect for displacement of [3H]prazosin from human alpha1D adrenergic receptor expressed in CHO cell membranes to compound effect for displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell m
AID422826	Displacement of [3H]prazosin from human Alpha-1D adrenoceptor expressed in CHO cells	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
AID1497047	Displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
AID35507	Binding affinity against native Alpha-2 adrenergic receptor from rat cerebral cortex using radioligand ([3H]rauwolscine) binding assay	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID4407	Binding affinity against native 5-HT1A-receptors from rat hippocampus using radioligand ([3H]8-hydroxy-2-(di-n-propylamino)-tetraline) binding assay	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID293997	Antagonist activity against adrenergic Alpha-1D receptor in rat thoracic aorta assessed as noradrenaline-induced response	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID1497046	Selectivity ratio of compound effect for antagonism of alpha1D adrenergic receptor in Wistar rat thoracic aorta to compound effect for antagonism of alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens
AID293996	Antagonist activity against adrenergic Alpha-1B receptor in rat spleen assessed as inhibition of phenylephrine-induced response	2007	Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6	Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
AID1497043	Antagonist activity at alpha1D adrenergic receptor in Wistar rat thoracic aorta assessed as inhibition of noradrenaline-induced contraction measured after 30 mins in presence of cocaine hydrochloride and beta-adrenoceptor blocker propranolol hydrochloride
AID1497045	Selectivity ratio of compound effect for antagonism of alpha1B adrenergic receptor in Wistar rat spleen to compound effect for antagonism of alpha1D adrenergic receptor in Wistar rat thoracic aorta
AID1497049	Displacement of [3H]prazosin from human alpha1D adrenergic receptor expressed in CHO cell membranes after 30 mins by rapid filtration method
AID422828	Antagonist activity at rat Alpha-1B adrenoceptor assessed as inhibition if phenylephrine-induced contraction of spleen	2009	Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15	Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
AID239799	Binding affinity for alpha 1a adrenoceptor	2005	Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15	Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID36909	Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat	1998	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11	Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.
AID35741	Compound was tested for binding affinity against cloned Alpha-1D adrenergic receptor from rat brain.	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID239800	Binding affinity for alpha 1b adrenoceptor	2005	Journal of medicinal chemistry, Jul-28, Volume: 48, Issue:15	Range and sensitivity as descriptors of molecular property spaces in dynamic QSAR analyses.
AID35608	Antagonistic affinity against Alpha-1D adrenergic receptor was determined in isolated thoracic aorta from rat	1998	Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11	Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.
AID1497050	Selectivity ratio of compound effect for displacement of [3H]prazosin from human alpha1B adrenergic receptor expressed in CHO cell membranes to compound effect for displacement of [3H]prazosin from human alpha1A adrenergic receptor expressed in CHO cell m
AID37043	Binding affinity against native Alpha-1A adrenergic receptor from rat hippocampus pretreated with chloroethylclonidine using radioligand ([3H]prazosin) binding assay	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID1497061	Selectivity ratio of compound effect for human alpha1B adrenergic receptor to compound effect for human alpha1D adrenergic receptor
AID1345908	Human alpha1A-adrenoceptor (Adrenoceptors)	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID1345971	Human alpha1D-adrenoceptor (Adrenoceptors)	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID1345920	Rat alpha1D-adrenoceptor (Adrenoceptors)	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
AID1346000	Human alpha1B-adrenoceptor (Adrenoceptors)	1996	Journal of medicinal chemistry, Nov-08, Volume: 39, Issue:23	Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
[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	6 (27.27)	18.2507
2000's	11 (50.00)	29.6817
2010's	3 (13.64)	24.3611
2020's	2 (9.09)	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 (4.55%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	21 (95.45%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
chlorine chloride : A halide anion formed when chlorine picks up an electron to form an an anion.	2.02	1	halide anion; monoatomic chlorine	cofactor; Escherichia coli metabolite; human metabolite
thymine [no description available]	2.75	3	pyrimidine nucleobase; pyrimidone	Escherichia coli metabolite; human metabolite; mouse metabolite
n-methyl-3,4-methylenedioxyamphetamine N-Methyl-3,4-methylenedioxyamphetamine: An N-substituted amphetamine analog. It is a widely abused drug classified as a hallucinogen and causes marked, long-lasting changes in brain serotonergic systems. It is commonly referred to as MDMA or ecstasy.. 3,4-methylenedioxymethamphetamine : A member of the class of benzodioxoles that is 1,3-benzodioxole substituted by a 2-(methylamino)propyl group at position 5.	2.04	1	amphetamines; benzodioxoles	neurotoxin
alfuzosin alfuzosin: structure given in first source	3.51	2	monocarboxylic acid amide; quinazolines; tetrahydrofuranol	alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent
benoxathian benoxathian: RN given refers to parent cpd; structure given in first source	2.02	1
bmy 7378 [no description available]	2.02	1	piperazines
bunazosin bunazosin: structure	2.02	1	quinazolines
clonidine Clonidine: An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.. clonidine (amino form) : A clonidine that is 4,5-dihydro-1H-imidazol-2-amine in which one of the amino hydrogens is replaced by a 2,6-dichlorophenyl group.	2.42	2	clonidine; imidazoline
[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2,3,4a,5,6,7,8,8a-octahydroquinoxalin-1-yl]-(2-furanyl)methanone [no description available]	1.99	1	N-arylpiperazine
doxazosin Doxazosin: A prazosin-related compound that is a selective alpha-1-adrenergic blocker.. doxazosin : A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl group at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure.	3.81	3	aromatic amine; benzodioxine; monocarboxylic acid amide; N-acylpiperazine; N-arylpiperazine; quinazolines	alpha-adrenergic antagonist; antihyperplasia drug; antihypertensive agent; antineoplastic agent; vasodilator agent
furosemide Furosemide: A benzoic-sulfonamide-furan. It is a diuretic with fast onset and short duration that is used for EDEMA and chronic RENAL INSUFFICIENCY.. furosemide : A chlorobenzoic acid that is 4-chlorobenzoic acid substituted by a (furan-2-ylmethyl)amino and a sulfamoyl group at position 2 and 5 respectively. It is a diuretic used in the treatment of congestive heart failure.	2.01	1	chlorobenzoic acid; furans; sulfonamide	environmental contaminant; loop diuretic; xenobiotic
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	biphenylyltetrazole; imidazoles	angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist
naftopidil [no description available]	2.04	1	piperazines
nan 190 1-(2-methoxyphenyl)-4-(4-(2-phthalimido)butyl)piperazine: RN from Toxlit. NAN 190 : An N-alkylpiperazine that consists of (2-methoxyphenyl)piperazine in which the amine hydrogen is substituted by a 4-(2-phthalimido)butyl group.	2.02	1	N-alkylpiperazine; N-arylpiperazine; phthalimides	serotonergic antagonist
prazosin Prazosin: A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.. prazosin : A member of the class of piperazines that is piperazine substituted by a furan-2-ylcarbonyl group and a 4-amino-6,7-dimethoxyquinazolin-2-yl group at positions 1 and 4 respectively.	4.99	12	aromatic ether; furans; monocarboxylic acid amide; piperazines; quinazolines	alpha-adrenergic antagonist; antihypertensive agent; EC 3.4.21.26 (prolyl oligopeptidase) inhibitor
spiperone Spiperone: A spiro butyrophenone analog similar to HALOPERIDOL and other related compounds. It has been recommended in the treatment of SCHIZOPHRENIA.. spiperone : An azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.	2.41	2	aromatic ketone; azaspiro compound; organofluorine compound; piperidines; tertiary amino compound	alpha-adrenergic antagonist; antipsychotic agent; dopaminergic antagonist; psychotropic drug; serotonergic antagonist
terazosin Terazosin: induces decreased blood pressure; used in the treatment of benign prostatic hyperplasia	3.51	2	furans; piperazines; primary amino compound; quinazolines	alpha-adrenergic antagonist; antihypertensive agent; antineoplastic agent
5-methylurapidil [no description available]	4.04	4
urethane [no description available]	2	1	carbamate ester	fungal metabolite; mutagen
n-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-n-(2-pyridinyl)cyclohexanecarboxamide [no description available]	2.02	1	piperazines
wb 4101 N-(2,3-dihydro-1,4-benzodioxin-2-ylmethyl)-2-(2,6-dimethoxyphenoxy)ethanamine : A benzodioxine that is 2,3-dihydro-1,4-benzodioxine bearing a [(2',6'-dimethoxyphenoxy)ethylamino]methyl group at position 2. An alpha1A-adrenergic selective antagonist.	3.8	3	aromatic ether; benzodioxine; secondary amino compound	alpha-adrenergic antagonist
phentolamine Phentolamine: A nonselective alpha-adrenergic antagonist. It is used in the treatment of hypertension and hypertensive emergencies, pheochromocytoma, vasospasm of RAYNAUD DISEASE and frostbite, clonidine withdrawal syndrome, impotence, and peripheral vascular disease.. phentolamine : A substituted aniline that is 3-aminophenol in which the hydrogens of the amino group are replaced by 4-methylphenyl and 4,5-dihydro-1H-imidazol-2-ylmethyl groups respectively. An alpha-adrenergic antagonist, it is used for the treatment of hypertension.	2.02	1	imidazoles; phenols; substituted aniline; tertiary amino compound	alpha-adrenergic antagonist; vasodilator agent
phenylephrine Phenylephrine: An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.. phenylephrine : A member of the class of the class of phenylethanolamines that is (1R)-2-(methylamino)-1-phenylethan-1-ol carrying an additional hydroxy substituent at position 3 on the phenyl ring.	2.73	3	phenols; phenylethanolamines; secondary amino compound	alpha-adrenergic agonist; cardiotonic drug; mydriatic agent; nasal decongestant; protective agent; sympathomimetic agent; vasoconstrictor agent
methoxamine Methoxamine: An alpha-1 adrenergic agonist that causes prolonged peripheral VASOCONSTRICTION.. methoxamine : An amphetamine in which the parent 1-phenylpropan-2-amine skeleton is substituted at position 1 with an hydroxy group and the phenyl ring is 2- and 5-substituted with methoxy groups. It is an antihypotensive agent (pressor), an agonist acting directly at alpha-adrenoceptors with selectivity for the alpha-1 adrenoceptor subtype similar to phenylephrine .	2.46	2	amphetamines	alpha-adrenergic agonist; antihypotensive agent
quinoxalines quinoxaline : A naphthyridine in which the nitrogens are at positions 1 and 4.	4.28	18	mancude organic heterobicyclic parent; naphthyridine; ortho-fused heteroarene
furan furan : A monocyclic heteroarene with a structure consisting of a 5-membered ring containing four carbons and one oxygen, with formula C4H4O. It is a toxic, flammable, low-boiling (31degreeC) colourless liquid.	7.03	1	furans; mancude organic heteromonocyclic parent; monocyclic heteroarene	carcinogenic agent; hepatotoxic agent; Maillard reaction product
yohimbine Yohimbine: A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.. yohimbine : An indole alkaloid with alpha2-adrenoceptor antagonist activity. It is produced by Corynanthe johimbe and Rauwolfia serpentina.	2.31	1	methyl 17-hydroxy-20xi-yohimban-16-carboxylate	alpha-adrenergic antagonist; dopamine receptor D2 antagonist; serotonergic antagonist
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.	4.28	18	azaarene; mancude organic heterobicyclic parent; ortho-fused heteroarene; quinazolines
cyproterone acetate [no description available]	2.02	1	20-oxo steroid; 3-oxo-Delta(4) steroid; acetate ester; chlorinated steroid; steroid ester	androgen antagonist; geroprotector; progestin
discretamine discretamine: structure	2.02	1	alkaloid
barium chloride barium chloride: RN given refers to parent cpd. barium chloride : The inorganic dichloride salt of barium.	2.02	1	barium salt; inorganic chloride	potassium channel blocker
indoramin Indoramin: An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent.	3.51	2	tryptamines
finasteride Finasteride: An orally active 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE inhibitor. It is used as a surgical alternative for treatment of benign PROSTATIC HYPERPLASIA.. finasteride : An aza-steroid that is a synthetic drug for the treatment of benign prostatic hyperplasia.	3.09	1	3-oxo steroid; aza-steroid; delta-lactam	androgen antagonist; antihyperplasia drug; EC 1.3.1.22 [3-oxo-5alpha-steroid 4-dehydrogenase (NADP(+))] inhibitor
niguldipine [no description available]	2.02	1	diarylmethane
turosteride turosteride: a 5alpha-reductase inhibitor; structure given in first source; RN given refers to the (5alpha,17beta)-isomer	3.09	1
epristeride epristeride: structure given in first source	3.09	1	steroid acid
corynanthine Corynanthine: A stereoisomer of yohimbine.	2.02	1	yohimban alkaloid
chlorethylclonidine chlorethylclonidine: RN refers to 2-chloroethyl derivative	2.42	2
cgp 42112a CGP 42112A: a hexapeptide analog of angiotensin II; activation of Receptor, Angiotensin, Type 2 results in vasodilation. CGP-42112A : A hexapeptide consisting of L-tyrosine, L-lysine, L-histidine, L-proline and L-isoleucine amino acid residues coupled in sequence and in which the amino group of the L-tyrosyl residue is substituted by a (pyridin-3-ylcarbonyl)nitrilo group and in which the L-lysyl side chain amino group is substituted by a {N(2)-[(benzyloxy)carbonyl]-L-arginyl}nitrilo group. It is a potent angiotensin II receptor type 2 (AT2 receptor) agonist.	2.01	1	benzyl ester; oligopeptide; pyridinecarboxamide	angiotensin receptor agonist; anti-inflammatory agent; antineoplastic agent; neuroprotective agent; vasodilator agent
sk&f 104856 SK&F 104856: structure given in first source	3.51	2
tamsulosin [no description available]	3.09	1	5-(2-{[2-(2-ethoxyphenoxy)ethyl]amino}propyl)-2-methoxybenzenesulfonamide	alpha-adrenergic antagonist; antineoplastic agent
rec 15-2739 Rec 15-2739: an alpha-1 antagonist selective for the lower urinary tract; structure given in first source	3.51	2
abanoquil [no description available]	2.02	1
ly 300502 [no description available]	3.09	1
bmy 7378 [no description available]	4.51	7
rs 100329 RS 100329: an alpha(1A)-adrenoceptor antagonist; structure in first source	2.75	3	piperazines
rs 17053 [no description available]	3.51	2	indoles
silodosin silodosin: an alpha(1a)-adrenoceptor-selective antagonist; structure given in first source	3.51	2	indolecarboxamide
17-n,n-diethylcarbamoyl-4-methyl-4-azaandrostane-3-one 17-N,N-diethylcarbamoyl-4-methyl-4-azaandrostane-3-one: inhibitor of testosterone 5-alpha reductase, receptor binding & nuclear uptake of androgens in the prostate	3.09	1
dexniguldipine niguldipine: structure given in first source; clinical modulator of multidrug resistance	3.09	1	diarylmethane
ro 70-0004 [no description available]	3.51	2

Condition	Relationship Strength	Studies
Adenoma, Prostatic [description not available]	2.91	1
Prostatic Hyperplasia Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both.	2.91	1
Cancer of Prostate [description not available]	2.05	1
Prostatic Neoplasms Tumors or cancer of the PROSTATE.	2.05	1
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.	2.74	3
Blood Pressure, High [description not available]	2.04	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.	2.04	1
Pyrexia [description not available]	2.04	1
Fever An abnormal elevation of body temperature, usually as a result of a pathologic process.	2.04	1

cyclazosin

Description

Cross-References

Synonyms (27)

Research Excerpts

Overview

Roles (1)

Drug Classes (6)

Protein Targets (16)

Inhibition Measurements

Activation Measurements

Biological Processes (54)

Molecular Functions (9)

Ceullar Components (11)

Bioassays (58)

Research

Studies (22)

Market Indicators

Research Demand Index: 11.61

Study Types

cyclazosin

Description

Cross-References

Synonyms (27)

Research Excerpts

Overview

Roles (1)

Drug Classes (6)

Protein Targets (16)

Inhibition Measurements

Activation Measurements

Biological Processes (54)

Molecular Functions (9)

Ceullar Components (11)

Bioassays (58)

Research

Studies (22)

Market Indicators

Research Demand Index: 11.61

Study Types

Related Drugs (51)

Related Conditions (9)