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ee 581

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

Description

EE 581: photosensitive azido derivative of tyrosine(3)-octreotide used to label the somatostatin receptor; amino acid sequence given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	3036100
MeSH ID	M0200722

Synonyms (8)

Synonym
azidophenylalanyl-cysteinyl-tyrosyl-tryptophyl-lysyl-threonyl-cysteinyl-threonin-ol
ee-581
141949-00-0
l-cysteinamide, 4-azido-d-phenylalanyl-l-cysteinyl-l-tyrosyl-d-tryptophyl-l-lysyl-l-threonyl-n-(2-hydroxy-1-(hydroxymethyl)propyl)-, cyclic (2-7)-disulfide, (r-(r,r))-
phe(n3)-cys-tyr-trp-lys-thr-cys-thr-ol
ee 581
(2s)-2-[[(2r)-3-[(1ar)-1a,2-dihydrothiireno[2,3-b]indol-6b-yl]-2-[[(2s)-2-[[(2s)-2-[[(2r)-2-amino-3-(4-azidophenyl)propanoyl]amino]propanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-n-[(2s,3r)-1-[[(2r)-2-(1,3-dihydroxybutan-2-ylamino)-3-
(2s)-2-((2r)-2-((s)-2-((s)-2-((r)-2-amino-3-(4-azidophenyl)propanamido)propanamido)-3-(4-hydroxyphenyl)propanamido)-3-((1ar)-1a,2-dihydro-6bh-thiireno[2,3-b]indol-6b-yl)propanamido)-n-((2s,3r)-1-((2r)-2-((1,3-dihydroxybutan-2-yl)amino)-3-mercaptopropanami

Research Excerpts

Bioavailability

Excerpt	Reference	Relevance
" Suvorexant (MK-4305) is a potent, selective, and orally bioavailable antagonist of OX(1)R and OX(2)R currently under clinical investigation as a novel therapy for insomnia."	( Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist. Breslin, MJ; Coleman, PJ; Cox, CD; Cui, D; Doran, SM; Fox, SV; Garson, SL; Gotter, AL; Harrell, CM; Reiss, DR; Renger, JJ; Stevens, J; Tannenbaum, PL; Winrow, CJ, 2011)	0.37

Dosage Studied

Excerpt	Relevance	Reference
" Dosed orally Suvorexant significantly and dose-dependently reduced locomotor activity and promoted sleep in rats (10, 30, and 100 mg/kg), dogs (1 and 3 mg/kg), and rhesus monkeys (10 mg/kg)."	( Promotion of sleep by suvorexant-a novel dual orexin receptor antagonist. Breslin, MJ; Coleman, PJ; Cox, CD; Cui, D; Doran, SM; Fox, SV; Garson, SL; Gotter, AL; Harrell, CM; Reiss, DR; Renger, JJ; Stevens, J; Tannenbaum, PL; Winrow, CJ, 2011)	0.37

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

Research

Studies (13)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	1 (7.69)	18.2507
2000's	4 (30.77)	29.6817
2010's	8 (61.54)	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]

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	1 (7.69%)	6.00%
Case Studies	1 (7.69%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (84.62%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
trimethylamine [no description available]	2.05	1	methylamines; tertiary amine	Escherichia coli metabolite; human xenobiotic metabolite
4-aminopyridine [no description available]	2.05	1	aminopyridine; aromatic amine	avicide; orphan drug; potassium channel blocker
pilocarpine Pilocarpine: A slowly hydrolyzed muscarinic agonist with no nicotinic effects. Pilocarpine is used as a miotic and in the treatment of glaucoma.. (+)-pilocarpine : The (+)-enantiomer of pilocarpine.	2.05	1	pilocarpine	antiglaucoma drug
azides Azides: Organic or inorganic compounds that contain the -N3 group.. azide : Any nitrogen molecular entity containing the group -N3.	5.1	13	pseudohalide anion	mitochondrial respiratory-chain inhibitor
triazoles Triazoles: Heterocyclic compounds containing a five-membered ring with two carbon atoms and three nitrogen atoms with the molecular formula C2H3N3.. triazoles : An azole in which the five-membered heterocyclic aromatic skeleton contains three N atoms and two C atoms.	2.06	1	1,2,3-triazole
quinine [no description available]	2.05	1	cinchona alkaloid	antimalarial; muscle relaxant; non-narcotic analgesic
suvorexant suvorexant: an orexin receptor antagonist; structure in first source. suvorexant : An aromatic amide obtained by formal condensation of the carboxy group of 5-methyl-2-(2H-1,2,3-triazol-2-yl)benzoic acid with the secondary amino group of 5-chloro-2-[(5R)-5-methyl-1,4-diazepan-1-yl]-1,3-benzoxazole. An orexin receptor antagonist used for the management of insomnia.	2.06	1	1,3-benzoxazoles; aromatic amide; diazepine; organochlorine compound; triazoles	central nervous system depressant; orexin receptor antagonist

Condition	Relationship Strength	Studies
Aura [description not available]	3.39	2
Abdominal Migraine [description not available]	3	1
Epilepsy A disorder characterized by recurrent episodes of paroxysmal brain dysfunction due to a sudden, disorderly, and excessive neuronal discharge. Epilepsy classification systems are generally based upon: (1) clinical features of the seizure episodes (e.g., motor seizure), (2) etiology (e.g., post-traumatic), (3) anatomic site of seizure origin (e.g., frontal lobe seizure), (4) tendency to spread to other structures in the brain, and (5) temporal patterns (e.g., nocturnal epilepsy). (From Adams et al., Principles of Neurology, 6th ed, p313)	3.39	2
Migraine Disorders A class of disabling primary headache disorders, characterized by recurrent unilateral pulsatile headaches. The two major subtypes are common migraine (without aura) and classic migraine (with aura or neurological symptoms). (International Classification of Headache Disorders, 2nd ed. Cephalalgia 2004: suppl 1)	3	1
Acute Lymphoid Leukemia [description not available]	2.11	1
Central Nervous System Disease [description not available]	2.11	1
Central Nervous System Diseases Diseases of any component of the brain (including the cerebral hemispheres, diencephalon, brain stem, and cerebellum) or the spinal cord.	2.11	1
Precursor Cell Lymphoblastic Leukemia-Lymphoma A neoplasm characterized by abnormalities of the lymphoid cell precursors leading to excessive lymphoblasts in the marrow and other organs. It is the most common cancer in children and accounts for the vast majority of all childhood leukemias.	2.11	1
Cognition Disorders Disorders characterized by disturbances in mental processes related to learning, thinking, reasoning, and judgment.	2.13	1
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.75	3
Fra(X) Syndrome [description not available]	2.13	1
Fragile X Syndrome A condition characterized genotypically by mutation of the distal end of the long arm of the X chromosome (at gene loci FRAXA or FRAXE) and phenotypically by cognitive impairment, hyperactivity, SEIZURES, language delay, and enlargement of the ears, head, and testes. INTELLECTUAL DISABILITY occurs in nearly all males and roughly 50% of females with the full mutation of FRAXA. (From Menkes, Textbook of Child Neurology, 5th ed, p226)	2.13	1
Disease Exacerbation [description not available]	2.13	1
Brain Inflammation [description not available]	2.13	1
Atrophy Decrease in the size of a cell, tissue, organ, or multiple organs, associated with a variety of pathological conditions such as abnormal cellular changes, ischemia, malnutrition, or hormonal changes.	2.13	1
Encephalitis Inflammation of the BRAIN due to infection, autoimmune processes, toxins, and other conditions. Viral infections (see ENCEPHALITIS, VIRAL) are a relatively frequent cause of this condition.	2.13	1
Anxiety Neuroses [description not available]	2.15	1
Separation Anxiety Disorder [description not available]	2.15	1
Anxiety Disorders Persistent and disabling ANXIETY.	2.15	1
Anxiety, Separation Anxiety experienced by an individual upon separation from a person or object of particular significance to the individual.	2.15	1
Abdominal Epilepsy [description not available]	2.05	1
Epilepsies, Partial Conditions characterized by recurrent paroxysmal neuronal discharges which arise from a focal region of the brain. Partial seizures are divided into simple and complex, depending on whether consciousness is unaltered (simple partial seizure) or disturbed (complex partial seizure). Both types may feature a wide variety of motor, sensory, and autonomic symptoms. Partial seizures may be classified by associated clinical features or anatomic location of the seizure focus. A secondary generalized seizure refers to a partial seizure that spreads to involve the brain diffusely. (From Adams et al., Principles of Neurology, 6th ed, pp317)	2.05	1
Absence Status [description not available]	2.03	1
Status Epilepticus A prolonged seizure or seizures repeated frequently enough to prevent recovery between episodes occurring over a period of 20-30 minutes. The most common subtype is generalized tonic-clonic status epilepticus, a potentially fatal condition associated with neuronal injury and respiratory and metabolic dysfunction. Nonconvulsive forms include petit mal status and complex partial status, which may manifest as behavioral disturbances. Simple partial status epilepticus consists of persistent motor, sensory, or autonomic seizures that do not impair cognition (see also EPILEPSIA PARTIALIS CONTINUA). Subclinical status epilepticus generally refers to seizures occurring in an unresponsive or comatose individual in the absence of overt signs of seizure activity. (From N Engl J Med 1998 Apr 2;338(14):970-6; Neurologia 1997 Dec;12 Suppl 6:25-30)	2.03	1

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