(1's, 2s)-4-amino-n-(1'-carbamoyl-2'-phenylethyl)-2-(4''-methyl-1''-naphthalenesulfonylamino)butanamide profile

(1'S, 2S)-4-amino-N-(1'-carbamoyl-2'-phenylethyl)-2-(4''-methyl-1''-naphthalenesulfonylamino)butanamide: a somatostatin receptor 4 agonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

ID Source	ID
PubMed CID	11442741
CHEMBL ID	4451852
SCHEMBL ID	4640775
MeSH ID	M0483203

Synonym
(1's, 2s)-4-amino-n-(1'-carbamoyl-2'-phenylethyl)-2-(4''-methyl-1''-naphthalenesulfonylamino)butanamide
j-2156
(1's,2s)-4-amino-n-(1'-carbamoyl-2'-phenylethyl)-2-(4''-methyl-1''-naphthalenesulfonylamino)butanamide
benzenepropanamide, .alpha.-(((2s)-4-amino-2-(((4-methyl-1-naphthalenyl)sulfonyl)amino)-1-oxobutyl)amino)-, (.alpha.s)-
H35JAI9M2X ,
848647-56-3
unii-h35jai9m2x
j 2156
SCHEMBL4640775
CHEMBL4451852
(s)-4-amino-n-((s)-1-amino-1-oxo-3-phenylpropan-2-yl)-2-((4-methylnaphthalene)-1-sulfonamido)butanamide
j-2156 tfa salt
j2156
gtpl10115
(2s)-4-amino-n-[(2s)-1-amino-1-oxo-3-phenylpropan-2-yl]-2-[(4-methylnaphthalen-1-yl)sulfonylamino]butanamide
CS-0088634
HY-111615
Q27279583
I8B ,
(2~{s})-2-[[(2~{s})-4-azanyl-2-[(4-methylnaphthalen-1-yl)sulfonylamino]butanoyl]amino]-3-phenyl-propanimidic acid
GLXC-26290
(2s)-4-amino-n-[(1s)-1-carbamoyl-2-phenylethyl]-2-(4-methylnaphthalene-1-sulfonamido)butanamide
EN300-1719195
AKOS040733479

Excerpt	Relevance	Reference
" Increasing concentrations of somatostatin-14 cause a concentration-dependent rightward shift of the dose-response curves for J-2156, without affecting its maximal response."	( Superagonism at the human somatostatin receptor subtype 4. Ahman, M; El-Darwish, K; Engström, M; Savola, JM; Tomperi, J; Wurster, S, 2005)	0.33

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Somatostatin receptor type 2	Homo sapiens (human)	Ki	5.0000	0.0000	0.4091	4.7200	AID1571204
Somatostatin receptor type 4	Homo sapiens (human)	Ki	0.0012	0.0006	0.2733	3.2000	AID1571203
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Process	via Protein(s)	Taxonomy
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Somatostatin receptor type 2	Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	Somatostatin receptor type 2	Homo sapiens (human)
spermatogenesis	Somatostatin receptor type 2	Homo sapiens (human)
negative regulation of cell population proliferation	Somatostatin receptor type 2	Homo sapiens (human)
cerebellum development	Somatostatin receptor type 2	Homo sapiens (human)
peristalsis	Somatostatin receptor type 2	Homo sapiens (human)
forebrain development	Somatostatin receptor type 2	Homo sapiens (human)
somatostatin signaling pathway	Somatostatin receptor type 2	Homo sapiens (human)
response to starvation	Somatostatin receptor type 2	Homo sapiens (human)
cellular response to glucocorticoid stimulus	Somatostatin receptor type 2	Homo sapiens (human)
cellular response to estradiol stimulus	Somatostatin receptor type 2	Homo sapiens (human)
neuropeptide signaling pathway	Somatostatin receptor type 2	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Somatostatin receptor type 4	Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	Somatostatin receptor type 4	Homo sapiens (human)
negative regulation of cell population proliferation	Somatostatin receptor type 4	Homo sapiens (human)
cell migration	Somatostatin receptor type 4	Homo sapiens (human)
forebrain development	Somatostatin receptor type 4	Homo sapiens (human)
somatostatin signaling pathway	Somatostatin receptor type 4	Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascade	Somatostatin receptor type 4	Homo sapiens (human)
positive regulation of arachidonic acid secretion	Somatostatin receptor type 4	Homo sapiens (human)
negative regulation of adenylate cyclase-activating G protein-coupled receptor signaling pathway	Somatostatin receptor type 4	Homo sapiens (human)
neuropeptide signaling pathway	Somatostatin receptor type 4	Homo sapiens (human)
cellular response to glucocorticoid stimulus	Somatostatin receptor type 4	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
protein binding	Somatostatin receptor type 2	Homo sapiens (human)
PDZ domain binding	Somatostatin receptor type 2	Homo sapiens (human)
somatostatin receptor activity	Somatostatin receptor type 2	Homo sapiens (human)
neuropeptide binding	Somatostatin receptor type 2	Homo sapiens (human)
protein binding	Somatostatin receptor type 4	Homo sapiens (human)
somatostatin receptor activity	Somatostatin receptor type 4	Homo sapiens (human)
neuropeptide binding	Somatostatin receptor type 4	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Process	via Protein(s)	Taxonomy
cytosol	Somatostatin receptor type 2	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 2	Homo sapiens (human)
neuron projection	Somatostatin receptor type 2	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 2	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 4	Homo sapiens (human)
neuron projection	Somatostatin receptor type 4	Homo sapiens (human)
plasma membrane	Somatostatin receptor type 4	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	5 (50.00)	29.6817
2010's	5 (50.00)	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	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	10 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.	2.04	1	ammonium salt; carbamate ester	cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic
tetradecanoylphorbol acetate Tetradecanoylphorbol Acetate: A phorbol ester found in CROTON OIL with very effective tumor promoting activity. It stimulates the synthesis of both DNA and RNA.. phorbol ester : Esters of phorbol, originally found in croton oil (from Croton tiglium, of the family Euphorbiaceae). A number of phorbol esters possess activity as tumour promoters and activate the mechanisms associated with cell growth. Some of these are used in experiments as activators of protein kinase C.. phorbol 13-acetate 12-myristate : A phorbol ester that is phorbol in which the hydroxy groups at the cyclopropane ring juction (position 13) and the adjacent carbon (position 12) have been converted into the corresponding acetate and myristate esters. It is a major active constituent of the seed oil of Croton tiglium. It has been used as a tumour promoting agent for skin carcinogenesis in rodents and is associated with increased cell proliferation of malignant cells. However its function is controversial since a decrease in cell proliferation has also been observed in several cancer cell types.	2.04	1	acetate ester; diester; phorbol ester; tertiary alpha-hydroxy ketone; tetradecanoate ester	antineoplastic agent; apoptosis inducer; carcinogenic agent; mitogen; plant metabolite; protein kinase C agonist; reactive oxygen species generator
capsaicin ALGRX-4975: an injectable capsaicin (TRPV1 receptor agonist) formulation for longlasting pain relief. capsaicinoid : A family of aromatic fatty amides produced as secondary metabolites by chilli peppers.	2.1	1	capsaicinoid	non-narcotic analgesic; TRPV1 agonist; voltage-gated sodium channel blocker
ovalbumin Ovalbumin: An albumin obtained from the white of eggs. It is a member of the serpin superfamily.	2.04	1
d-phenylalanyl-cysteinyl-tyrosyl-tryptophyl-lysyl-cysteinyl-threoninamide TT2-32: induces a biphasic activation of phosphotyrosine phosphatase activity in human colon tumor cell line, SW620	2.04	1
guanosine 5'-o-(3-thiotriphosphate) Guanosine 5'-O-(3-Thiotriphosphate): Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.	2.03	1	nucleoside triphosphate analogue

Condition	Relationship Strength	Studies
Innate Inflammatory Response [description not available]	2.46	2
Ache [description not available]	2.46	2
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	2.46	2
Pain An unpleasant sensation induced by noxious stimuli which are detected by NERVE ENDINGS of NOCICEPTIVE NEURONS.	2.46	2
Disease Models, Animal Naturally-occurring or experimentally-induced animal diseases with pathological processes analogous to human diseases.	2.52	2
Allodynia [description not available]	2.46	2
Neuritis A general term indicating inflammation of a peripheral or cranial nerve. Clinical manifestation may include PAIN; PARESTHESIAS; PARESIS; or HYPESTHESIA.	2.11	1
Anxiety Feelings or emotions of dread, apprehension, and impending disaster but not disabling as with ANXIETY DISORDERS.	2.13	1
Depression Depressive states usually of moderate intensity in contrast with MAJOR DEPRESSIVE DISORDER present in neurotic and psychotic disorders.	2.13	1
Chronic Illness [description not available]	2.03	1
Acute Disease Disease having a short and relatively severe course.	2.03	1
Chronic Disease Diseases which have one or more of the following characteristics: they are permanent, leave residual disability, are caused by nonreversible pathological alteration, require special training of the patient for rehabilitation, or may be expected to require a long period of supervision, observation, or care (Dictionary of Health Services Management, 2d ed). For epidemiological studies chronic disease often includes HEART DISEASES; STROKE; CANCER; and diabetes (DIABETES MELLITUS, TYPE 2).	2.03	1
Neurogenic Inflammation Inflammation caused by an injurious stimulus of peripheral neurons and resulting in release of neuropeptides which affect vascular permeability and help initiate proinflammatory and immune reactions at the site of injury.	2.03	1
Adjuvant Arthritis [description not available]	2.03	1
Anasarca [description not available]	2.03	1
Eosinophilia, Pulmonary [description not available]	2.03	1
Edema Abnormal fluid accumulation in TISSUES or body cavities. Most cases of edema are present under the SKIN in SUBCUTANEOUS TISSUE.	2.03	1
Pulmonary Eosinophilia A condition characterized by infiltration of the lung with EOSINOPHILS due to inflammation or other disease processes. Major eosinophilic lung diseases are the eosinophilic pneumonias caused by infections, allergens, or toxic agents.	2.03	1
Bacterial Pneumonia [description not available]	2.04	1
Asthma, Bronchial [description not available]	2.04	1
Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL).	2.04	1
Bronchial Hyperreactivity Tendency of the smooth muscle of the tracheobronchial tree to contract more intensely in response to a given stimulus than it does in the response seen in normal individuals. This condition is present in virtually all symptomatic patients with asthma. The most prominent manifestation of this smooth muscle contraction is a decrease in airway caliber that can be readily measured in the pulmonary function laboratory.	2.04	1
Pneumonia, Bacterial Inflammation of the lung parenchyma that is caused by bacterial infections.	2.04	1

Assay ID	Title	Year	Journal	Article
AID1571203	Displacement of [125I]-LTT-SRIF-28 from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 60 mins by scintillation counting method
AID1571204	Displacement of [125I]-LTT-SRIF-28 from recombinant human SST2 receptor expressed in CHO cell membranes after 60 mins by scintillation counting method
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

(1's, 2s)-4-amino-n-(1'-carbamoyl-2'-phenylethyl)-2-(4''-methyl-1''-naphthalenesulfonylamino)butanamide

Description

Cross-References

Synonyms (24)

Research Excerpts

Dosage Studied

Protein Targets (2)

Inhibition Measurements

Biological Processes (17)

Molecular Functions (4)

Ceullar Components (3)

Bioassays (2)

Research

Studies (10)

Market Indicators

Research Demand Index: 12.06

Study Types