Page last updated: 2024-11-12

pd 168368

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

Description

PD 168368: a neuromedin B receptor antagonist; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	9937534
CHEMBL ID	329650
SCHEMBL ID	6249801
MeSH ID	M0378152

Synonyms (19)

Synonym
CHEMBL329650 ,
(2s)-3-(1h-indol-3-yl)-2-methyl-2-[(4-nitrophenyl)carbamoylamino]-n-[(1-pyridin-2-ylcyclohexyl)methyl]propanamide
pd 168368
pd-168368
pd168368 ,
gtpl621
(s)-3-(1h-indol-3-yl)-2-methyl-2-[3-(4-nitro-phenyl)-ureido]-n-(1-pyridin-2-yl-cyclohexylmethyl)-propionamide
bdbm50071735
(s)-a-methyl-a-[[[(4-nitrophenyl)amino]carbonyl]amino]-n-[[1-(2-pyridinyl)cyclohexyl]methyl]-1h-indole-3-propanamide
SCHEMBL6249801
204066-82-0
J-013285
(s)-3-(1h-indol-3-yl)-2-methyl-2-(3-(4-nitrophenyl)ureido)-n-((1-(pyridin-2-yl)cyclohexyl)methyl)propanamide
Q27088274
pd 168368 is known as an nmbr antagonist.
MS-30117
HY-116216
CS-0064383
AKOS040759496

Research Excerpts

Dosage Studied

Excerpt	Relevance	Reference
" The first aim of this study was to pharmacologically compare the dose-response curves for scratching induced by intrathecally administered bombesin-related peptides versus morphine, which is known to elicit itch in humans."	( Physiological function of gastrin-releasing peptide and neuromedin B receptors in regulating itch scratching behavior in the spinal cord of mice. Ko, MC; Sukhtankar, DD, 2013)	0.39

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

Protein Targets (2)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Neuromedin-B receptor	Homo sapiens (human)	Ki	0.0002	0.0002	0.0008	0.0020	AID42490
Gastrin-releasing peptide receptor	Homo sapiens (human)	Ki	0.0170	0.0002	0.0061	0.0170	AID42630
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (17)

Process	via Protein(s)	Taxonomy
phospholipase C-activating G protein-coupled receptor signaling pathway	Neuromedin-B receptor	Homo sapiens (human)
neuropeptide signaling pathway	Neuromedin-B receptor	Homo sapiens (human)
bombesin receptor signaling pathway	Neuromedin-B receptor	Homo sapiens (human)
negative regulation of interleukin-6 production	Neuromedin-B receptor	Homo sapiens (human)
positive regulation of interferon-alpha production	Neuromedin-B receptor	Homo sapiens (human)
positive regulation of osteoclast proliferation	Neuromedin-B receptor	Homo sapiens (human)
antiviral innate immune response	Neuromedin-B receptor	Homo sapiens (human)
sneeze reflex	Neuromedin-B receptor	Homo sapiens (human)
positive regulation of respiratory gaseous exchange	Neuromedin-B receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Neuromedin-B receptor	Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathway	Gastrin-releasing peptide receptor	Homo sapiens (human)
neuropeptide signaling pathway	Gastrin-releasing peptide receptor	Homo sapiens (human)
learning or memory	Gastrin-releasing peptide receptor	Homo sapiens (human)
social behavior	Gastrin-releasing peptide receptor	Homo sapiens (human)
psychomotor behavior	Gastrin-releasing peptide receptor	Homo sapiens (human)
regulation of cell population proliferation	Gastrin-releasing peptide receptor	Homo sapiens (human)
response to external biotic stimulus	Gastrin-releasing peptide receptor	Homo sapiens (human)
motor behavior	Gastrin-releasing peptide receptor	Homo sapiens (human)
positive regulation of respiratory gaseous exchange	Gastrin-releasing peptide receptor	Homo sapiens (human)
positive regulation of behavioral fear response	Gastrin-releasing peptide receptor	Homo sapiens (human)
G protein-coupled receptor signaling pathway	Gastrin-releasing peptide receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Process	via Protein(s)	Taxonomy
bombesin receptor activity	Neuromedin-B receptor	Homo sapiens (human)
neuropeptide receptor activity	Neuromedin-B receptor	Homo sapiens (human)
neuropeptide receptor activity	Gastrin-releasing peptide receptor	Homo sapiens (human)
G protein-coupled peptide receptor activity	Gastrin-releasing peptide receptor	Homo sapiens (human)
neuropeptide binding	Gastrin-releasing peptide receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (2)

Process	via Protein(s)	Taxonomy
cytosol	Neuromedin-B receptor	Homo sapiens (human)
plasma membrane	Neuromedin-B receptor	Homo sapiens (human)
plasma membrane	Neuromedin-B receptor	Homo sapiens (human)
plasma membrane	Gastrin-releasing peptide receptor	Homo sapiens (human)
plasma membrane	Gastrin-releasing peptide receptor	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay ID	Title	Year	Journal	Article
AID42490	Antagonism of recombinant human bombesin receptor (bb1) labeled with [125I]- [Tyr] bombesin stably expressed in CHO cells	1998	Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18	PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID42630	In vitro binding affinity at Bombesin BB2 receptor in the presence of [125I]-[Tyr] bombesin.	1998	Bioorganic & medicinal chemistry letters, Sep-22, Volume: 8, Issue:18	PD 176252--the first high affinity non-peptide gastrin-releasing peptide (BB2) receptor antagonist.
AID1346439	Human BB1 receptor (Bombesin receptors)	2009	Peptides, Aug, Volume: 30, Issue:8	Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors.
AID1346539	Human BB2 receptor (Bombesin receptors)	2009	Peptides, Aug, Volume: 30, Issue:8	Characterization of putative GRP- and NMB-receptor antagonist's interaction with human receptors.
AID1346497	Rat BB1 receptor (Bombesin receptors)	1999	The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3	Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368.
AID1346539	Human BB2 receptor (Bombesin receptors)	1999	The Journal of pharmacology and experimental therapeutics, Sep, Volume: 290, Issue:3	Comparative pharmacology of the nonpeptide neuromedin B receptor antagonist PD 168368.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (15)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	2 (13.33)	18.2507
2000's	4 (26.67)	29.6817
2010's	9 (60.00)	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]

Market Indicators

Research Demand Index: 12.01

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

Metric	This Compound (vs All)
Research Demand Index	12.01 (24.57)
Research Supply Index	2.77 (2.92)
Research Growth Index	4.78 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (12.01)

All Compounds (24.57)

Study Types

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	15 (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
tyrosine Tyrosine: A non-essential amino acid. In animals it is synthesized from PHENYLALANINE. It is also the precursor of EPINEPHRINE; THYROID HORMONES; and melanin.. tyrosine : An alpha-amino acid that is phenylalanine bearing a hydroxy substituent at position 4 on the phenyl ring.	2	1	amino acid zwitterion; erythrose 4-phosphate/phosphoenolpyruvate family amino acid; L-alpha-amino acid; proteinogenic amino acid; tyrosine	EC 1.3.1.43 (arogenate dehydrogenase) inhibitor; fundamental metabolite; micronutrient; nutraceutical
toluene 2,4-diisocyanate Toluene 2,4-Diisocyanate: Skin irritant and allergen used in the manufacture of polyurethane foams and other elastomers.. toluene 2,4-diisocyanate : A toluene meta-diisocyanate in which the isocyanato groups are at positions 2 and 4 relative to the methyl group on the benzene ring.	2.21	1	toluene meta-diisocyanate	allergen; hapten
rc 3095 bombesin (6-14), Tpi(6)-Leu(13)-psi(CH2NH)-Leu(14)-: an antagonist of bombesin	2.48	2
morphine Meconium: The thick green-to-black mucilaginous material found in the intestines of a full-term fetus. It consists of secretions of the INTESTINAL GLANDS; BILE PIGMENTS; FATTY ACIDS; AMNIOTIC FLUID; and intrauterine debris. It constitutes the first stools passed by a newborn.	2.08	1	morphinane alkaloid; organic heteropentacyclic compound; tertiary amino compound	anaesthetic; drug allergen; environmental contaminant; geroprotector; mu-opioid receptor agonist; opioid analgesic; plant metabolite; vasodilator agent; xenobiotic
neurokinin b Neurokinin B: A mammalian neuropeptide of 10 amino acids that belongs to the tachykinin family. It is similar in structure and action to SUBSTANCE P and NEUROKININ A with the ability to excite neurons, dilate blood vessels, and contract smooth muscles, such as those in the URINARY BLADDER and UTERUS.	2.95	4	polypeptide
pd 176252 PD 176252: a non-peptide gastrin-releasing peptide (BB2) receptor antagonist; structure in first source	3.28	6
bombesin [no description available]	1.99	1
neuromedin b neuromedin B: decapeptide isolated from porcine spinal cord	2.95	4
gastrin-releasing peptide Gastrin-Releasing Peptide: Neuropeptide and gut hormone that helps regulate GASTRIC ACID secretion and motor function. Once released from nerves in the antrum of the STOMACH, the neuropeptide stimulates release of GASTRIN from the GASTRIN-SECRETING CELLS.	2.98	4

Condition	Relationship Strength	Studies
Allergic Contact Dermatitis [description not available]	2.21	1
Itching [description not available]	2.79	3
Pruritus An intense itching sensation that produces the urge to rub or scratch the skin to obtain relief.	2.79	3
Dermatitis, Allergic Contact A contact dermatitis due to allergic sensitization to various substances. These substances subsequently produce inflammatory reactions in the skin of those who have acquired hypersensitivity to them as a result of prior exposure.	2.21	1
Breast Cancer [description not available]	2.49	2
Metastase [description not available]	2.13	1
Invasiveness, Neoplasm [description not available]	2.13	1
Breast Neoplasms Tumors or cancer of the human BREAST.	2.49	2
Neoplasm Metastasis The transfer of a neoplasm from one organ or part of the body to another remote from the primary site.	2.13	1
Pregnancy The status during which female mammals carry their developing young (EMBRYOS or FETUSES) in utero before birth, beginning from FERTILIZATION to BIRTH.	2.05	1
Angiogenesis, Pathologic [description not available]	2.06	1
Cancer of Lung [description not available]	2.01	1
Lung Neoplasms Tumors or cancer of the LUNG.	2.01	1

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