Page last updated: 2024-12-11

pd 136450

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

Description

PD 136450: gastrin receptor antagonist; dipeptoid which resembles the carboxy-terminal moiety of gastrin [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	6439414
CHEMBL ID	341460
CHEMBL ID	3351022
SCHEMBL ID	6895211
MeSH ID	M0208408

Synonyms (22)

Synonym
2-butenoic acid, 4-((2-((3-(1h-indol-3-yl)-2-methyl-1-oxo-2-(((tricyclo(3.3.1.1(3,7))dec-2-yloxy)carbonyl)amino)propyl)amino)-1-phenylethyl)amino)-4-oxo-, (r-(r,r))-
gtpl867
pd-136,450
139067-52-0
cam-1189
cam 1189
pd-136450
4-((2- ((3-(1h-indol-3-yl)-2-methyl-1-oxo-2-(((tricyclo(3.3.1.1(3,7))dec-2-yloxy)carbonyl)amino)propyl)amino)-1-phenylethyl)amino)-4-oxo-2-butenoic acid
pd136450 ,
cam1189
pd 136450
CHEMBL341460 ,
bdbm50007439
3-{2-[2-(adamantan-2-yloxycarbonylamino)-3-(1h-indol-3-yl)-2-methyl-propionylamino]-1-phenyl-ethylcarbamoyl}-acrylic acid
(e)-4-[[(1r)-2-[[(2r)-2-(2-adamantyloxycarbonylamino)-3-(1h-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobut-2-enoic acid
SCHEMBL6895211
CHEMBL3351022 ,
Q27088262
bdbm50230677
(e)-4-[[2-[[2-(2-adamantyloxycarbonylamino)-3-(1h-indol-3-yl)-2-methylpropanoyl]amino]-1-phenylethyl]amino]-4-oxobut-2-enoic acid
2-butenoic acid, 4-[[(1r)-2-[[(2r)-3-(1h-indol-3-yl)-2-methyl-1-oxo-2-[[(tricyclo[3.3.1.13,7]dec-2-yloxy)carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxo-
AKOS040749145

Research Excerpts

Dosage Studied

Excerpt	Relevance	Reference
" Increasing concentrations of PD 136450 caused a monophasic dose-response curve in contrast to the well-known biphasic amylase release in response to CCK8."	( A new CCK-B/gastrin receptor antagonist acts as an agonist on the rat pancreas. Arnold, R; Eissele, R; Koop, H; Koop, I; Meyer, F; Mössner, J; Patberg, H; Richter, S, 1994)	0.58

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

Protein Targets (1)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Cholecystokinin receptor type A	Rattus norvegicus (Norway rat)	IC50 (µMol)	0.7900	0.0000	0.4362	4.3000	AID53030
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (7)

Assay ID	Title	Year	Journal	Article
AID51119	Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to mouse cerebral cortex Cholecystokinin type B receptor	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID50513	Ratio calculated as IC50 ratio of Cholecystokinin type A receptor to that of Cholecystokinin type B receptor	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID178584	Effective dose to inhibit pentagastrin stimulated gastric acid secretion in rats(iv administration)	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID178585	Effective dose to inhibit pentagastrin stimulated gastric acid secretion in rats(sc administration)	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID53030	Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas Cholecystokinin type A receptor	1991	Journal of medicinal chemistry, Jan, Volume: 34, Issue:1	Rationally designed "dipeptoid" analogues of CCK. alpha-Methyltryptophan derivatives as highly selective and orally active gastrin and CCK-B antagonists with potent anxiolytic properties.
AID51280	Cholecystokinin type B receptor binding assay performed on homogenized cerebral cortex from male mouse	1992	Journal of medicinal chemistry, May-01, Volume: 35, Issue:9	Rationally designed "dipeptoid" analogues of CCK. A Free-Wilson/Fujita-Ban analysis of some alpha-methyltryptophan derivatives as CCK-B antagonists.
AID1346809	Rat CCK1 receptor (Cholecystokinin receptors)	1994	The Journal of pharmacology and experimental therapeutics, Jun, Volume: 269, Issue:3	Characterization of cholecystokininA receptor agonist activity by a family of cholecystokininB receptor antagonists.
[information is prepared from bioassay 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	10 (76.92)	18.2507
2000's	2 (15.38)	29.6817
2010's	1 (7.69)	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: 11.50

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	11.50 (24.57)
Research Supply Index	2.71 (2.92)
Research Growth Index	4.20 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (11.50)

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	14 (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
histamine [no description available]	1.98	1	aralkylamino compound; imidazoles	human metabolite; mouse metabolite; neurotransmitter
indomethacin Indomethacin: A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.. indometacin : A member of the class of indole-3-acetic acids that is indole-3-acetic acid in which the indole ring is substituted at positions 1, 2 and 5 by p-chlorobenzoyl, methyl, and methoxy groups, respectively. A non-steroidal anti-inflammatory drug, it is used in the treatment of musculoskeletal and joint disorders including osteoarthritis, rheumatoid arthritis, gout, bursitis and tendinitis.	2.44	2	aromatic ether; indole-3-acetic acids; monochlorobenzenes; N-acylindole	analgesic; drug metabolite; EC 1.14.99.1 (prostaglandin-endoperoxide synthase) inhibitor; environmental contaminant; gout suppressant; non-steroidal anti-inflammatory drug; xenobiotic metabolite; xenobiotic
lansoprazole Lansoprazole: A 2,2,2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a racemic mixture of (R)- and (S)-isomers.	2.44	2	benzimidazoles; pyridines; sulfoxide	anti-ulcer drug; EC 3.6.3.10 (H(+)/K(+)-exchanging ATPase) inhibitor
omeprazole Omeprazole: A 4-methoxy-3,5-dimethylpyridyl, 5-methoxybenzimidazole derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits an H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS.. omeprazole : A racemate comprising equimolar amounts of (R)- and (S)-omeprazole.. 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole : A member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a [4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl group at position 2 and a methoxy group at position 5.	2.9	4	aromatic ether; benzimidazoles; pyridines; sulfoxide
meglumine Meglumine: 1-Deoxy-1-(methylamino)-D-glucitol. A derivative of sorbitol in which the hydroxyl group in position 1 is replaced by a methylamino group. Often used in conjunction with iodinated organic compounds as contrast medium.. N-methylglucamine : A hexosamine that is D-glucitol in which the hydroxy group at position 1 is substituted by the nitrogen of a methylamino group. A crystalline base, it is used in preparing salts of certain acids for use as diagnostic radiopaque media, while its antimonate is used as an antiprotozoal in the treatment of leishmaniasis.	2.39	2	hexosamine; secondary amino compound
adamantane Adamantane: A tricyclo bridged hydrocarbon.	1.99	1	adamantanes; polycyclic alkane
ng-nitroarginine methyl ester NG-Nitroarginine Methyl Ester: A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.	2.06	1	alpha-amino acid ester; L-arginine derivative; methyl ester; N-nitro compound	EC 1.14.13.39 (nitric oxide synthase) inhibitor
ci 988 PD 134308: selective cholecystokinin type B receptor antagonist; inhibits growth of LoVo, a human colon cancer cell line; structure given in first source	2.9	4
b 823-08 B 823-08: structure given in first source	2.67	3	aromatic ether
devazepide Devazepide: A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.. devazepide : An indolecarboxamide obtained by formal condensation of the carboxy group of indole-2-carboxylic acid with the exocyclic amino group of (3S)-3-amino-1-methyl-5-phenyl-1,3-dihydro-1,4-benzodiazepin-2-one. A cholecystokinin antagonist used for treatment of gastrointestinal disorders.	2.9	4	1,4-benzodiazepinone; indolecarboxamide	antineoplastic agent; apoptosis inducer; cholecystokinin antagonist; gastrointestinal drug
ranitidine Ranitidine: A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.. ranitidine : A member of the class of furans used to treat peptic ulcer disease (PUD) and gastroesophageal reflux disease.	2.06	1	C-nitro compound; furans; organic sulfide; tertiary amino compound	anti-ulcer drug; drug allergen; environmental contaminant; H2-receptor antagonist; xenobiotic
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	2.9	4	benzodiazepine
sincalide Sincalide: An octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.	2.9	4	oligopeptide
pentagastrin Pentagastrin: A synthetic pentapeptide that has effects like gastrin when given parenterally. It stimulates the secretion of gastric acid, pepsin, and intrinsic factor, and has been used as a diagnostic aid.	2.38	2	organic molecular entity
pd 140548 [no description available]	2.39	2
cholecystokinin Cholecystokinin: A peptide, of about 33 amino acids, secreted by the upper INTESTINAL MUCOSA and also found in the central nervous system. It causes gallbladder contraction, release of pancreatic exocrine (or digestive) enzymes, and affects other gastrointestinal functions. Cholecystokinin may be the mediator of satiety.	1.98	1
gastrins Gastrins: A family of gastrointestinal peptide hormones that excite the secretion of GASTRIC JUICE. They may also occur in the central nervous system where they are presumed to be neurotransmitters.	3.08	5
gastrin 17 gastrin-17 : One of the primary forms of gastrin that is a 17-membered peptide consisting of Glp, Gly, Pro, Trp, Leu, Glu, Glu, Glu, Glu, Glu, Ala, Tyr, Gly, Trp, Met, Asp and Phe-NH2 residues joined in sequence.	1.98	1	gastrin	antineoplastic agent
pd 135158 PD 135158: selective cholecystokinin type B receptor agonist; structure given in first source	1.98	1

Condition	Relationship Strength	Studies
Gastric Ulcer [description not available]	2.44	2
Stomach Ulcer Ulceration of the GASTRIC MUCOSA due to contact with GASTRIC JUICE. It is often associated with HELICOBACTER PYLORI infection or consumption of nonsteroidal anti-inflammatory drugs (NSAIDS).	2.44	2
Achlorhydria A lack of HYDROCHLORIC ACID in GASTRIC JUICE despite stimulation of gastric secretion.	2.39	2

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