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sincalide

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Description

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. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9833444
CHEMBL ID1121
CHEBI ID135946
SCHEMBL ID122365
MeSH IDM0019891

Synonyms (90)

Synonym
cck-8 (sulphated)
(3s)-3-[[(2s)-2-[[(2s)-2-[[2-[[(2s)-2-[[(2s)-2-[[(2s)-2-amino-4-hydroxy-4-oxobutanoyl]amino]-3-(4-sulfooxyphenyl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]acetyl]amino]-3-(1h-indol-3-yl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-[[(2s)-1-ami
gtpl864
l-alpha-aspartyl-o-sulfo-l-tyrosyl-l-methionylglycyl-l-tryptophyl-l-methionyl-l-alpha-aspartyl-l-phenylalaninamide
1-de(5-oxo-l-proline)-2-de-l-glutamine-5-l-methioninecaerulein
kinevac
sincalidum [inn-latin]
caerulein, 1-de(5-oxo-l-proline)-2-de-l-glutamine-5-l-methionine-
sq 19844
einecs 246-639-0
sincalide
l-aspartyl-l-tyrosyl-l-methionylglycyl-l-tryptophyl-l-methionyl-l-aspartylphenyl-l-alaninamide hydrogen sulfate (ester)
sincalida [inn-spanish]
25126-32-3
D05845
cholecystokinin-pancreozymin
kinevac (tn)
sincalide (usan/inn)
cck-8
[125i]cck-8
syncalide
cck-8(so3)
(3s)-3-[(2s)-2-[(2s)-2-{2-[(2s)-2-[(2s)-2-[(3s)-3-amino-3-formamidopropanoic acid]-3-[4-(sulfooxy)phenyl]propanamido]-4-(methylsulfanyl)butanamido]acetamido}-3-(1h-indol-3-yl)propanamido]-4-(methylsulfanyl)butanamido]-3-{[(1s)-1-carbamoyl-2-phenylethyl]ca
chembl1121 ,
bdbm21147
h-asp-tyr(so3h)-met-gly-trp-met-asp-phe-nh2
NCGC00167273-01
cholecystokinin pancreozymin c terminal octapeptide
op-cck
cholecystokinin pancreozymin c-terminal octapeptide
cholecystokinin octapeptide
cck-op
sq19844
sq-19844
pancreozymin
CHEBI:135946
cck c-terminal octapeptide
cholecystokinin c-terminal octapeptide
cholecystokinin 8
tox21_112955
tox21_113481
dtxsid7048617 ,
dtxcid4028543
cas-25126-32-3
unii-m03giq7z6p
human cck-8
sincalidum
sincalide [usan:usp:inn:ban]
m03giq7z6p ,
sincalida
AKOS016340423
SCHEMBL122365
HS-2026
cck octapeptide, sulfated
cholecystokinin octapeptide, sulfated
sincalide [usan]
sincalide [usp impurity]
sincalide [vandf]
sincalide [mart.]
sincalide [who-dd]
l-.alpha.-aspartyl-o-sulfo-l-tyrosyl-l-methionylglycyl-l-tryptophyl-l-methionyl-l-.alpha.-aspartyl-l-phenylalaninamide
sincalide [mi]
sincalide [inn]
cholecystokinin c-terminal octapeptide [mi]
sincalide [orange book]
mfcd00079849
DB09142
HY-P0093
(3s,6s,9s,15s,18s,21s)-9-((1h-indol-3-yl)methyl)-21-amino-3-(((s)-1-amino-1-oxo-3-phenylpropan-2-yl)carbamoyl)-6,15-bis(2-(methylthio)ethyl)-5,8,11,14,17,20-hexaoxo-18-(4-(sulfooxy)benzyl)-4,7,10,13,16,19-hexaazatricosane-1,23-dioic acid
CS-5963
(3s,6s,9s,15s,18s,21s)-9-((1h-indol-3-yl)methyl)-21-amino-3-((s)-1-amino-1-oxo-3-phenylpropan-2-ylcarbamoyl)-6,15-bis(2-(methylthio)ethyl)-5,8,11,14,17,20-hexaoxo-18-(4-(sulfooxy)benzyl)-4,7,10,13,16,19-hexaazatricosane-1,23-dioic acid
IZTQOLKUZKXIRV-YRVFCXMDSA-N
(3s,6s,9s,15s,18s,21s)-9-((1h-indol-3-yl)methyl)-21-amino-3-(((s)-1-amino-1-oxo-3-phenylpropan-2-yl)carbamoyl)-6,15-bis(2-(methylthio)ethyl)-5,8,11,14,17,20-hexaoxo-18-(4-(sulfooxy)benzyl)-4,7,10,13,16,19-hexaazatricosanedioic acid
asp26-tyr(so3h)-met-gly-trp-met-asp-phenh2
cholecystokinin, cck octapeptide (26-33)
Q7521885
coralynechloridehydrate,98+%
3-10-caerulein, 5-l-methionine-
sq19844cholecystokinin octapeptide
E78048
(3s)-3-[(2s)-2-[(2s)-2-{2-[(2s)-2-[(2s)-2-[(2s)-2-amino-3-carboxypropanamido]-3-[4-(sulfooxy)phenyl]propanamido]-4-(methylsulfanyl)butanamido]acetamido}-3-(1h-indol-3-yl)propanamido]-4-(methylsulfanyl)butanamido]-3-{[(1s)-1-carbamoyl-2-phenylethyl]carbamo
EN300-19650945
sincalide (usp impurity)
sincalide (usan:usp:inn:ban)
l-aspartyl-l-tyrosyl-l-methionylglycyl-l-tryptophyl-l-methionyl-l-aspartylphenyl-l-alaninamide hydrogen sulfate(ester)
sincalidum (inn-latin)
v04cc03
sincalida (inn-spanish)
sincalide (mart.)
EX-A8006C

Research Excerpts

Overview

Sincalide is a peptide hormone product administered parenterally as an aid for diagnostic imaging of hepatobiliary conditions. It is a rapid-acting, synthetic analog of cholecystokinin.

ExcerptReferenceRelevance
"Sincalide is a peptide hormone product administered parenterally as an aid for diagnostic imaging of hepatobiliary conditions."( Chemical Stability of Reconstituted Sincalide in Sterile Water Under 2 Different Storage Conditions.
Belanger, E; Christoff, J; Rojeab, Y; Wolf, SM; Zatt, SA, 2020
)
1.55
"Sincalide (CCK-8) is an antiopioid substance. "( Protein c-fos induction in rat brain and spinal dorsal horn by sincalide and opioids in vitro.
Chen, SZ; Han, JS, 1994
)
1.97
"Sincalide is a rapid-acting, synthetic analog of cholecystokinin for intravenous use in postevacuation cholecystography. "( Kinevac (sincalide for injection)/Squibb Diagnostics.
Maher, KA, 1991
)
2.14

Treatment

ExcerptReferenceRelevance
"Sincalide pretreatment, when administered at the physiologic rate, is helpful in conditions in which functional resistance to tracer flow into the gallbladder are present."( Pharmacologic intervention for the diagnosis of acute cholecystitis: cholecystokinin pretreatment or morphine, or both?
Kim, CK, 1997
)
1.02

Toxicity

ExcerptReferenceRelevance
" CR-1409 completely abolished the adverse effects of hydrocortisone on pancreatitis."( Involvement of cholecystokinin receptors in the adverse effect of glucocorticoids on diet-induced necrotizing pancreatitis.
Gomez, G; Green, D; Rajaraman, S; Thompson, JC; Townsend, CM; Uchida, T, 1989
)
0.28
" However, dantrolene dose-dependently blocked the toxicity in the recipient culture, suggesting that the release of intracellular stores of calcium is involved in the toxic effect."( Trauma-induced neurotoxicity in rat hippocampal neurons.
Broder, LD; Brooker, RW; Delisle, RK; Mitchell, HL; Yoon, KW, 1996
)
0.29
" These data suggest a mechanism of action for Mel, inhibition of assembly of toxic polymers and protection of neurons from their effect."( Effect of melatonin on α-synuclein self-assembly and cytotoxicity.
Ikeda, T; Mochizuki, H; Nihira, T; Ono, K; Takasaki, J; Teplow, DB; Yamada, M, 2012
)
0.38

Pharmacokinetics

ExcerptReferenceRelevance
" The aim of this study was to compare the in vivo half-life and metabolism of CCK-58 with that of synthetic CCK-8."( Comparison of clearance and metabolism of infused cholecystokinins 8 and 58 in dogs.
Bünte, RH; Eberlein, GA; Eysselein, VE; Goebell, H; Grandt, D; Hoffmann, P; Reeve, JR, 1993
)
0.29
" The peptides were given to 12 dogs as an intravenous (IV) bolus injection to determine the half-life of circulating CCK."( Comparison of clearance and metabolism of infused cholecystokinins 8 and 58 in dogs.
Bünte, RH; Eberlein, GA; Eysselein, VE; Goebell, H; Grandt, D; Hoffmann, P; Reeve, JR, 1993
)
0.29
"The longer half-life of CCK-58 compared with CCK-8 and the minimal conversion into smaller forms during constant IV infusion are consistent with the finding that CCK-58 is not only the major stored form but also the circulating form of CCK after endogenous stimulation in dogs."( Comparison of clearance and metabolism of infused cholecystokinins 8 and 58 in dogs.
Bünte, RH; Eberlein, GA; Eysselein, VE; Goebell, H; Grandt, D; Hoffmann, P; Reeve, JR, 1993
)
0.29

Compound-Compound Interactions

ExcerptReferenceRelevance
" For this purpose Diamidino yellow (DY) injection into the oculomotor nerve was combined with Fast blue (FB) injection either into the extraocular muscles (EOMs), or the cornea, or the superior eyelid."( Peripheral territory and neuropeptides of the trigeminal ganglion neurons centrally projecting through the oculomotor nerve demonstrated by fluorescent retrograde double-labeling combined with immunocytochemistry.
Barazzoni, AM; Bortolami, R; Callegari, E; Calzà, L; Giardino, L; Lalatta Costerbosa, G; Lucchi, ML; Manni, E; Pettorossi, VE, 1991
)
0.28
" When combined with ultrasound imaging, modern biliary scintigraphy can (a) provide excellent discrimination between intrahepatic and extrahepatic cholestasis and (b) help determine the need for subsequent invasive diagnostic studies in selected patients."( Intrahepatic versus extrahepatic cholestasis. Discrimination with biliary scintigraphy combined with ultrasound.
Krishnamurthy, GT; Lieberman, DA, 1986
)
0.27
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
0.38
" Therefore, we hypothesize that prepared phosphatidylserine (PS)-modified microbubbles (PS-MBs) combined with ultrasound-targeted microbubble destruction (UTMD) can safely open the blood-brain barrier (BBB) and target activated microglia for inflammatory area in the later stage of ischemia reperfusion."( Phosphatidylserine-microbubble targeting-activated microglia/macrophage in inflammation combined with ultrasound for breaking through the blood-brain barrier.
Chen, M; Jiang, J; Li, H; Liang, X; Liu, R; Sun, S; Wang, S; Zhao, R, 2018
)
0.48
"PS-MBs combined with ultrasound (US) exposure could safely open BBB, and the resulting PS nanoparticles (PS-NPs) could further target activated M/M in the neuroinflammation."( Phosphatidylserine-microbubble targeting-activated microglia/macrophage in inflammation combined with ultrasound for breaking through the blood-brain barrier.
Chen, M; Jiang, J; Li, H; Liang, X; Liu, R; Sun, S; Wang, S; Zhao, R, 2018
)
0.48
" This study aimed to explore the in vitro and in vivo efficiency of histone deacetylase (HDAC) inhibitor panobinostat (PANO) in combination with mTOR inhibitor rapamycin (RAPA) against TNBC."( Histone deacetylase inhibitor panobinostat in combination with rapamycin confers enhanced efficacy against triple-negative breast cancer.
Chen, L; Chen, X; Kong, L; Lin, J; Mo, C; Wu, K; Xu, S; Zhang, H; Zhou, L, 2022
)
0.72

Bioavailability

ExcerptReferenceRelevance
" Together these results demonstrate that CCK analogues with increased in vivo bioavailability can affect food intake beyond a single meal."( Potent and sustained satiety actions of a cholecystokinin octapeptide analogue.
Ameglio, PJ; Lombard, MA; McHugh, PR; Moran, TH; Sawyer, TK; Seeb, DH, 1992
)
0.28
" (3R)-N-[1-[(tert-butylcarbonyl)methyl]-2,3-dihydro-2-oxo-5-(2-pyri dyl) -1H-1,4-benzodiazepin-3-yl]-N'-[3-(methylamino)phenyl]urea, 15c (YF476), and (3R)-N-[1-[(tert-Butylcarbonyl)methyl]-2,3-dihydro-2-oxo-5- (2-pyridyl)-1H-1,4-benzodiazepin-3-yl]-N'-[3-(dimethylamino)phenyl ]urea hydrochloride, 15d, showed potent dose-dependent effects in both models with the former showing excellent oral bioavailability and an ED50 of 21nmol/kg po in dogs."( (3R)-N-(1-(tert-butylcarbonylmethyl)-2,3-dihydro-2-oxo-5-(2-pyridyl)-1H-1,4-benzodiazepin-3-yl)-N'-(3-(methylamino)phenyl)urea (YF476): a potent and orally active gastrin/CCK-B antagonist.
Akuzawa, S; Batt, AR; Kendrick, DA; Miyata, K; Nishida, A; Ohta, M; Rooker, DP; Ryder, H; Satoh, M; Semple, G; Szelke, M, 1997
)
0.3
" Oral administration of compounds 14a and 15a also produced a lasting antagonism to the hypomotility induced by CCK-8 in mice, suggesting a good bioavailability and metabolic stability."( 5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.
Ballaz, S; Bartolomé-Nebreda, JM; Cenarruzabeitia, E; Del Río, J; García-López, MT; Gómez-Monterrey, I; González-Muñiz, R; Herranz, R; LaTorre, M; Martín-Martínez, M, 1999
)
0.3
"Supramolecular aggregates obtained by self-aggregation of five new cationic amphiphilic CCK8 peptides have been obtained in water solution and characterized for: (i) aggregate structure and stability; (ii) CCK8 peptide conformation and bioavailability on the external aggregate surface; and (iii) for their cell binding properties."( Amphiphilic CCK peptides assembled in supramolecular aggregates: structural investigations and in vitro studies.
Accardo, A; Morelli, G; Morisco, A; Palladino, P; Palumbo, R; Tesauro, D, 2011
)
0.37
", ip) indicate that the liver is the primary site of biotransformation of the compound, suggesting that both 22a and its metabolite(s) are active, compensating probably low bioavailability of the parent molecule."( Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Bednarski, M; Gunia-Krzyżak, A; Marona, H; Nitek, W; Pękala, E; Powroźnik, B; Słoczyńska, K; Walczak, M; Waszkielewicz, AM; Żesławska, E, 2016
)
0.43
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51
" A prodrug of EGCG (pro-EGCG) enhances the bioavailability of EGCG."( A prodrug of epigallocatechin-3-gallate alleviates high glucose-induced pro-angiogenic factor production by inhibiting the ROS/TXNIP/NLRP3 inflammasome axis in retinal Müller cells.
Du, J; Guo, Y; Liu, X; Qin, X; Song, E; Sun, X; Tu, Y; Wang, L; Wang, Y; Xu, X; Zhu, M, 2020
)
0.56

Dosage Studied

ExcerptRelevanceReference
" All these antagonists caused a concentration-dependent rightward shift of the dose-response curve for carbachol-stimulated amylase release without altering the maximal response."( Characterization of muscarinic receptor subtypes on rat pancreatic acini: pharmacological identification by secretory responses and binding studies.
Kashima, K; Kataoka, K; Kato, M; Kuriyama, K; Ohkuma, S, 1992
)
0.28
" In permeabilized acini, mepacrine shifted the dose-response curve for calcium to the right by a factor 2 and inhibited the release of amylase stimulated by GTPrS."( Inhibition by mepacrine and amylase secretion from intact and permeabilized rat pancreatic acini.
Dehaye, JP; Gomez, F; Grosfils, K, 1992
)
0.28
" Similarly, dose-response curves for pepsinogen secretion and the increase in membrane-associated PKC activity induced by a membrane-permeant DAG (1-oleoyl-2-acetylglycerol) were superimposable."( Cellular distribution of gastric chief cell protein kinase C activity: differential effects of diacylglycerol, phorbol esters, carbachol, and cholecystokinin.
Raffaniello, RD; Raufman, JP, 1992
)
0.28
" Both antagonists caused a rightward shift of the dose-response curve for CCK-8s on the monkey iris sphincter."( Cholecystokinin contracts isolated human and monkey iris sphincters; a study with CCK receptor antagonists.
Almegård, B; Bill, A; Stjernschantz, J, 1992
)
0.28
"h-1) shifted the dose-response curve to bethanechol (1-32 mg."( Effects of atropine on pancreatic response to bethanechol, cholecystokinin, and food intake in rats.
O'Rourke, MF; Reidelberger, RD; Solomon, TE, 1991
)
0.28
" Therefore, we determined in isolated pancreatic acini from 3 month ethanol-fed rats and controls the dose-response effects of secretagogues on enzyme secretion, both in the presence and absence of ethanol in the incubation medium."( Differing effects of ethanol on in vitro stimulated pancreatic enzyme secretion in ethanol-fed and control rats.
Pandol, SJ; Schmidt, DN, 1990
)
0.28
"5 mg/kg) shifted the dose-response curve to CCK-8 (25-3,200 pmol."( Effect of CCK antagonist L 364718 on meal-induced pancreatic secretion in rats.
O'Rourke, MF; Reidelberger, RD; Solomon, TE, 1990
)
0.28
" The dose-response of pancreatic enzyme secretion to PACAP 38 was nearly identical with that to VIP."( The stimulatory effect of PACAP 38 on amylase release in dispersed rat pancreatic acini.
Kashimura, J; Kikuchi, Y; Koizumi, M; Shimosegawa, T; Toyota, T, 1991
)
0.28
" The downward shift of the dose-response relation for these secretagogs in the acini of obese rats was analogous to that in streptozotocin-induced diabetic rats, cold-exposed rats, or lactating rats, as demonstrated previously."( Characterization of secretory responses in exocrine pancreas of genetically obese Zucker rats.
Habara, Y; Kanno, T; Namiki, M; Takasugi, Y; Uehara, A,
)
0.13
" The depressive effects induced by the mu agonist PL017 (5 micrograms), delta agonist DADLE (25 micrograms) and kappa agonist 66A-078 (1 microgram) were antagonized by CCK-8 within a dosage of 10 micrograms in a dose dependent manner."( [Cholecystokinin-octapeptide antagonizes the central depressive effect of opioid peptides in rats].
Han, JS; Mei, L, 1991
)
0.28
" The dose-response curve of the antagonistic action was bell-shaped."( A cholecystokinin agonist/antagonist according to dose and time of action: effect on food intake.
Cohen, Y; Gourch, A; Jacquot, C; Martinez, J; Orosco, M; Rodriguez, M, 1990
)
0.28
" Two types of experiments were performed in dogs with pancreatic fistulas: first, secretagogue interactions were examined by studying the effect of intraduodenal GGA (8 mg/kg) or its carrier (control) on the dose-response curves to exogenous secretin and cholecystokinin octapeptide (CCK-8); second, the effect of graded doses of intraduodenal GGA on pancreatic bicarbonate and plasma secretin-like immunoreactivity (SLI) responses was tested directly."( Geranyl-geranyl acetone: a novel stimulant of secretin release in the dog.
Chey, WY; Debas, HT; Goto, Y; Pappas, TN, 1990
)
0.28
" Atropine or tetrodotoxin (TTX) caused a similar rightward shift of the CCK-8 dose-response curve for stimulation of SO contraction."( Characterization of cholecystokinin receptors on the sphincter of Oddi.
Cox, KL; Gardner, JD; Jensen, RT; Moran, TH; von Schrenck, T, 1990
)
0.28
" CR 1409 caused a rightward and parallel shift in the dose-response curve of CCK-8-stimulated pancreatic protein secretion in anesthetized rats, demonstrating a competitive mechanism of inhibition."( The effect of CR 1409, a potent CCK receptor antagonist, on basal and stimulated pancreatic secretion in rat.
Nagy, I; Pap, A; Takács, T; Varró, V, 1990
)
0.28
" CLN and CCK-8 was found to have a complex effect on the acetylcholine and choline contents depending on the brain region, dosage and treatment time."( Effects of caerulein and cholecystokinin-octapeptide on acetylcholine and choline contents in the brains of intact and vagotomized mice.
Miyate, H, 1990
)
0.28
" Schild analysis of the CCK dose-response curve indicates that L-364,718 and CR1409 exert their inhibitory effects on CCK-8-stimulated chief cell responses in a competitive manner."( Effects of CCK-receptor antagonists on CCK-stimulated pepsinogen secretion and calcium increase in isolated guinea pig gastric chief cells.
Konda, Y; Matozaki, T; Nagao, M; Nakano, O; Nishisaki, H; Sakamoto, C, 1990
)
0.28
" The gallbladder emptied in a dose-response manner to the intravenous administration of the octapeptide of cholecystokinin (CCK-OP)."( Feline cholescintigraphy. Studies on role of cholecystokinin in regulation of gallbladder function.
Fisher, RS; Krevsky, B; Maurer, AH; Niewiarowski, T, 1990
)
0.28
" The dose-response curves to Ca2+ ionophore for amylase release were similarly shaped in both groups."( Effect of obstructive jaundice on amylase secretion in rat pancreatic acini.
Fukumoto, T; Iwamoto, Y; Kanazawa, K; Kasahara, K; Kashii, A; Miyata, M; Tenmoku, S, 1985
)
0.27
" We compared the dose-response effects of CCK octapeptide (CCK-8) on feeding, sham feeding, and pancreatic secretion to gauge whether the feeding effect might be physiological."( Comparative effects of CCK-8 on feeding, sham feeding, and exocrine pancreatic secretion in rats.
Reidelberger, RD; Solomon, TE, 1986
)
0.27
" In the presence of TMB-8 the dose-response curve for carbachol-induced amylase release shifts to the right, suggesting competitive antagonism at the muscarinic receptor."( Stimulatory and inhibitory effects of TMB-8 on pancreatic enzyme secretion.
De Pont, JJ; Van Nooij, IG; Willems, PH, 1986
)
0.27
" ICT showed the greatest response to CCK-8 with a maximal concentration 30 times above basal levels resulting in the steepest slope of the dose-response curve."( Effects of cholecystokinin, food intake and cephalic stimuli on plasma levels of amylase, lipase, and immunoreactive cationic trypsinogen in rats.
Delgado, G; Largman, C; Reidelberger, RD; Tsukamoto, H, 1986
)
0.27
" Biphasic dose-response curves to cholecystokinin for amylase release shifted to the right with an increase in the concentration of the drug."( CR-1409: a potent inhibitor of cholecystokinin-stimulated amylase release and cholecystokinin binding in rat pancreatic acini.
Iwamoto, Y; Kuzuya, T; Yamamoto, R, 1987
)
0.27
" In the isolated acini, pirenzepine did not have any significant effect on cholecystokinin-induced amylase release but caused an inhibition of amylase secretion initiated by secretin and shifted the dose-response curve for amylase secretion to the right."( Inhibitory effects of pirenzepine on cholecystokinin and secretin stimulation on exocrine and endocrine rat pancreas.
Baba, S; Fujii, M; Nakamura, T; Oka, T; Okabayashi, Y; Otsuki, M; Tani, S, 1987
)
0.27
" Dose-response curves for CCK-8- or CCh-stimulated amylase release in TPA-pretreated acini revealed attenuation of both maximal efficacy and sensitivity."( Downregulation of protein kinase C in guinea pig pancreatic acini: effects on secretion.
Hootman, SR; Kuroiwa, C; Stuenkel, EL; Sung, CK; Williams, JA, 1988
)
0.27
" L364,718 (3-100 nM), proglumide (1-10 mM), and the proglumide derivative CR1409 (1-30 microM) each caused a progressive rightward shift in the CCK-8 dose-response curve without a change in maximal amylase secretion."( Characterization of a new CCK antagonist, L364,718: in vitro and in vivo studies.
Liang, JP; Louie, DS; Owyang, C, 1988
)
0.27
" Evaluation of time courses and dose-response curves indicated that carbachol, CCK-OP, bombesin, and substance P cause extracellular Ca2+-independent transient increases in [Ca2+]i and transient bursts in amylase release (initial secretion)."( Free cytosolic calcium and secretagogue-stimulated initial pancreatic exocrine secretion.
Krims, PE; Pandol, SJ, 1988
)
0.27
" With substance P, bombesin and cholecystokinin, [DPro4,DTrp7,9,10]substance P-4-11 caused a parallel rightward shift in the dose-response curve for stimulation of amylase secretion with no change in the maximal response."( An analogue of substance P with broad receptor antagonist activity.
Gardner, JD; Jensen, RT; Mantey, S; Zhang, L, 1988
)
0.27
"When pancreatic acini are incubated with increasing concentrations of cholecystokinin octapeptide (CCK-8) the dose-response curve for stimulation of enzyme secretion increases, reaches a maximum and then decreases."( CCK-JMV-180: a peptide that distinguishes high-affinity cholecystokinin receptors from low-affinity cholecystokinin receptors.
Gardner, JD; Jensen, RT; Martinez, J; Sharp, CM; Stark, HA; Sutliff, VE, 1989
)
0.28
" CCK8-stimulated amylase secretion showed a typical biphasic dose-response curve in acini from both adrenalectomized and sham-operated animals with similar basal secretions, similar sensitivities to various CCK8 concentrations, but a statistically significant elevation of maximal amylase secretion after adrenalectomy."( Influence of adrenalectomy on pancreatic enzyme secretion.
Böhm, S; Mössner, J; Stieber, S, 1988
)
0.27
" The dose-response curve for CCK-8-induced inhibition of binding of 125I-[Tyr4]BN appears to to reflect occupation of low-affinity CCK receptors by CCK-8."( Regulation of bombesin receptors on pancreatic acini by cholecystokinin.
Gardner, JD; Jensen, RT; Vinayek, R; Wank, SA; Younes, M, 1989
)
0.28
" Loxiglumide caused a concentration-dependent rightward shift of the dose-response curve for CCK-8-stimulated amylase release without altering the maximal response."( [Inhibitory effect of a new proglumide derivative, loxiglumide, on CCK action in isolated rat pancreatic acini].
Baba, S; Fujii, M; Fujisawa, T; Koide, M; Nakamura, T; Okabayashi, Y; Otsuki, M; Tani, S, 1989
)
0.28
" Complete dose-response studies (10(-11)-10(-3) M) in the presence of bombesin, CCK-8 and carbachol revealed that dopamine does not affect amylase release in response to these secretagogues."( Effect of dopamine on amylase secretion from guinea pig pancreatic acinar cells in vitro.
Hernandez, DE; Xue, BG, 1989
)
0.28
" Comparison of the dose-response curve for calcium mobilization and amylase release stimulated by CCK-8 or CCK-JMV-180 indicates that very low concentrations of each peptide stimulate amylase release without causing detectable calcium mobilization."( Receptor occupation, calcium mobilization, and amylase release in pancreatic acini: effect of CCK-JMV-180.
Beaven, MA; Gardner, JD; Jensen, RT; Martinez, J; Sato, S; Stark, HA, 1989
)
0.28
" In the isolated acini, CR 1392 caused a parallel rightward shift of the dose-response curve for amylase secretion stimulated by cholecystokinin octapeptide (CCK-8)."( Effects of a new proglumide analogue CR 1392 on pancreatic exocrine secretion in the rat.
Baba, S; Fujii, M; Fujisawa, T; Koide, M; Nakamura, T; Okabayashi, Y; Otsuki, M; Tani, S, 1989
)
0.28
" As a result, the dose-response curve shifted upwards."( Augmentation of secretagogue-induced amylase secretion in pancreatic acini of heat-exposed rats.
Habara, Y, 1989
)
0.28
"03 mg/kg) caused a parallel, rightward shift in the dose-response curve to CCK-8 [1-128 nmol/kg, half-maximal effective dose (ED50) increased 16-fold] but did not alter the maximal response, consistent with competitive-like kinetics."( Potent cholecystokinin antagonist L 364718 stimulates food intake in rats.
O'Rourke, MF; Reidelberger, RD, 1989
)
0.28
" In acini from cold-exposed rats, amylase release in response to cholecystokinin octapeptide or carbamylcholine was simultaneously reduced when expressed relative to acinar DNA or protein concentration and the dose-response curve shifted downward."( Suppression of secretagogue-induced amylase secretion in pancreatic acini of cold-exposed rats.
Habara, Y, 1989
)
0.28
" The ED50's and slopes of the dose-response curves in the steroid and cyclic nucleotide ELISAs are compared with those parameters obtained earlier by RIA using the same antisera."( A competitive enzyme-linked immunosorbent assay: applications in the assay of peptides, steroids, and cyclic nucleotides.
Kingan, TG, 1989
)
0.28
" As in experiment 1, CCK produced "biphasic" dose-response effects with strong attenuation that persisted throughout the entire 60-min test at both high (1 microgram) and low (1 ng) doses."( CCK-8 injected into the nucleus accumbens attenuates the supersensitive locomotor response to apomorphine in 6-OHDA and chronic-neuroleptic treated rats.
Ettenberg, A; Koob, GF; Weiss, F, 1989
)
0.28
" The dose-response relationships for somatostatin release and inhibition of aminopyrine uptake were similar."( Inhibition of acid formation and stimulation of somatostatin release by cholecystokinin-related peptides in rabbit gastric glands.
Bengtsson, P; Lundqvist, G; Nilsson, G, 1989
)
0.28
" Dose-response curves for inositol phospholipid synthesis stimulated by carbachol and CCK-8 in mouse acini were biphasic and superimposable with those of amylase secretion."( The effects of gamma-hexachlorocyclohexane on amylase secretion and inositol phospholipid metabolism in mouse pancreatic acini.
Crouch, MF; Roberts, ML, 1985
)
0.27
"Lys-Trp-Nle-Asp-Phe-NH2) was ineffective to modify the self-stimulation behaviour when administered alone while a 150 pmol BC-197 dosage was able to antagonize the decreasing effect of 150 pmol CCK-8 on ICSS."( Similar potencies of CCK-8 and its analogue BOC(Nle28;Nle31)CCK27-33 on the self-stimulation behaviour both are antagonized by a newly synthesized cyclic CCK analogue.
De Witte, P; Heidbreder, C; Roques, BP,
)
0.13
" Dose-response curves to CCK-8 and BN were generated for each tissue."( In vitro response of rat gastrointestinal segments to cholecystokinin and bombesin.
Margolis, RL; McHugh, PR; Moran, TH,
)
0.13
" Close correlation between the decrease in gall bladder volume and the dosage of CCK or the increments in plasma CCK-bioactivity was observed."( CCK receptor antagonism by loxiglumide and gall bladder contractions in response to cholecystokinin, sham feeding and ordinary feeding in man.
Bogdal, J; Konturek, JW; Konturek, SJ; Kurek, A; Oleksy, J; Rovati, L, 1989
)
0.28
" Neither GE 410 nor dbcGMP affected the ACH and histamine (His) response of the muscle strips but both antagonists shifted the dose-response curve of CCK 7 to the right, GE 410 (cholecystokinin antagonist) being a much more potent antagonist of CCK 7 as compared to dbcGMP."( Responses of guinea-pig gastric, ileal and gall bladder smooth muscle to desamino-cholecystokinin-octapeptide (CCK 7).
Henklein, P; Milenov, K; Nieber, K; Oehme, P; Rakovska, A, 1988
)
0.27
" In chronic pancreatic fistula dogs, dose-response studies were performed to determine the effect of proglumide on the pancreatic responses to octapeptide of CCK (CCK-OP), intravenous bethanechol, intraduodenal amino acids, and intraduodenal fat."( Role of cholecystokinin in pancreatic exocrine response to intraluminal amino acids and fat.
Stabile, BE; Stubbs, RS, 1985
)
0.27
" The dose-response curves for CCK8 were shifted in parallel to the right by 10(-6) to 10(-5) M of the three benzodiazepines, although the maximum response to CCK8 was depressed by higher concentrations."( Cholecystokinin antagonism by benzodiazepines in the contractile response of the isolated guinea-pig gallbladder.
Kubota, K; Matsuda, I; Sugaya, K; Sunagane, N; Uruno, T, 1985
)
0.27
" Somatostatin, administered at a dosage of 7 micrograms/kg X h, prevented the gallbladder emptying responses to both test meals, sham feeding, and bethanechol."( Effects of somatostatin on gallbladder emptying.
Fisher, RS; Levin, G; Malmud, L; Rock, E, 1987
)
0.27
" The dose-response curve for glucose on insulin secretion was shifted to the left by 10 nM CCK8; the EC50 of glucose was 11."( Cholecystokinin (CCK8) regulates glucagon, insulin, and somatostatin secretion from isolated rat pancreatic islets: interaction with glucose.
Ammon, HP; Verspohl, EJ, 1987
)
0.27
" Dose-response quantitative generalization was obtained by using 1 and 2 micrograms/kg caerulein."( Neuroleptic-like properties of cholecystokinin analogs: distinctive mechanisms underlying similar behavioral profiles depending on the route of administration.
De Witte, P; Gewiss, M; Roques, B; Vanderhaeghen, JJ,
)
0.13
" Proglumide shifted the dose-response curves of the inhibitory as well as excitatory effects of CCK analogues to the right."( Structure-activity relationship of subtypes of cholecystokinin receptors in the cat lower esophageal sphincter.
Goyal, RK; Rattan, S, 1986
)
0.27
" The dose-response curves for 45Ca uptake and release were identical to those of the hormonally evoked [Ca2+]i increase."( Agonist-sensitive calcium pool in the pancreatic acinar cell. I. Permeability properties.
Fimmel, CJ; Muallem, S; Pandol, SJ; Schoeffield, MS, 1988
)
0.27
" A U-shaped dose-response relationship was observed for the ability of CCK-8-S to attenuate (by approximately 50%, at most) morphine-induced tail flick analgesia."( Antagonism of morphine analgesia by CCK-8-S does not extend to all assays nor all opiate analgesics.
Barbaz, BS; Hall, NR; Liebman, JM,
)
0.13
" Atropine or tetrodotoxin significantly reduced CCK-8-evoked initial phasic contraction and produced a rightward shift of the dose-response curve for CCK-8 (10(-10)-3 x 10(-7) M)."( Effects of cholecystokinin octapeptide on contractile motility of guinea pig common bile duct.
Kantoh, M; Kusunoki, M; Takahashi, T; Utsunomiya, J; Yamamura, T, 1988
)
0.27
" A dose-response curve was obtained, with the 10 ng/kg/min dose producing serum levels of 725 pg/ml."( Peptide YY inhibits cholecystokinin-stimulated sphincter of Oddi activity in the prairie dog.
Couse, NF; Grace, PA; Pitt, HA; Taylor, IL, 1988
)
0.27
" The dose-response relationship for female mice, however, was not linear: lean females failed to suppress food intake following 4 or 8 micrograms/kg and obese females did not suppress food intake at 4 micrograms/kg."( A sex difference in the effect of CCK-8 on food and water intake in obese (ob/ob) and lean (+/+) mice.
Smith, GP; Strohmayer, AJ,
)
0.13
" The dose-response curve of CCK for pepsinogen secretion was superimposed on that for the binding to its receptors."( Cholecystokinin-stimulated pepsinogen secretion and cholecystokinin receptors on gastric chief cells in guinea pigs.
Adachi, H; Aoki, E; Honda, T; Noguchi, M; Ohnishi, S; Sato, S; Torizuka, K, 1987
)
0.27
" Atropine sulfate (10(-6) M) slightly but significantly reduced CCK-OP (10(-11) M-3 X 10(-7) M) induced contractions and the dose-response curve for CCK-OP was shifted to the right of the muscle strips of the human gallbladders."( Effects of cholecystokinin-octapeptide on the human gallbladder both in vivo and in vitro.
Ishikawa, Y; Kantoh, M; Takahashi, T; Utsunomiya, J; Yamamura, T, 1986
)
0.27
" All the subcellular liver fractions caused an approximately 70% decrease in the CCK-effect, as calculated from dose-response relationships."( Inactivation of cholecystokinin octapeptide by normal and cirrhotic liver in rats.
Berger, Z; Pap, A; Ungi, I; Varró, V, 1986
)
0.27
" At the same concentrations the antagonist shifted to the right in parallel to the dose-response curves for CCK-7 and CCK-8 without decreasing their maximum response."( Suc-Tyr(SE)-Met-Gly-Trp-Met-Asp-beta-phenethylamide(410): a competitive antagonist of cholecystokinin-induced contractions in smooth muscles in vitro.
Henklein, P; Milenov, K; Nieber, K; Oehme, P; Rakovska, A, 1987
)
0.27
" The dose-response curves for acetylcholine- and cholecystokinin-octapeptide-stimulated pyloric muscle contraction were similar for both the obese and the lean rats."( Role of pylorus in mediating cholecystokinin-stimulated satiety in the Zucker rat.
Berk, T; Crochelt, RF; Peikin, SR, 1986
)
0.27
" Dose-response curves were constructed for each agonist in each age group and analyzed with respect to the maximal force developed and the pD2 value (negative logarithm of the dose of agonist which produces a one-half maximal response)."( Development of gallbladder contractility in the guinea pig.
Denehy, CM; Ryan, JR, 1986
)
0.27
"5 ng CCK-8) of cholecystokinin octapeptide (CCK-8) resulted in a 3-fold greater maximal concentration of ICT and an 80% steeper slope of the dose-response curve compared to those of pair-fed control animals."( Increased pancreatic acinar content and secretion of cationic trypsinogen following 30-day continuous ethanol intoxication in rats.
Delgado, G; Deveney, CW; Largman, C; Reidelberger, RD; Sankaran, H; Tsukamoto, H, 1986
)
0.27
" However, no obvious dose-response relationship was observed in either intensity or duration of inhibitory action of ceruletide."( A behavioral pharmacological study on CCK-8 related peptides in mice.
Hagino, Y; Moroji, T, 1986
)
0.27
"The dose-response curves for the anticonvulsive activity of sulfated and nonsulfated cholecystokinin octapeptide (CCK-8-SE and CCK-8-NS) against picrotoxin-induced (6 mg/kg SC) seizures were assessed either following or without pretreatment with a single high dose of CCK-8-SE or CCK-8-NS, to examine acute tolerance to the effect after IP injections in mice."( Multiple treatment potentiates the anticonvulsive activity of cholecystokinin octapeptides.
Kádár, T; Penke, B; Pesti, A; Telegdy, G,
)
0.13
" Dose-response curves were constructed to CCK-8 alone and to VIP alone."( Interactions of vasoactive intestinal polypeptide and cholecystokinin octapeptide on the control of gallbladder contraction.
Debas, HT; Melendez, RL; Pappas, TN; Strah, KM, 1986
)
0.27
" The identity of dose-response profiles of single cells and suspensions of cells, particularly the wide span of the dose-response curves and the low Hill coefficients (0."( Measurement of function in isolated single smooth muscle cells.
Bitar, KN; Makhlouf, GM, 1986
)
0.27
" While CCK-8-S resulted in a linear dose-response effect (0."( Cholecystokinin octapeptides influence tolerance to ethanol in mice.
Kovács, GL; Penke, B; Szabó, G; Telegdy, G, 1985
)
0.27
" Pregnancy was characterized by significant decreases in the magnitude of the contractile responses to acetylcholine and cholecystokinin-octapeptide at each point along their respective dose-response curves."( Effect of pregnancy on gallbladder contractility in the guinea pig.
Ryan, JP, 1984
)
0.27
" Eighteen patients (14 males, 4 females) meeting Research Diagnostic Criteria for schizophrenia had been receiving neuroleptics at a dosage that had not changed for 3 months, and to which the patients were at best only partially responsive."( Cholecystokinin-octapeptide in chronic schizophrenia: a double-blind placebo-controlled study.
Bloom, DM; Debonnel, G; Mosticyan, S; Nair, NP; Schwartz, G, 1984
)
0.27
"Determinations of dose-response curves for synthetic secretin and for the octapeptide of cholecystokinin (CCK-8) in the isolated perfused rat pancreas reveal that both secretin and CCK stimulate the pancreatic secretory flow and enzyme secretion."( The action of synthetic secretin, cholecystokinin-octapeptide and combinations of these hormones on the secretion of the isolated perfused rat pancreas.
Kasper, H; Sommer, H, 1981
)
0.26
" Cycloheximide acted on the steps by which secretagogues mobilize cellular Ca2+ because the dose-response curve for 45Ca2+ efflux was shifted to the same extent as that for amylase release, whereas the dose-response curve for amylase release induced by the Ca2+ ionophore A23187 was not altered."( Protein synthesis inhibitors enhance secretagogue sensitivity of in vitro rat pancreatic acini.
Otsuki, M; Williams, JA, 1982
)
0.26
" The dose-response curves for CCK8 were similarly shaped in both CCK8-treated and control rats, but they were shifted 3- to 10-fold toward higher concentrations of CCK8 after 7 and 14 days of CCK8 treatment."( Amylase secretion by isolated pancreatic acini after chronic cholecystokinin treatment in vivo.
Otsuki, M; Williams, JA, 1983
)
0.27
" IBMX but not Ro 20-1724 caused a parallel rightward shift in the dose-response curve for the stimulation of amylase secretion caused by carbachol."( Effects of inhibitors of cyclic nucleotide phosphodiesterase on actions of cholecystokinin, bombesin, and carbachol on pancreatic acini.
Gardner, JD; Jensen, RT; Sutliff, VE; Walker, MD, 1983
)
0.27
" Dose-response curves of pGRP for amylase release and AIB uptake were found to be biphasic."( Effects of porcine gastrin-releasing peptide on amylase release, 2-deoxyglucose uptake, and alpha-aminoisobutyric acid uptake in mouse pancreatic acini.
Akanuma, Y; Iwamoto, Y; Nakamura, R, 1983
)
0.27
" CCK octapeptide (CCK-8) induced biphasic dose-response curves for stimulation of pancreatic juice and amylase secretion."( Effects of C-terminal fragments of cholecystokinin on exocrine and endocrine secretion from isolated perfused rat pancreas.
Baba, S; Ohki, A; Okabayashi, Y; Otsuki, M; Sakamoto, C, 1983
)
0.27
" Ac-CCK-(26-32) caused a parallel rightward shift in the dose-response curve for CCK-(26-33)-stimulated amylase secretion."( Derivatives of CCK-(26-32) as cholecystokinin receptor antagonists in guinea pig pancreatic acini.
Gardner, JD; Jensen, RT; Knight, M; Sutliff, VE; Tamminga, CA, 1984
)
0.27
" Doses of stimulants were chosen from dose-response experiments to avoid supramaximal amounts which inhibited the pancreatic response."( Secretin-pancreozymin test with synthetic secretin and cholecystokinin octapeptide.
Berger, Z; Pap, A; Varró, V, 1983
)
0.27
" Dose-response curves to CCK for amylase release shifted to the right with increase in proglumide concentration."( In vitro and in vivo effect of proglumide on cholecystokinin-stimulated amylase release in mouse pancreatic acini.
Akanuma, Y; Iwamoto, Y; Nakamura, R, 1984
)
0.27
"The substance P antagonist, [D-Pro4-D- Trp7 ,9,10]substance P4-11, caused a pig parallel shift to the right of the cholecystokinin (CCK-8) dose-response curve in guinea pig ileum longitudinal muscle without changing the maximal contraction."( Further evidence that substance P partly mediates the action of cholecystokinin octapeptide (CCK-8) on the guinea pig ileum but not gall bladder: studies with a substance P antagonist.
Chang, RS; Chen, TB; Lotti, VJ, 1984
)
0.27
" The span of the dose-response curves was wide, suggesting the existence of receptor heterogeneity."( Receptors on smooth muscle cells: characterization by contraction and specific antagonists.
Bitar, KN; Makhlouf, GM, 1982
)
0.26
" The muscle strips were challenged with either acetylcholine or the octapeptide of cholecystokinin and dose-response relationships were determined."( Effect of progesterone pretreatment on guinea pig gallbladder motility in vitro.
Pellecchia, D; Ryan, JP, 1982
)
0.26
" The effect by this route, however, was not behaviorally specific: BBS produced equivalent inhibitions of food and water intake at every point on the dose-response curve, and produced a marked increase in grooming which dominated the behavioral display."( Effects of peripheral and central bombesin on feeding behavior of rats.
Gibbs, J; Kulkosky, PJ; Smith, GP, 1981
)
0.26
" A dose-response study of the competetion of CCK-8 with [3H]-dopamine binding indicates an IC50 for the peptide of 450 nM; desulfated CCK-8 and the related peptide caerulin are at least 4-fold less active than CCK-8."( Modulation of [3H]-dopamine binding by cholecystokinin octapeptide (CCK-8).
Murphy, RB; Schuster, DI,
)
0.13
" Both CCK-8-NS and CCK-8-SE enhanced the latency of passive avoidance after all forms of treatment while showing different dose-response patterns depending on time of administration."( Modulation of passive avoidance behaviour of rats by intracerebroventricular administration of cholecystokinin octapeptide sulfate ester and nonsulfated cholecystokinin octapeptide.
Fekete, M; Kádár, T; Telegdy, G, 1981
)
0.26
" Inhibition by proglumide was competitive and resulted in a parallel rightward shift of the cholecystokinin dose-response curve."( Cholecystokinin-induced contraction of dispersed smooth muscle cells.
Collins, SM; Gardner, JD, 1982
)
0.26
"05), without any significant shift of the normalized dose-response curves."( Defective gallbladder contractility in the ground squirrel and prairie dog during the early stages of cholesterol gallstone formation.
Davison, JS; Fridhandler, TM; Shaffer, EA, 1983
)
0.27
" Tremorolytic potency (ED50) was calculated from dose-response curves."( Cholecystokinin octapeptide (CCK-8), ceruletide and analogues of ceruletide: effects on tremors induced by oxotremorine, harmine and ibogaine. A comparison with prolyl-leucylglycine amide (MIF), anti-Parkinsonian drugs and clonazepam.
Zetler, G, 1983
)
0.27
" Comparison of dose-response curves prepared in each animal indicated that the sensitivity of the cystic duct was significantly lower than that of the gallbladder."( Cholecystokinin constricts the canine cystic duct.
Clanachan, AS; Courtney, DF; Scott, GW, 1983
)
0.27
"To establish the sensitivity of the gallbladder in relation to plasma concentrations of cholecystokinin, a dose-response study was performed in five normal volunteers."( Infusion of cholecystokinin octapeptide in man: relation between plasma cholecystokinin concentrations and gallbladder emptying rates.
Chadwick, VS; FitzPatrick, ML; Maton, PN; Selden, AC, 1984
)
0.27
" Duplicate dose-response experiments using exogenous cholecystokinin (CCK) and intraduodenal amino acids were performed with and without a simultaneous intravenous infusion of mixed amino acids, which simulated postprandial hyperaminoacidemia."( Inhibition of the stimulated exocrine pancreas by absorbed amino acids.
Stabile, BE; Stubbs, RS, 1984
)
0.27
" The dose-response curves for CCK8 were similarly shaped in both CCK8-pretreated and control rats but shifted threefold toward higher concentrations of CCK8 2 or 14 h after CCK8 treatment."( Amylase secretion by isolated pancreatic acini after acute cholecystokinin treatment in vivo.
Baba, S; Hootman, SR; Ohki, A; Okabayashi, Y; Otsuki, M; Williams, JA, 1984
)
0.27
"Verified bilateral abdominal vagotomy (with hepatic branch intact) did not alter the ability of 20% pure cholecystokinin (CCK) or octapeptide of cholecystokinin (CCK-8) to inhibit sham feeding of liquid diet in dose-response studies for male Sprague-Dawley rats with open gastric fistula."( Vagotomy does not alter cholecystokinin's inhibition of sham feeding.
Kraly, FS, 1984
)
0.27
" The antagonism was competitive in nature because LY219,057 caused a parallel rightward shift of the dose-response curve for CCK-8-stimulated amylase secretion without altering the maximal increase."( Characterization of a new diphenylpyrazolidinone cholecystokinin antagonist in vitro isolated rat pancreatic acini.
Akiyama, T; Otsuki, M; Tachibana, I, 1993
)
0.29
" The downward portion of the dose-response curve has been referred to as "high-dose" inhibition."( Novel CCK analogues and bombesin: a detailed analysis between phosphoinositide breakdown and high-dose inhibition of pancreatic enzyme secretion in three rodent species.
Bianchi, BR; Lin, CW; Miller, TR; Witte, DG, 1994
)
0.29
" The dose-response relationship for CCK-induced secretion is bell-shaped, with a characteristic supramaximal inhibition."( Supramaximal inhibition of cholecystokinin-induced pancreatic amylase release involves desensitization to cytoplasmic Ca2+.
Gylfe, E; Nilsson, J; Sjödin, L, 1994
)
0.29
" 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
)
0.29
" In contrast, the dose-response curve for amylase secretion induced by the phorbol ester phorbolmyristate-13-acetate was shifted to the right without a reduction of the maximal secretory response."( Cyclosporine A inhibits protein-kinase-C-mediated amylase release from isolated rat pancreatic acini.
Domagk, KA; Fölsch, UR; Höcker, M; Kern, HF; Schmidt, WE; Schwarzhoff, R; Waschulewski, IH, 1994
)
0.29
" High EGF concentrations shifted the dose-response curve for CCK8-induced amylase release to lower CCK8 concentrations, whereas low EGF concentrations (17 nM) shifted this dose-response curve to higher CCK8 concentrations."( Effect of epidermal growth factor on cholecystokinin-induced amylase release and inositol 1,4,5-trisphosphate production in pancreatic acinar cells.
Caspary, WF; Piiper, A; Stryjek-Kaminska, D; Zeuzem, S, 1993
)
0.29
" The dose-response curve for CCK-8 alone to induce gallbladder contraction was not significantly different from those caused by CCK-8 plus 1 mumol/L tetrodotoxin or 1 mumol/L atropine."( Characterization of cholecystokinin receptors on the human gallbladder.
Coleman, R; Concepcion, W; Cox, KL; Esquivel, CO; Nakazato, P; Tokunaga, Y, 1993
)
0.29
" The present findings support our previous hypothesis that pancreatic acinar cells possess three classes of CCK receptors and suggest that high-affinity CCK receptors do not mediate the action of CCK-8 on enzyme secretion, that low-affinity CCK receptors may mediate the action of CCK on cytosolic calcium that does not involve IP3(1,4,5) and produce the upstroke of the dose-response curve for CCK-8-stimulated amylase secretion and that very low-affinity CCK receptors mediate the actions of CCK on IP3(1,4,5) and cytosolic calcium and produce the downstroke of the dose-response curve for CCK-8-stimulated amylase secretion."( Occupation of low-affinity cholecystokinin (CCK) receptors by CCK activates signal transduction and stimulates amylase secretion in pancreatic acinar cells.
Gardner, JD; Gregory, J; Jensen, RT; Menozzi, D; Mrozinski, JE; Patto, RJ; Vinayek, R, 1993
)
0.29
" The dose-response curve for cell-recruitment coincides with that of the apparent [Ca2+]i increase in a suspension of acinar cells."( Dose-dependent recruitment of pancreatic acinar cells during receptor-mediated calcium mobilization.
De Pont, JJ; Van Emst-De Vries, SE; Van Os, CH; Willems, PH, 1993
)
0.29
" Repetitive [Ca2+]c change is attributable to the upstroke of the bell-shaped dose-response relationship and the biphasic change is responsible for the downstroke of the relation (so called high-dose inhibited secretion)."( Stimulus-secretion coupling and Ca2+ dynamics in pancreatic acinar cells.
Habara, Y; Kanno, T, 1994
)
0.29
" To further evaluate the role of cholecystokinin (CCK) in regulating acid output in humans, dose-response curves were constructed to CCK8 or G17 (6."( Cholecystokinin is a physiological regulator of gastric acid secretion in man.
Aufderhaar, U; Bauerfeind, P; Beglinger, C; Burckhardt, B; Delco, F; Ensinck, JW; Gyr, K; Ketterer, S; Meier, R, 1994
)
0.29
" The antagonism was competitive in nature because these three compounds caused a parallel rightward shift of the dose-response curve for CCK-8-stimulated amylase secretion, without altering the maximal increase."( Characterization of a new cholecystokinin receptor antagonist FK480 in in vitro isolated rat pancreatic acini.
Akiyama, T; Otsuki, M, 1994
)
0.29
" A similar dose-response relationship was seen in carbachol- and CCK-8-induced [Ca2+]i increase and pepsinogen secretion."( Somatostatin inhibits pepsinogen secretion without influencing cytosolic free Ca2+ increase induced by carbachol and cholecystokinin octapeptide in rat chief cells.
Miyadera, K; Tanaka, T; Tani, S, 1993
)
0.29
"The present series of experiments was designed to determine the dose-response characteristics of the cholecystokinin suppression effect on rat pups ingesting through suckling and adult modes."( Effects of CCK-8 on ingestive behaviors of suckling and weanling rats.
Lorenz, DN, 1994
)
0.29
" Dose-response studies indicated the following rank order of potency: Suc-CCK-7 > or = Suc-(Thr28, Leu29, MePhe33)-CCK-7 > or = CCK-8 > or = (Nle28,31)-CCK-8 >> desulfated CCK-8 = CCK-4 = 0 in the case of ip administration and Suc-(Thr28, Leu29, MePhe33)-CCK-7 >> Suc-CCK-7 > or = CCK-8 > or = (Nle28,31)-CCK-8 >> desulfated CCK-8 = CCK-4 = 0 in the case of icv administration."( Cholecystokinin octapeptide analogues suppress food intake via central CCK-A receptors in mice.
Baba, S; Himori, N; Hirosue, Y; Inui, A; Kasuga, M; Miura, M; Nakajima, M; Nakajima, Y; Okita, M; Teranishi, A, 1993
)
0.29
" Both devazepide and L-365,260 showed a bell-shaped dose-response curve."( Increased release of immunoreactive cholecystokinin octapeptide by morphine and potentiation of mu-opioid analgesia by CCKB receptor antagonist L-365,260 in rat spinal cord.
Han, JS; Sun, YH; Zhang, ZW; Zhou, Y, 1993
)
0.29
" CCK-8 caused a half-maximal increase in [3H]IP3 at 2 nM, and the dose-response curve was monophasic, whereas with gastrin the curve was biphasic, with an EC50 of the initial component (20% maximal) at 38 nM and the second component at 10 microM."( Gastrin and CCK activate phospholipase C and stimulate pepsinogen release by interacting with two distinct receptors.
Jensen, RT; Qian, JM; Rowley, WH, 1993
)
0.29
" The ID50S and the slopes of the dose-response functions of the two peptides were not significantly different."( Comparison of the satiating potencies of cholecystokinin-33 and cholecystokinin-8.
Gibbs, J; Melville, LD; Smith, GP, 1993
)
0.29
" In acini prepared from the camostate-treated rats, responsiveness to both CCK-8 and carbamylcholine was greatly decreased with no shift in the dose-response curves compared to control acini prepared from saline-treated rats."( Chronic oral administration of synthetic trypsin inhibitor camostate reduces amylase release from isolated rat pancreatic acini.
Fujii, M; Nakamura, T; Okabayashi, Y; Otsuki, M; Tani, S, 1995
)
0.29
" The relative potencies of SP-related peptides to stimulate pepsinogen secretion and [Ca2+]i demonstrated a close agreement with their abilities to inhibit the binding of 125I-BH-SP, and comparison of the dose-response curves suggests occupation of the low affinity sites mediate changes in biologic activity."( Gastric chief cells possess NK1 receptors which mediate pepsinogen secretion and are regulated by agents that increase cAMP and phospholipase C.
Jensen, RT; Kitsukawa, Y; Pradhan, TK; Turner, RJ, 1996
)
0.29
" Trp inhibited cholecystokinin-octapeptide (CCK-8)-stimulated amylase secretion, causing a downward shift in the dose-response curve."( Tryptophan modulates exocrine secretory function in rat pancreatic acini.
Fujii, M; Hasegawa, H; Kasuga, M; Kido, Y; Koide, M; Matsushita, K; Okabayashi, Y; Okutani, T; Otsuki, M, 1996
)
0.29
" Dose-response curves to cholecystokinin-octapeptide and carbachol were obtained."( Gallbladder motility in vitro in men with gallstones following Billroth II gastric resection.
Caruso, ML; Lorusso, D; Maselli, MA; Pezzolla, F; Piepoli, AL, 1996
)
0.29
" TP-680 caused a parallel rightward shift of the dose-response curve for CCK-8-stimulated amylase release as did MK-329 and loxiglumide."( Pharmacological profile of TP-680, a new cholecystokininA receptor antagonist.
Akiyama, T; Hirohata, Y; Otsuki, M; Shirohara, H; Tachibana, I; Yamamoto, M, 1996
)
0.29
"h-1) evoked a characteristic biphasic dose-response curve for pancreatic juice and protein output in the LETO rats, whereas the OLETF rats were totally insensitive to CCK-8 stimulation."( Defect in pancreatic exocrine and endocrine response to CCK in genetically diabetic OLETF rats.
Akiyama, T; Furumi, K; Kanagawa, K; Otsuki, M; Shiohara, H; Tachibana, I; Watanabe, N, 1996
)
0.29
" infusion of TP-680 in rats caused a parallel rightward shift of the entire dose-response curve for cholecystokinin octapeptide (CCK-8)-stimulated pancreatic exocrine secretion without altering the maximal response (ID50 = 480 nmol/kg)."( Pharmacological profile of a new serine derivative cholecystokinin receptor antagonist TP-680 on pancreatic, biliary and gastric function.
Kanagawa, K; Otsuki, M; Tachibana, I; Yamamoto, Y, 1996
)
0.29
" In the first set, the aim of the experiments was to investigate the dose-response effect of selective serotonin re-uptake inhibitor (SSRI) citalopram on rat exploratory behaviour in the elevated plus-maze."( The effects of cholecystokinin A and B receptor antagonists, devazepide and L 365260, on citalopram-induced decrease of exploratory behaviour in rat.
Allikmets, L; Harro, J; Matto, V, 1996
)
0.29
" The dose-response curves to LCRF-(1-35) and to monitor peptide were similar and biphasic, with higher doses producing submaximal pancreatic secretory responses."( An amino-terminal fragment of LCRF, LCRF-(1-35), has the same activity as the natural peptide.
Green, GM; Guan, D; Liddle, RA; Reeve, JR; Spannagel, AW, 1997
)
0.3
" Dose-response experiments revealed the following potencies for SOM secretion: G-17s = CCK-8s > G-17 ns >> CCK-8ns."( Cholecystokinin (CCK) regulates somatostatin secretion through both the CCK-A and CCK-B/gastrin receptors in sheep.
Shulkes, A; Zavros, Y, 1997
)
0.3
" Short-term (3 min) pretreatment with the PKC activator 12-O-tetradecanoylphorbol 13-acetate (TPA) evoked a rightward shift of the dose-response curve for the Ca2+ mobilizing effect of CCK-8-S in both cell lines."( Protein kinase C-mediated inhibition of transmembrane signalling through CCK(A) and CCK(B) receptors.
De Pont, JJ; Fouraux, MA; Smeets, RL; van Emst-de Vries, SE; Willems, PH, 1998
)
0.3
" The dose-response curves for CCK-8-induced cyclic AMP accumulation and inositol 1,4,5-trisphosphate (Ins(1,4,5)P3) formation were shifted to the left in CHO-CCK(A)MT cells."( Mutational analysis of the potential phosphorylation sites for protein kinase C on the CCK(A) receptor.
De Pont, JJ; Fouraux, MA; Pouwels, W; Ronken, E; Smeets, RL; van Emst-de Vries, SE; Willems, PH, 1998
)
0.3
" Dose-response curves to cholecystokinin-octapeptide and carbachol were first established."( Effect of somatostatin on human gallbladder motility: an in vitro study.
Caruso, ML; Lorusso, D; Maselli, MA; Pezzolla, F; Piepoli, AL, 1999
)
0.3
" TS-941 caused a parallel rightward shift of the entire dose-response curve for CCK-8-stimulated amylase release without altering the maximal increase, as did devazepide and loxiglumide."( Pharmacologic profile of TS-941, a new benzodiazepine derivative cholecystokinin-receptor antagonist, in in vitro isolated rat pancreatic acini.
Akiyama, T; Hirohata, Y; Kihara, Y; Otsuki, M; Tashiro, M, 1999
)
0.3
" In the control group, the step-wise increasing doses of CCK-8 resulted in a characteristic dose-response curve for the pancreatic volume, protein and amylase secretion (maximal volume, protein and amylase output at 600 ng/kg/30 min of CCK-8: 157 +/- 20."( Pancreatic secretory responses in L-arginine-induced pancreatitis: comparison of diabetic and nondiabetic rats.
Czako, L; Hegyi, P; Lonovics, J; Szilvassy, Z; Takacs, T, 1999
)
0.3
" Atropine displaced the dose-response curve for carbamylcholine to the right so that in the presence of 7 microM atropine a concentration of 1 mM carbamylcholine now gave an optimal rate of enzyme secretion."( Morphological changes in rat pancreatic slices associated with inhibition of enzyme secretion by high concentrations of secretagogues.
Savion, N; Selinger, Z, 1978
)
0.26
"Muscle strips from the body and neck of the gallbladder were suspended in organ baths and dose-response curves were constructed for CCK-8 and carbachol."( In vitro responses of gallbladder muscle from patients with acalculous biliary pain.
Ahmed, R; Bird, NC; Chess-Williams, R; Johnson, AG; Thomas, WE, 2000
)
0.31
" We compared cumulative CCK dose-response relationship in control cells and in cells where P450 had been induced by prior injection of animals with beta-naphthoflavone."( Pharmacological evaluation of the role of cytochrome P450 in intracellular calcium signalling in rat pancreatic acinar cells.
Bruce, JI; Elliott, AC, 2000
)
0.31
" Both lorglumide and PD-135,158 induced a significant shift to the left in the morphine dose-response curves as well as a significant decrease in ED50 of the STR."( Stimulation of either cholecystokinin receptor subtype reduces while antagonists potentiate or sensitize a morphine-induced excitatory response.
Cacheiro, RG; Cruz, TN; Felicio, LF; Flório, JC; Mazzini, BK; Nasello, AG, 2001
)
0.31
" The comparison of CCK-8 and JMV-180 dose-response curves of amylase release to those of PtdIns and PtdOH labelling with [(32)P]-Pi showed the existence of an amplification mechanism between phospholipase C and amylase release for both agonists."( The cholecystokinin analogues JMV-180 and CCK-8 stimulate phospholipase C through the same binding site of CCK(A) receptor in rat pancreatic acini.
Claro, E; Ramos, B; Salido, GM; Sarri, E, 2001
)
0.31
" The effect of selective concentrations of CCK(1) and CCK(2) receptor antagonists (L-364,718 and JB93182, respectively) was determined on agonist concentration-effect (E/[A]) curves obtained by cumulative dosing with sulphated CCK."( Pharmacological characterization of cholecystokinin receptors mediating contraction of human gallbladder and ascending colon.
Morton, MF; Shankley, NP; Tavares, IA; Welsh, NJ, 2002
)
0.31
" Baseline tone, electrical field stimulation (EFS)-induced nitric oxide-mediated off responses, and changes in the cholecystokinin (CCK)-8 dose-response relationship were measured."( The effect of phosphodiesterase inhibition on gallbladder motility in vitro.
Conklin, JL; Cullen, JJ; Hinkhouse, MM; Lindaman, BA, 2002
)
0.31
" Caffeine (10(-5) M) and EHNA increased the CCK-8 dose-response contractions."( The effect of phosphodiesterase inhibition on gallbladder motility in vitro.
Conklin, JL; Cullen, JJ; Hinkhouse, MM; Lindaman, BA, 2002
)
0.31
" The dose-response and time-effect curves observed following HWI and sodium arsenite treatments were evaluated."( Induction of HSP72 by sodium arsenite fails to protect against cholecystokinin-octapeptide-induced acute pancreatitis in rats.
Boros, I; Iványi, B; Kaszaki, J; Lonovics, J; Mándi, Y; Rakonczay, Z; Takacs, T, 2002
)
0.31
" The dose-response (5-40 mg/kg) and time-course (6-72 h) curves of methylprednisolone on pancreatic HSP60 and HSP72 synthesis were evaluated following methylprednisolone treatment."( The anti-inflammatory effect of methylprednisolone occurs down-stream of nuclear factor-kappaB DNA binding in acute pancreatitis.
Boros, I; Duda, E; Iványi, B; Kaszaki, J; Lonovics, J; Rakonczay, Z; Takács, T, 2003
)
0.32
" The CCK dose-response curve for TyrP for sites in each kinase was similar."( Phosphospecific site tyrosine phosphorylation of p125FAK and proline-rich kinase 2 is differentially regulated by cholecystokinin receptor type A activation in pancreatic acini.
Bragado, MJ; García-Marin, LJ; Jensen, RT; Pace, A; Tapia, JA, 2003
)
0.32
" After investigating different dosing paradigms, it was found that pulsatile delivery of CCK8S (intravenous infusion for 1 min every 10 min) produced a readily quantifiable contractile response that did not exhibit tachyphylaxis."( A novel, quantitative bio-assay for cholecystokinin type-1 receptor activity in the anaesthetised rat.
Barrett, TD; Freedman, JM; Shankley, NP,
)
0.13
" CCK8 generated a biphasic secretion dose-response curve, and high concentrations increased intracellular active trypsin levels."( Secretagogues differentially activate endoplasmic reticulum stress responses in pancreatic acinar cells.
Kubisch, CH; Logsdon, CD, 2007
)
0.34
" The control group was immunized with same dosage of HSA."( Effects of active immunization against cholecystokinin 8 on performance, contents of serum hormones, and expressions of CCK gene and CCK receptor gene in pigs.
Bing, Y; Chen, D; Chen, X; Ding, X; Yuan, Z; Zhang, K, 2007
)
0.34
" Cholecystokinin-8 stimulation induced a typical biphasic dose-response curve for amylase secretion in acinar cells isolated from both PKC delta(-/-) and wild type mice, with maximal stimulation at 10-pmol/L CCK."( Protein kinase C delta-mediated processes in cholecystokinin-8-stimulated pancreatic acini.
Cheriyan, S; Gorelick, FS; Kolodecik, TR; Lugea, A; Pandol, SJ; Reeve, JR; Thrower, EC; Wang, J; Yuan, J, 2009
)
0.35
" With both strategies, dose-response curves were generated for the natural agonist CCK-8S, the partial agonist JMV-180 as well as the antagonist lorglumide."( Time-resolved quantitative analysis of CCK1 receptor-induced intracellular calcium increase.
De Vos, WH; Smagghe, G; Staljanssens, D; Van Camp, J; Willems, P, 2012
)
0.38
" However, the literature lacks meal pattern analysis and an appropriate dose-response curve for this peptide."( The short term satiety peptide cholecystokinin reduces meal size and prolongs intermeal interval.
Lateef, DM; Sayegh, AI; Washington, MC, 2011
)
0.37
" Both CQ and 3-MA were synergistic with VCR to inhibit the growth of retinoblastoma cells and the combinational use significantly reduced the dosage of each drug."( Low concentrations of chloroquine and 3-methyladenine suppress the viability of retinoblastoma cells synergistically with vincristine independent of autophagy inhibition.
Chen, X; Chen, YH; Jiang, PF; Li, LJ; Li, W; Shen, HQ; Zheng, XY, 2015
)
0.42
"Compared with mono-culture, cell proliferation increased, apoptosis decreased, and DNA damage decreased in a dose-response relationship in co-culture."( Acute cytotoxicity test of PM
Chen, Y; Du, Y; Huang, Z; Liang, L; Liu, J; Liu, Y; Xie, R; Yang, Q; Zhou, J; Zou, H, 2022
)
0.72
"hDPSCs were found to be susceptible to infection by a novel oncolytic adenovirus named YSCH-01 and were capable of transporting this virus to tumor sites at 1000 VP/cell infectious dosage in vitro and in vivo."( Potent antitumor efficacy of human dental pulp stem cells armed with YSCH-01 oncolytic adenovirus.
He, X; Jin, X; Liu, XY; Yao, W; Zhang, KJ; Zhao, SL; Zhu, JD, 2023
)
0.91
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (1)

ClassDescription
oligopeptideA peptide containing a relatively small number of amino acids.
[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 Targets (17)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, Ferritin light chainEquus caballus (horse)Potency5.62345.623417.292931.6228AID485281
estrogen nuclear receptor alphaHomo sapiens (human)Potency17.04080.000229.305416,493.5996AID743075; AID743077; AID743079
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency3.34910.001723.839378.1014AID743083
thyroid hormone receptor beta isoform aHomo sapiens (human)Potency1.41250.010039.53711,122.0200AID1479
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency16.50750.000323.4451159.6830AID743065; AID743066
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Cholecystokinin receptor type AMus musculus (house mouse)Ki0.00030.00030.00030.0003AID52248
Cholecystokinin receptor type ARattus norvegicus (Norway rat)IC50 (µMol)0.00060.00000.43624.3000AID52896; AID52898; AID52899; AID52912; AID52916; AID53031; AID53032; AID53035
Cholecystokinin receptor type ARattus norvegicus (Norway rat)Ki0.00020.00010.27892.8900AID50501; AID50502; AID50506
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)Ki0.00070.00060.11960.6800AID51456; AID51458; AID51461
Cholecystokinin receptor type AHomo sapiens (human)IC50 (µMol)0.00060.00010.30381.9000AID1285622; AID1336315; AID1572001; AID346410; AID52744; AID52746; AID52748; AID52749; AID52750; AID52751; AID52753
Cholecystokinin receptor type AHomo sapiens (human)Ki0.00030.00000.31902.2760AID346410
Gastrin/cholecystokinin type B receptorHomo sapiens (human)IC50 (µMol)0.00100.00010.36154.0000AID1285623; AID1336316; AID1572002; AID346411; AID50690; AID50974; AID50976; AID50977; AID50978; AID51096; AID51097; AID51098
Gastrin/cholecystokinin type B receptorHomo sapiens (human)Ki0.00050.00010.03660.3450AID346411; AID50951; AID50955
Gastrin/cholecystokinin type B receptorMus musculus (house mouse)IC50 (µMol)0.00080.00031.33674.0000AID51105; AID51121
Gastrin/cholecystokinin type B receptorMus musculus (house mouse)Ki0.00030.00030.01660.0940AID52248
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)IC50 (µMol)0.00040.00041.13803.5000AID52438
Cholecystokinin receptor type ACavia porcellus (domestic guinea pig)Ki0.00050.00030.13770.6310AID51623; AID52252; AID52253; AID52254; AID52578; AID52580; AID52581
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
5-hydroxytryptamine receptor 2ARattus norvegicus (Norway rat)EC50 (µMol)0.00010.00010.49294.0000AID50973
Gastrin/cholecystokinin type B receptorRattus norvegicus (Norway rat)EC50 (µMol)0.00060.00040.00080.0014AID51295; AID51296
Cholecystokinin receptor type AHomo sapiens (human)EC50 (µMol)0.01130.00000.05050.2691AID1572003; AID264443; AID52405; AID52743
Cholecystokinin receptor type AHomo sapiens (human)Kd0.00190.00190.00190.0019AID1798047
Gastrin/cholecystokinin type B receptorHomo sapiens (human)EC50 (µMol)0.00910.00000.00850.0270AID1572004; AID264444; AID380501; AID50973; AID52405
Gastrin/cholecystokinin type B receptorHomo sapiens (human)Kd0.00160.00050.00530.0217AID1798046; AID1798047
Mu-type opioid receptorRattus norvegicus (Norway rat)Kd0.00130.00021.296510.0000AID1798046
Delta-type opioid receptorHomo sapiens (human)Kd0.00130.00040.51471.9800AID1798046
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Km11.10000.03912.93886.4000AID680210
Solute carrier organic anion transporter family member 1B2Rattus norvegicus (Norway rat)Km14.90001.10005.28339.4500AID681646
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (39)

Processvia Protein(s)Taxonomy
neuron migrationCholecystokinin receptor type AHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayCholecystokinin receptor type AHomo sapiens (human)
axonogenesisCholecystokinin receptor type AHomo sapiens (human)
forebrain developmentCholecystokinin receptor type AHomo sapiens (human)
cholecystokinin signaling pathwayCholecystokinin receptor type AHomo sapiens (human)
G protein-coupled receptor signaling pathwayCholecystokinin receptor type AHomo sapiens (human)
cellular response to hormone stimulusCholecystokinin receptor type AHomo sapiens (human)
regulation of hormone secretionCholecystokinin receptor type AHomo sapiens (human)
gastric acid secretionGastrin/cholecystokinin type B receptorHomo sapiens (human)
cell surface receptor signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationGastrin/cholecystokinin type B receptorHomo sapiens (human)
positive regulation of cell population proliferationGastrin/cholecystokinin type B receptorHomo sapiens (human)
cholecystokinin signaling pathwayGastrin/cholecystokinin type B receptorHomo sapiens (human)
pH reductionGastrin/cholecystokinin type B receptorHomo sapiens (human)
digestive tract developmentGastrin/cholecystokinin type B receptorHomo sapiens (human)
gland developmentGastrin/cholecystokinin type B receptorHomo sapiens (human)
immune responseDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerDelta-type opioid receptorHomo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
adult locomotory behaviorDelta-type opioid receptorHomo sapiens (human)
negative regulation of gene expressionDelta-type opioid receptorHomo sapiens (human)
negative regulation of protein-containing complex assemblyDelta-type opioid receptorHomo sapiens (human)
positive regulation of CREB transcription factor activityDelta-type opioid receptorHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationDelta-type opioid receptorHomo sapiens (human)
response to nicotineDelta-type opioid receptorHomo sapiens (human)
G protein-coupled opioid receptor signaling pathwayDelta-type opioid receptorHomo sapiens (human)
eating behaviorDelta-type opioid receptorHomo sapiens (human)
regulation of mitochondrial membrane potentialDelta-type opioid receptorHomo sapiens (human)
regulation of calcium ion transportDelta-type opioid receptorHomo sapiens (human)
cellular response to growth factor stimulusDelta-type opioid receptorHomo sapiens (human)
cellular response to hypoxiaDelta-type opioid receptorHomo sapiens (human)
cellular response to toxic substanceDelta-type opioid receptorHomo sapiens (human)
neuropeptide signaling pathwayDelta-type opioid receptorHomo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (15)

Processvia Protein(s)Taxonomy
cholecystokinin receptor activityCholecystokinin receptor type AHomo sapiens (human)
peptide hormone bindingCholecystokinin receptor type AHomo sapiens (human)
peptide bindingCholecystokinin receptor type AHomo sapiens (human)
cholecystokinin receptor activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
protein bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
gastrin receptor activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
peptide hormone bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
type B gastrin/cholecystokinin receptor bindingGastrin/cholecystokinin type B receptorHomo sapiens (human)
1-phosphatidylinositol-3-kinase regulator activityGastrin/cholecystokinin type B receptorHomo sapiens (human)
G protein-coupled opioid receptor activityDelta-type opioid receptorHomo sapiens (human)
protein bindingDelta-type opioid receptorHomo sapiens (human)
receptor serine/threonine kinase bindingDelta-type opioid receptorHomo sapiens (human)
G protein-coupled enkephalin receptor activityDelta-type opioid receptorHomo sapiens (human)
neuropeptide bindingDelta-type opioid receptorHomo sapiens (human)
serine-type endopeptidase inhibitor activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (15)

Processvia Protein(s)Taxonomy
nucleoplasmCholecystokinin receptor type AHomo sapiens (human)
cytosolCholecystokinin receptor type AHomo sapiens (human)
plasma membraneCholecystokinin receptor type AHomo sapiens (human)
membraneCholecystokinin receptor type AHomo sapiens (human)
plasma membraneCholecystokinin receptor type AHomo sapiens (human)
plasma membraneGastrin/cholecystokinin type B receptorHomo sapiens (human)
intracellular membrane-bounded organelleGastrin/cholecystokinin type B receptorHomo sapiens (human)
plasma membraneGastrin/cholecystokinin type B receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
synaptic vesicle membraneDelta-type opioid receptorHomo sapiens (human)
dendrite membraneDelta-type opioid receptorHomo sapiens (human)
presynaptic membraneDelta-type opioid receptorHomo sapiens (human)
axon terminusDelta-type opioid receptorHomo sapiens (human)
spine apparatusDelta-type opioid receptorHomo sapiens (human)
postsynaptic density membraneDelta-type opioid receptorHomo sapiens (human)
neuronal dense core vesicleDelta-type opioid receptorHomo sapiens (human)
plasma membraneDelta-type opioid receptorHomo sapiens (human)
neuron projectionDelta-type opioid receptorHomo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (179)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID264441Displacement of [125I]CCK-8(SO3) from human CCK1 receptor expressed in HEK293 cells2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
AID51465Inhibition of [3H]- pCCK-8 binding to Cholecystokinin type B receptor of rat cerebral cortex membranes1997Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.
AID140128In vivo percent emptying of mouse gallbladder when administered intraperitoneally1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID180188The compound was evaluated for the dose(ip) required to achieve half-maximal inhibition of feeding at 30 min in rats1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID380501Displacement of [125I]CCK-8 from CCK2 receptor in human FGS7 Jurkat cells2006Journal of natural products, Mar, Volume: 69, Issue:3
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
AID1285623Displacement of [125I]CCK-8s from human recombinant CCK-B receptor expressed in CHO cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID79882The compound was tested for effective concentration for amylase release in guinea pig pancreatic Acini1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-a receptor agonists.
AID50950Displacement of [3H]pCCK-8 from cholecystokinin type B receptor in guinea pig brain membrane1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives.
AID232676Selectivity ratio of IC50 of CCK-B to IC50 of CCK-A1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
AID52438Displacement of [125I]BH-CCK-8 from Cholecystokinin type A receptor in guinea pig pancreas1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.
AID52578Ability to displace 1 nM [3H]pCCK-8 from Cholecystokinin type A receptor in guinea pig pancreatic membranes2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
AID74025The compound was tested for the agonistic activity of contractile activities of Guinea pig ileum1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue.
AID79883Effective concentration for hydrolysis of phosphoinositide in guinea pig pancreatic Acini1991Journal of medicinal chemistry, Sep, Volume: 34, Issue:9
Boc-CCK-4 derivatives containing side-chain ureas as potent and selective CCK-a receptor agonists.
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID680210TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Gastroenterology, Nov, Volume: 121, Issue:5
Hepatic uptake of cholecystokinin octapeptide by organic anion-transporting polypeptides OATP4 and OATP8 of rat and human liver.
AID186239Maximal response of the rat to anorectic potency 30 min after intraperitoneal administration (0.5 uM/Kg)1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".
AID51120Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to mouse cerebral cortex cholecystokinin type B receptor1991Journal 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.
AID177924Anorectic potency in rats conditioned to a palatable liquid diet and fasted for 2 hours1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".
AID52253The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig brain1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue.
AID51296Effective concentration for the stimulation of Inositol Phosphate accumulation in CHO cells expressing wild-type Cholecystokinin type B receptor1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.
AID52899Compound was evaluated for the binding affinity towards rat pancreatic Cholecystokinin type A receptor2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1132973Agonist activity at cholecystokinin receptor in NIH guinea pig pancreatic acinar cells assessed as induction of amylase secretion at 0.03 to 0.3 nM1978Journal of medicinal chemistry, Oct, Volume: 21, Issue:10
Cholecystokinin (pancreozymin). 4. Synthesis and properties of a biologically active analogue of the C-terminal heptapeptide with epsilon-hydroxynorleucine sulfate replacing tyrosine sulfate.
AID177402Ability of intraperitoneally administered compound, to inhibit food intake was measured 3 hr after feeding the rats.2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.
AID233655Selectivity ratio of Inhibition of CCK-A vs CCK-B1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID78645Compound was tested for agonist activity of isolated guinea pig gallbladder by using functional assay1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
AID264443Antagonist activity at CCK1 receptor expressed in HEK 293 cells assessed as accumulation of [3H]inositol phosphates by PI assay2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
AID194318Compound was tested in vivo for its Percent Maximal anorectic potency in rats at dose of 0.1 umol/kg ip1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID77909Potency in displacing [3H]Boc(Nle28,Nle31)-CCk27-33 from guinea pig pancreatic acini.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Synthesis and biological activity of CCK26-33-related analogues modified in position 31.
AID78501mCCK-8 contraction induced by 30 uM in vitro, normalized to CCK-8 (1 uM)1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID52916Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type A receptor in the rat pancreas.1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.
AID140120Compound was tested in vivo for its activity in mouse gallbladder emptying assay at dose of 0.1 umol/kg ip1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID52254The compound was tested for the inhibition of [3H]propionyl specific binding to CCK-8 receptor of guinea pig pancreatic membrane1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue.
AID51295Affinity against Cholecystokinin type B receptor expressed in CHO cells on rat brain.2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.
AID52407Displacement of [3H]pentagastrin from Cholecystokinin receptor of mouse cerebral cortex1987Journal of medicinal chemistry, Apr, Volume: 30, Issue:4
Synthesis and binding affinities of analogues of cholecystokinin-(30-33) as probes for central nervous system cholecystokinin receptors.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID78509In vitro concentration required to induce contraction of isolated GPGB1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID1336316Displacement of [125I]CCK-8s from human recombinant CCK2 receptor expressed in CHO cells measured after 60 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID185555Maximal response at 0.5 umol/kg intraperitoneal dose1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
AID95432Compound was evaluated for calcium mobilization in Jurkat cells2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.
AID234374Selectivity ratio is IC50 value of CCK-A receptor to that of CCK-B receptor1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.
AID175484Compound was evaluated for the inhibition of amylase secretion in isolated rat pancreatic acini2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.
AID52746Binding affinity against human Cholecystokinin type A receptor by displacement of [125I]CCK-81996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
AID52248Potency in displacing [3H]propionyl-Cholecystokinin from mouse brain membranes.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Synthesis and biological activity of CCK26-33-related analogues modified in position 31.
AID51096Displacement of CCK-8 from human Cholecystokinin type B receptor expressing CHO cell membranes 1995Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).
AID51440Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type B receptor from rat cerebral cortex membrane1999Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.
AID1572004Agonist activity at human CCK2R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID176573Feeding inhibitory potency in 21 hr fasted rat was determined after 3h intravenous administration of the compound1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.
AID50512Ratio calculated as IC50 ratio of CCK-A to that of CCK-B1991Journal 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.
AID51097In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type B receptor expressed in CHO-K1 cells1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID232267Selectivity ratio between IC50 values of CCK-A and CCK-B1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID52748Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type A receptor1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID52898Binding affinity by competitive inhibition of the radioligand [3H]pCCK-8 at Cholecystokinin type A receptor from rat pancreas1999Journal of medicinal chemistry, Nov-04, Volume: 42, Issue:22
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structural modifications at the tryptophan domain.
AID51443Inhibition of the specific binding of [125I](BH)-CCK-8 to Cholecystokinin type B receptor in rat brain cortex1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.
AID346410Displacement of radiolabeled CCK-8s from human CCK1 receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID50955Binding affinity against cholecystokinin type B receptor on guinea pig cortex.2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.
AID1336315Displacement of [125I]CCK-8s from human recombinant CCK1 receptor expressed in CHO cells measured after 60 mins by scintillation counting method2017Bioorganic & medicinal chemistry, 01-15, Volume: 25, Issue:2
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
AID264444Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accumulation of [3H]inositol phosphates by PI assay2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
AID194680The compound was evaluated for the maximal reduction in feeding achieved at 1 uM/kg dose(ip)1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID52425In vitro agonist activity against Cholecystokinin type A receptor isolated from guinea pig gall bladder.1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
AID52581Compound was tested for binding affinity against CCK1 (cholecystokinin) receptor on guinea pig pancreatic membranes2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.
AID1572003Agonist activity at human CCK1R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
AID346411Displacement of radiolabeled CCK-8s from human CCK2 receptor2008Journal of medicinal chemistry, Nov-27, Volume: 51, Issue:22
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.
AID52896Evaluated for inhibition of cholecystokinin type A receptor by displacing [125I]bolton hunter CCK-8 radioligand in the rat pancreas1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
Rationally designed "dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.
AID51460Binding affinity towards Cholecystokinin type B receptor in rat cortex synaptosomes using [125I]BH-CCK-8 as radioligand2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.
AID51458Affinity to inhibit [3H]pCCK-8 specific binding on rat brain Cholecystokinin type B receptor expressed in CHO cells1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.
AID78504In vitro functional agonist activity in the isolated guinea pig gall bladder, concentration at which 50% of the maximal contraction observed was reported.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
AID176572Feeding inhibitory potency in 21 hr fasted rat was determined after 0.5 hr intravenous administration of the compound1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.
AID588963Substrates of transporters of clinical importance in the absorption and disposition of drugs, OATP1B32010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID52741Compound was evaluated for maximal stimulation induced by 1 uM test compound, normalized to CCK-8 (1 uM) in stably transfected CHO-K1 cell lines expressing the human Cholecystokinin type A receptor1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID52405Ability to stimulate intracellular calcium response was determined using CCK receptor-bearing chinese hamster ovary cell line1999Journal of medicinal chemistry, Jun-17, Volume: 42, Issue:12
A peptide agonist acts by occupation of a monomeric G protein-coupled receptor: dual sites of covalent attachment to domains near TM1 and TM7 of the same molecule make biologically significant domain-swapped dimerization unlikely.
AID51459Binding affinity for Cholecystokinin type B receptor using [125I]-BH-CCK-8 in rat cortex synaptosomes1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.
AID50977Compound was tested in vitro for its ability to displace [125I]Bolton-Hunter CCK-8 from membrane preparation isolated from CHO-KI cells stably transfected with cDNA of human Cholecystokinin type B receptor1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID169972Compound was evaluated for (in vivo) gastrin like activity measured on perfused rat stomach after intravenous administration1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Synthesis of potent heptapeptide analogues of cholecystokinin.
AID78507relative efficacy as determined by maximal concentration observed at 1 uM standardized to CCK-8 (1 uM) =100% was determined1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID78646Relative efficacy as determined maximal contraction was observed at 30 uM standardized to CCK-81996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID51098In vitro for binding affinity against human cholecystokinin type B receptor.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
AID53031Half-maximal inhibition of specific binding of [125I]bolton hunter CCK-8 to rat pancreas cholecystokinin type A receptor1991Journal 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.
AID52406Binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in mouse brain membranes at a KD concentration of 0.19 nM1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Investigation of peripheral cholecystokinin receptor heterogeneity by cyclic and related linear analogues of CCK26-33: synthesis and biological properties.
AID140124Effective dose against mouse gall bladder emptying when administered intraperitoneally1996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID680766TP_TRANSPORTER: inhibition of E1S uptake (E1S: 0.004 uM, CCK-8: 100 uM) in Xenopus laevis oocytes2003The Journal of pharmacy and pharmacology, Jul, Volume: 55, Issue:7
Contribution of organic anion transporting polypeptide OATP-C to hepatic elimination of the opioid pentapeptide analogue [D-Ala2, D-Leu5]-enkephalin.
AID50511Ratio between IC50 CCK-A vs IC50 CCK-B(B2)1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID241978Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type A receptor of rat pancreas homogenates2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.
AID113869Intraperitoneal dose that produces a half maximal response in mouse gall bladder emptying assay (in vivo)1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
AID75932Agonist activity by measuring the effect on amylase secretion from guinea pig acini.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Synthesis and biological activity of CCK26-33-related analogues modified in position 31.
AID75931Agonist activity by measuring the ability to stimulate the contraction of the isolated guinea pig ileum.1988Journal of medicinal chemistry, May, Volume: 31, Issue:5
Synthesis and biological activity of CCK26-33-related analogues modified in position 31.
AID223181Evaluated for contractile activities of guinea pig ileum for agonistic activity1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Investigation of peripheral cholecystokinin receptor heterogeneity by cyclic and related linear analogues of CCK26-33: synthesis and biological properties.
AID242136Inhibition of [3H]-pCCK-8 binding to Cholecystokinin type B receptor of rat cerebral cortex homogenates2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.
AID50968Compound was evaluated for maximal stimulation induced by 1 uM test compound, normalized to CCK-8 (1 uM) in stably transfected CHO-K1 cell lines expressing the human Cholecystokinin type B receptor1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID167754Compound was evaluated for cholecystokinin activity measured in isolated rabbit gallbladder strips (in vitro)1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Synthesis of potent heptapeptide analogues of cholecystokinin.
AID50951Inhibition of [3H]pCCK-8 binding to Guinea pig cortex membrane Cholecystokinin type B receptor1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.
AID50978Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type B receptor stably expressed in CHO-K1 cells1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".
AID52411Evaluated for binding affinity measured by inhibiting [3H]Boc[Nle28,31]CCK27-33 specific binding to Cholecystokinin receptor in rat pancreas membranes at a KD concentration of 4.4 nM1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Investigation of peripheral cholecystokinin receptor heterogeneity by cyclic and related linear analogues of CCK26-33: synthesis and biological properties.
AID233446Selectivity ratio measured as the pIC50 ratio of CCK-A to that of CCK-B.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
AID175500Compound was tested in vitro for its ability to stimulate dispersed rat pancreatic acini to secrete amylase into the medium using CCK-8 as an agonist control1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
Structurally similar small molecule photoaffinity CCK-A agonists and antagonists as novel tools for directly probing 7TM receptors-ligand interactions.
AID679168TP_TRANSPORTER: cell accumulation in OATP2-expressing HEK293 cells2004The Journal of pharmacology and experimental therapeutics, Oct, Volume: 311, Issue:1
Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans.
AID53035Inhibition of [3H]pCCK-8 binding to cholecystokinin type A receptor of rat pancreas2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold.
AID51623Displacement of [3H]-pCCK-8 from cholecystokinin-A receptor in guinea pig pancreatic membrane1993Journal of medicinal chemistry, Jan-08, Volume: 36, Issue:1
CCK-B agonist or antagonist activities of structurally hindered and peptidase-resistant Boc-CCK4 derivatives.
AID74024The compound was tested for the agonistic activity of amylase secretion by Guinea pig acini1989Journal of medicinal chemistry, Feb, Volume: 32, Issue:2
Full agonists of CCK8 containing a nonhydrolyzable sulfated tyrosine residue.
AID678974TP_TRANSPORTER: cell accumulation in OATP8-expressing HEK293 cells2004The Journal of pharmacology and experimental therapeutics, Oct, Volume: 311, Issue:1
Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans.
AID52252Displacement of 0.1 nM [3H]pCCK-8 from guinea pig pancreatic membranes1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.
AID51456Ability to displace 1 nM [3H]pCCK-8 from rat Cholecystokinin type B receptor stably expressing in CHO cells2004Bioorganic & medicinal chemistry letters, Jan-19, Volume: 14, Issue:2
Synthesis and biological characterisation of [3H]BBL454, a new CCK2 selective radiolabelled agonist displaying original pharmacological properties.
AID78648Maximum contractile response at 30 uM, normalized to CCK-8 (1 uM)1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID231666CCK-A selectivity is the Ratio of CCK-B to CCK-A binding affinity2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.
AID78650In-vitro potency on the isolated guinea pig gallbladder1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID50946Displacement of 0.2 nM [3H]pCCK-8 from guinea pig brain membranes1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.
AID231512Ratio of binding affinity towards CCK-B receptor to that of CCK-A receptor1995Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID232488Selectivity as ratio of Ki against CCK-A and CCK-B receptors1997Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.
AID52751In vitro displacement of [125I]BH-CCK-8 from cDNA of human Cholecystokinin type A receptor expressed in CHO-K1 cells1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID264442Displacement of [125I]CCK-8(SO3) from human CCK2 receptor expressed in HEK293 cells2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID50690Displacement of [125I]BH-CCK-8 from Cholecystokinin type B receptor of guinea pig cortex1990Journal of medicinal chemistry, Nov, Volume: 33, Issue:11
Development of CCK-tetrapeptide analogues as potent and selective CCK-A receptor agonists.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID233622Ratio of binding affinity towards CCK-A receptor to that of CCK-B receptor1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.
AID52749Concentration required to displace [125I]Bolton-Hunter CCK-8 from human Cholecystokinin type A receptor stably expressed in CHO-K1 cells1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".
AID50510Inhibition ratio on CCK-A receptor with respect to CCK-B receptor1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
Rationally designed "dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.
AID140130Compound was tested in vivo Percent Maximal response activity in mouse gallbladder emptying assay at dose of 0.1 umol/kg ip1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID52744Binding affinity against human Cholecystokinin type A receptor in membrane preparation isolated from CHO-K1 cells stably transfected with cDNA of human CCK-A using [125I]-Bolton-Hunter CCK-8 as radioligand1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
AID50506Inhibition of [3H]pCCK-8 specific binding to Cholecystokinin type A receptor of rat pancreas1997Journal of medicinal chemistry, Oct-10, Volume: 40, Issue:21
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.
AID52580Inhibition of [3H]pCCK-8 binding to Cholecystokinin type A receptor of Guinea pig pancreatic membranes1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.
AID681646TP_TRANSPORTER: uptake in Xenopus laevis oocytes2001Gastroenterology, Nov, Volume: 121, Issue:5
Hepatic uptake of cholecystokinin octapeptide by organic anion-transporting polypeptides OATP4 and OATP8 of rat and human liver.
AID115307Maximal response at 1 nmol/kg intraperitoneal dose1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
AID51113Inhibition of binding of [125I]Bolton-Hunter labeled CCK-8 to cholecystokinin type B receptor in the mouse cerebral cortex1993Journal of medicinal chemistry, Mar-05, Volume: 36, Issue:5
Cholecystokinin dipeptoid antagonists: design, synthesis, and anxiolytic profile of some novel CCK-A and CCK-B selective and "mixed" CCK-A/CCK-B antagonists.
AID52255Relative affinity for guinea pig membranes of pancreas and brain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and binding affinities of cyclic and related linear analogues of CCK8 selective for central receptors.
AID176340Compound was tested in vivo for its anorectic potency in rats at dose of 0.1 umol/kg ip1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID76918Relative efficacy determined by the maximal contraction observed at 30 uM, standardized to CCK-81996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
AID52753In vitro for binding affinity against human cholecystokinin type A receptor.1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
AID177923Anorectic potency in rat was tested and intraperitoneal dose that produces a half maximal response (in vivo)1997Journal of medicinal chemistry, Aug-15, Volume: 40, Issue:17
Optimization of 3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines as potent, orally active CCK-A agonists.
AID52750Displacement of CCK-8 from CHO cell membranes expressing human Cholecystokinin type A receptor1995Journal of medicinal chemistry, Jan-06, Volume: 38, Issue:1
CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).
AID52912Concentration required to inhibit by 50% specific binding of [125I](BH)-CCK-8 to cholecystokinin type A receptor in rat pancreatic acini1992Journal of medicinal chemistry, Jan, Volume: 35, Issue:1
Structure-antigastrin activity relationships of new (R)-4-benzamido-5-oxopentanoic acid derivatives.
AID50501Binding affinity for Cholecystokinin type A receptor using [125I]BH-CCK-8 in rat pancreatic tissue1997Journal of medicinal chemistry, Dec-19, Volume: 40, Issue:26
Synthesis and biological evaluation of potent, selective, hexapeptide CCK-A agonist anorectic agents.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID51105Binding affinity towards Cholecystokinin type B receptor in mouse cortex membrane2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
The design and synthesis of the high efficacy, non-peptide CCK1 receptor agonist PD170292.
AID1572002Displacement of [125I]-CCK-8 from human CCK2R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
AID51107Evaluated for inhibition of cholecystokinin type B receptor by displacing [125I]-Bolton hunter CCK-8 radioligand in the mouse cerebral cortex1992Journal of medicinal chemistry, Jul-10, Volume: 35, Issue:14
Rationally designed "dipeptoid" analogues of CCK. Acid mimics of the potent and selective non-peptide CCK-B receptor antagonist CI-988.
AID231773Ratio of compound affinity on CCK-A receptor with respect to CCK-B receptor1997Journal of medicinal chemistry, Feb-28, Volume: 40, Issue:5
Structure-based design of new constrained cyclic agonists of the cholecystokinin CCK-B receptor.
AID175694Evaluated for agonist activity measured as amylase secretion by rat pancreas1987Journal of medicinal chemistry, Jun, Volume: 30, Issue:6
Investigation of peripheral cholecystokinin receptor heterogeneity by cyclic and related linear analogues of CCK26-33: synthesis and biological properties.
AID235357Selectivity ratio between human CCK-A receptor/ human CCK-B receptor1996Journal of medicinal chemistry, Jan-19, Volume: 39, Issue:2
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity. 1. Optimization of the agonist "trigger".
AID109525Anticonvulsive activity against picrotoxin-induced (6 mg/kg sc) convulsions in mice, time of death1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Synthesis of potent heptapeptide analogues of cholecystokinin.
AID244174Ratio of IC50 values for binding to Cholecystokinin A and Cholecystokinin B receptors2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
5-(tryptophylamino)-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based cholecystokinin receptor antagonists: reversal of CCK1 receptor subtype selectivity toward CCK2 receptors.
AID194321Compound was tested in vivo for its Percent Maximal anorectic potency in rats at dose of 1 umol/kg po; ia = Inactive1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID52743Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type A receptor1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID140132Compound was tested in vivo for Percent Maximal response in mouse gallbladder emptying assay at dose of 1 umol/kg po; ND = Not determined1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID50976Binding affinity against human Cholecystokinin type B receptor by displacement of [125I]CCK-81996Journal of medicinal chemistry, Jul-05, Volume: 39, Issue:14
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
AID51121In vitro binding affinity against Cholecystokinin type B receptor in mouse cerebral cortical membranes using [125I]Tyr(SO3H)27]-CCK-8 binding assay2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold.
AID126873Compound tested in vivo for mouse gallbladder emptying at 0.1 nM/kg ip1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
AID50973Compound was evaluated for the [Ca2+] mobilization innstably transfected CHO-K1 cell lines expressing human Cholecystokinin type B receptor1995Journal of medicinal chemistry, Aug-18, Volume: 38, Issue:17
Modification of receptor selectivity and functional activity in cholecystokinin peptoid ligands.
AID1572001Displacement of [125I]-CCK-8 from human CCK1R expressed in human 1321N1 cell membranes after 2 hrs by SPA assay2019Journal of medicinal chemistry, 02-14, Volume: 62, Issue:3
Structure-Activity Relationships and Characterization of Highly Selective, Long-Acting, Peptide-Based Cholecystokinin 1 Receptor Agonists.
AID50502Inhibition of [125I]BH-CCK-8 binding to Cholecystokinin type A receptor of rat pancreatic tissue2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.
AID109526Anticonvulsive potency against picrotoxin induced (6 mg/kg sc) convulsions in mice, first tonic seizure1984Journal of medicinal chemistry, Jul, Volume: 27, Issue:7
Synthesis of potent heptapeptide analogues of cholecystokinin.
AID50974Binding affinity against human Cholecystokinin type B receptor in CHO-K1 cells using [125I]-Bolton-Hunter CCK-8 as radioligand1996Journal of medicinal chemistry, Jul-19, Volume: 39, Issue:15
3-[2-(N-phenylacetamide)]-1,5-benzodiazepines: orally active, binding selective CCK-A agonists.
AID51461Compound was tested for binding affinity against Cholecystokinin type B receptor expressed in CHO cells on the rat brain.2000Journal of medicinal chemistry, Oct-05, Volume: 43, Issue:20
Replacement of glycine with dicarbonyl and related moieties in analogues of the C-terminal pentapeptide of cholecystokinin: CCK(2) agonists displaying a novel binding mode.
AID1285622Displacement of [125I]CCK-8s from human recombinant CCK-A receptor expressed in CHO cells2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
AID53032Displacement of 125I]-D-Tyr-Gly-[(Nle28,31)CCK-26-33] from rat cell membrane Cholecystokinin type A receptor1998Bioorganic & medicinal chemistry letters, Nov-17, Volume: 8, Issue:22
Structurally similar small molecule photoaffinity CCK-A agonists and antagonists as novel tools for directly probing 7TM receptors-ligand interactions.
AID140121Compound was tested in vivo for its activity in mouse gallbladder emptying assay at dose of 1 umol/kg po; ND = Not determined1996Journal of medicinal chemistry, Dec-20, Volume: 39, Issue:26
Discovery of 1,5-benzodiazepines with peripheral cholecystokinin (CCK-A) receptor agonist activity (II): Optimization of the C3 amino substituent.
AID42901Inhibition of [3H]pCCK-8 binding to cholecystokinin type B receptor of rat cerebral cortex2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
5-(Tryptophyl)amino-1,3-dioxoperhydropyrido[1,2-c]pyrimidine-based potent and selective CCK(1) receptor antagonists: structure-activity relationship studies on the central 1,3-dioxoperhydropyrido[1,2-c]pyrimidine scaffold.
AID177401Ability of intraperitoneally administered compound, to inhibit food intake was measured 0.5 hr after feeding the rats.2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
CCK peptides with combined features of hexa- and tetrapeptide CCK-A agonists.
AID1346883Human CCK2 receptor (Cholecystokinin receptors)1993The Journal of biological chemistry, Apr-15, Volume: 268, Issue:11
The human brain cholecystokinin-B/gastrin receptor. Cloning and characterization.
AID1346883Human CCK2 receptor (Cholecystokinin receptors)1993The Journal of biological chemistry, Aug-25, Volume: 268, Issue:24
Functional characterization of a human brain cholecystokinin-B receptor. A trophic effect of cholecystokinin and gastrin.
AID1346809Rat CCK1 receptor (Cholecystokinin receptors)1990Proceedings of the National Academy of Sciences of the United States of America, Sep, Volume: 87, Issue:17
Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity.
AID1798047Radioligand Labeled Binding Assay and Phosphatidylinositol Hydrolysis Assay for the CCK Receptor from Article 10.1021/jm050921q: \\Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin r2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
AID1798046Radioligand Labeled Binding Assay and [35S]GTP-gamma-S Binding Assay from Article 10.1021/jm050921q: \\Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.\\2006Journal of medicinal chemistry, May-18, Volume: 49, Issue:10
Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,809)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901201 (31.53)18.7374
1990's1422 (37.33)18.2507
2000's608 (15.96)29.6817
2010's370 (9.71)24.3611
2020's208 (5.46)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 39.09

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 strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index39.09 (24.57)
Research Supply Index8.32 (2.92)
Research Growth Index4.53 (4.65)
Search Engine Demand Index65.76 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (39.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials72 (1.79%)5.53%
Reviews91 (2.27%)6.00%
Case Studies12 (0.30%)4.05%
Observational0 (0.00%)0.25%
Other3,840 (95.64%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]