Page last updated: 2024-12-05

pirenzepine

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Description

Pirenzepine is an anticholinergic drug that acts as a selective antagonist of the M1 subtype of muscarinic acetylcholine receptors. It was first synthesized in the 1970s and has been used to treat various conditions, including peptic ulcers, irritable bowel syndrome, and urinary incontinence. Pirenzepine is thought to exert its therapeutic effects by blocking the actions of acetylcholine at M1 receptors, which are found in the gastrointestinal tract, bladder, and central nervous system. Pirenzepine is studied for its potential to treat a variety of conditions, including Alzheimer's disease, Parkinson's disease, and schizophrenia, due to its ability to modulate cholinergic neurotransmission.'

Pirenzepine: An antimuscarinic agent that inhibits gastric secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular, and urinary function. It promotes the healing of duodenal ulcers and due to its cytoprotective action is beneficial in the prevention of duodenal ulcer recurrence. It also potentiates the effect of other antiulcer agents such as CIMETIDINE and RANITIDINE. It is generally well tolerated by patients. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID4848
CHEMBL ID9967
CHEBI ID8247
SCHEMBL ID41705
MeSH IDM0016894

Synonyms (117)

Synonym
gastrozepin
pirenzepinum [inn-latin]
pirenzepina [inn-spanish]
brn 0628987
pirenzepine [inn:ban]
5,11-dihydro-11-((4-methyl-1-piperazinyl)acetyl)-6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one
pirenzepin
einecs 249-228-4
6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one, 5,11-dihydro-11-((4-methyl-1-piperazinyl)acetyl)-
AB00053603-08
BRD-K89375097-300-05-4
gtpl328
DIVK1C_000127
KBIO1_000127
11-[(4-methylpiperazin-1-yl)acetyl]-5,11-dihydro-6h-pyrido[2,3-b][1,4]benzodiazepin-6-one
SPECTRUM_001378
PDSP2_000949
tocris-1071
NCGC00015836-02
NCGC00024297-02
cas-29868-97-1
NCGC00015836-01
lopac-p-7412
PRESTWICK2_000129
pirenzepinum
pirenzepina
CHEBI:8247 ,
BPBIO1_000196
PDSP1_000965
BSPBIO_002945
LOPAC0_000962
SPECTRUM5_001344
BSPBIO_000178
AB00053603
LS-519 ,
28797-61-7
pirenzepine
C07508
DB00670
11-((4-methyl-1-piperazinyl)acetyl)-5,11-dihydro-6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one
IDI1_000127
PRESTWICK3_000129
NCGC00024297-05
KBIO2_001858
KBIO2_004426
KBIO2_006994
KBIO3_002445
KBIOSS_001858
KBIOGR_000794
PRESTWICK1_000129
SPBIO_002117
SPECTRUM3_001453
NINDS_000127
SPECTRUM2_001417
PRESTWICK0_000129
SPBIO_001494
SPECTRUM4_000437
NCGC00015836-03
NCGC00024297-04
HMS2089K21
NCGC00015836-09
L000485
aci-91
CHEMBL9967 ,
D08389
pirenzepine (inn)
11-[2-(4-methylpiperazin-1-yl)acetyl]-5h-pyrido[2,3-b][1,4]benzodiazepin-6-one
NCGC00015836-08
dtxcid303487
tox21_110239
dtxsid7023487 ,
cas-28797-61-7
CCG-205042
AKOS015969751
NCGC00015836-05
NCGC00015836-10
NCGC00015836-04
NCGC00015836-07
NCGC00015836-06
3g0285n20n ,
unii-3g0285n20n
FT-0673943
FT-0600051
pirenzepine [mi]
pirenzepine [who-dd]
pirenzepine [inn]
pirenzepine [vandf]
SCHEMBL41705
NCGC00015836-12
tox21_110239_1
11-[2-(4-methylpiperazin-1-yl)-acetyl]-5,11-dihydro-6h-pyrido[2,3-b][1,4]benzodiazepin-6-one
cid_185248
11-[2-(4-methylpiperazin-1-yl)acetyl]-5h-pyrido[2,3-b][1,4]benzodiazepin-6-one;hydrochloride
bdbm39341
11-[2-(4-methylpiperazin-1-yl)ethanoyl]-5h-pyrido[2,3-b][1,4]benzodiazepin-6-one;hydrochloride
11-[2-(4-methyl-1-piperazinyl)-1-oxoethyl]-5h-pyrido[2,3-b][1,4]benzodiazepin-6-one;hydrochloride
11-[2-(4-methylpiperazino)acetyl]-5h-pyrido[2,3-b][1,4]benzodiazepin-6-one;hydrochloride
5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-6h-pyrido[2,3-b][1,4]benzodiazepin-6-one
6h-pyrido[2,3-b][1,4]benzodiazepin-6-one, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]-
11-[(4-methyl-1-piperazinyl)acetyl]-5,11-dihydro-6h-pyrido[2,3-b][1,4]benzodiazepin-6-one #
AB00053603_09
2-[2-(4-methylpiperazin-1-yl)acetyl]-2,4,9-triazatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,12,14-hexaen-10-one
SBI-0050935.P003
Q419550
11-(2-(4-methylpiperazin-1-yl)acetyl)-5,11-dihydro-6h-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
11-[2-(4-methyl-piperazin-1-yl)-acetyl]-5,11-dihydro-benzo[e]pyrido[3,2-b][1,4]diazepin-6-one
BCP12188
BRD-K89375097-300-06-2
SDCCGSBI-0050935.P004
NCGC00015836-19
HMS3742G13
HMS3742E07
6h-pyrido[2,3-b][1,4]benzodiazepin-6-one, 5,11-dihydro-11-[(4-methyl-1-piperazinyl)acetyl]- (8ci,9ci)
6h-pyrido[2,3-b][1,4]benzodiazepin-6-one, 5,11-dihydro-11-[2-(4-methyl-1-piperazinyl)acetyl]-
STARBLD0016668
CS-0013749
HY-17037A

Research Excerpts

Overview

Pirenzepine is an anti-ulcer agent which belongs to the anti-cholinergic group of gastrointestinal disorder drugs and functions as an M1 receptor selective antagonist. It is a peripheral antiacetylcholine drug more selective for reducing gastric acid secretion than for increasing pupil diameter.

ExcerptReferenceRelevance
"Pirenzepine is an anti-ulcer agent which belongs to the anti-cholinergic group of gastrointestinal disorder drugs and functions as an M1 receptor selective antagonist. "( Unravelling the interaction of pirenzepine, a gastrointestinal disorder drug, with calf thymus DNA: An in vitro and molecular modelling study.
Afrin, S; Ali, A; Husain, MA; Rahman, Y; Sarwar, T; Tabish, M, 2017
)
2.18
"Pirenzepine is an atropine analogue approved to treat peptic ulcer disease in Europe that is devoid of central actions, which are mostly responsible for anti-muscarinic agents side effects."( Autonomic modulation during acute myocardial ischemia by low-dose pirenzepine in conscious dogs with a healed myocardial infarction: a comparison with beta-adrenergic blockade.
Adamson, PB; Foreman, RD; Pedretti, RF; Prete, G; Vanoli, E, 2003
)
1.28
"Pirenzepine is suggested to be a relatively selective muscarinic (M(1)) antagonist and is currently under investigation for the treatment of myopia. "( Effects of pirenzepine on pupil size and accommodation in rhesus monkeys.
Frishman, LJ; Glasser, A; Ostrin, LA, 2004
)
2.16
"Pirenzepine is a peripheral antiacetylcholine drug more selective for reducing gastric acid secretion than for increasing pupil diameter and with little central antiacetylcholine effect."( Pirenzepine selectively inhibits gastric acid secretion: a comparative pharmacological study between pirenzepine and seven other antiacetylcholine drugs.
Heathcote, BV; Parry, M, 1980
)
2.43
"Pirenzepine appears to be an effective drug for the short-term treatment of duodenal ulcer."( Pirenzepine in the treatment of peptic ulcer disease. Review and commentary.
Bianchi Porro, G; Petrillo, M, 1982
)
2.43
"Pirenzepine is a new anticholinergic agent which selectively binds to gastric mucosal muscarinic receptors. "( The efficacy and selectivity of pirenzepine. Review and commentary.
Reilly, PA; Texter, EC, 1982
)
1.99
"Pirenzepine (GZ) is a drug recently introduced in the therapy of gastroduodenal ulcer (GDU)."( Inhibition of carbonic anhydrase by pirenzepine.
Búzás, G; Domuta, M; Puşcaş, I; Surányi, P, 1981
)
1.26
"Pirenzepine (Gastrozepin) is a drug recently introduced in the therapy of gastroduodenal ulcer (GDU). "( Inhibition of gastric mucosa carbonic anhydrase by pirenzepine in patients with gastroduodenal ulcers.
Búzás, G; Domuta, M; Puşcaş, I; Surányi, P, 1981
)
1.96
"Pirenzepine is a very hydrophilic compound. "( An international pharmacokinetic study on pirenzepine following a single oral dose.
Bozler, G; Hammer, R, 1980
)
1.97
"Pirenzepine is a new antimuscarinic drug with a peculiar affinity for gastric parietal cells' acetylcholine receptors. "( The effect of pirenzepine on meal-stimulated gastric acid secretion, gastrin release and gastric emptying.
Bianchi Porro, G; Lazzaroni, M; Parente, F; Prada, A; Sangaletti, O, 1982
)
2.07
"Pirenzepine is a M1 receptor antagonist and effective in vagally-induced bronchoconstriction."( Comparison of the bronchodilator efficacy of nebulized pirenzepine and ipratropium bromide in patients with airway obstructive lung disease.
Celikel, T; Ceyhan, B; Kandemir, B; Simsir, S, 1993
)
1.25
"Pirenzepine is a tricyclic antimuscarine drug with antisecretory effect on gastric secretion and inhibitory effect on esophageal peristalsis (EP). "( Effects of pirenzepine and atropine on basal lower esophageal pressure and gastric acid secretion in man: a placebo-controlled randomized study.
Aggestrup, S; Jensen, SL, 1991
)
2.11
"Pirenzepine is a newly developed anticholinergic drug that reduces gastric acid secretion and is therefore used in Europe and Japan to treat patients with peptic ulcer. "( Pirenzepine inhibits pancreatic exocrine secretion in the rat.
Baba, S; Fujii, M; Nakamura, T; Oka, T; Okabayashi, Y; Otsuki, M, 1986
)
3.16
"Pirenzepine is an antisecretory anticholinergic type drug that has recently been shown to be relatively free of usual anticholinergic side effects on esophageal smooth muscle. "( Pirenzepine and propantheline effects on esophageal pressure responses to bethanechol.
Castell, DO; Castell, JA; Dalton, CB; Hassan, M, 1986
)
3.16
"Pirenzepine is known to be an antiulcer drug with antimuscarinic activity. "( Effect of the antimuscarinic agent pirenzepine on the in vivo biliary secretion of dogs in response to various stimuli.
Madrid, JA; Martínez de Victoria, E; Salido, GM, 1988
)
1.99
"Pirenzepine is an antimuscarinic drug highly selective for M1 receptors, which proved to be effective in the treatment of peptic ulcer. "( [Pharmacologic treatment of duodenal ulcer. Short and long-term results with pirenzepine in ambulatory patients].
Barberani, F; Carpinelli, D; D'Ambrosio, C; Della Spoletina, A; Fiorini, MA; Nicolao, V; Schiaroli, G; Valentini, P, 1986
)
1.94
"Pirenzepine is a 'selective' antimuscarinic agent which, unlike classic anticholinergic agents, inhibits gastric acid secretion at lower doses than are required to affect gastrointestinal motility, salivary, central nervous system, cardiovascular, ocular and urinary functions. "( Pirenzepine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in peptic ulcer disease and other allied diseases.
Brogden, RN; Carmine, AA, 1985
)
3.15

Effects

Pirenzepine has been shown to bind with high affinity to muscarinic receptors of certain brain regions and peripheral ganglia (M1 subtype) and with low affinity to receptors of the heart and upper gastrointestinal tract (M2 subtype). The drug has been widely used for the treatment of gastric and duodenal ulcer.

ExcerptReferenceRelevance
"Pirenzepine (Gastrozepin) has a proven positive effect in the treatment of peptic ulcers by blocking the so called muscarinic acetylcholine receptors of the gastric glands. "( [Effect of pirenzepine on motility of Oddi's sphincter].
Brandstätter, G; Kratochvil, P; Wurzer, H, 1992
)
2.12
"Pirenzepine has been shown to evoke a variety of antimuscarinic effects in animals. "( Pirenzepine--a ligand with original binding properties to muscarinic receptors.
Birdsall, NJ; Burgen, AS; Hammer, R; Hulme, EC; Stockton, J, 1980
)
3.15
"Pirenzepine has inhibitory effects on gastrin secretion both in vivo and in vitro. "( Effects of pirenzepine on omeprazole-induced gastrin gene expression in rat antral tissues.
Fukino, Y; Hamada, M; Kajiyama, G; Kamiyasu, T; Sumii, K; Sumii, M; Tari, A, 1996
)
2.13
"Pirenzepine has been reported to inhibit gastrin secretion."( Effects of pirenzepine on omeprazole-induced hypergastrinemia and acid suppression in peptic ulcer patients.
Fukino, Y; Hamada, M; Haruma, K; Inoue, M; Kajiyama, G; Kamiyasu, T; Sumii, K; Sumii, M; Tari, A, 1996
)
1.41
"Pirenzepine (Gastrozepin) has a proven positive effect in the treatment of peptic ulcers by blocking the so called muscarinic acetylcholine receptors of the gastric glands. "( [Effect of pirenzepine on motility of Oddi's sphincter].
Brandstätter, G; Kratochvil, P; Wurzer, H, 1992
)
2.12
"Pirenzepine has been widely used for the treatment of gastric and duodenal ulcer. "( Pirenzepine as anti-inflammatory drug in a model of experimental colitis in rat.
Bustos-Fernández, L; Celener, D; González, E; Hamamura, S; Kofoed, JA; Ledesma de Paolo, MI; Schiffrin, E, 1987
)
3.16
"[3H]Pirenzepine ([ 3H]PZ) has been shown to interact with a subset of [3H]QNB binding sites in forebrain and heart."( Antibodies to a synthetic peptide can be used to distinguish between muscarinic acetylcholine receptor binding sites in brain and heart.
Artymyshyn, RP; Harkness, J; Luthin, GR; Wolfe, BB, 1988
)
0.76
"But pirenzepine has also been found to have a cytoprotective effect on gastric mucosa in rats."( Cytoprotective effect of pirenzepine and palm wine on rats gastric mucosa.
Ezeamuzie, IC; Ibu, JO; Ngeribara, CO; Obuforoibo, AA, 1986
)
1.06
"Pirenzepine has been proposed to selectively inhibit gastric acid production. "( Oral pirenzepine does not affect esophageal pressures in man.
Blackwell, JN; Castell, DO; Dalton, CB, 1986
)
2.23
"Pirenzepine has been shown to bind with high affinity to muscarinic receptors of certain brain regions and peripheral ganglia (M1 subtype) and with low affinity to receptors of the heart and upper gastrointestinal tract (M2 subtype)."( Characterization of muscarinic receptors of the rabbit ear artery smooth muscle and endothelium.
Banner, W; Duckles, SP; Hynes, MR; Yamamura, HI, 1986
)
0.99

Actions

Pirenzepine reduces lower esophageal sphincter pressure (LESP), amplitude, and duration of contractions. It increases velocity of propagation of esophagal contractions in patients with chronic heart failure. PirenZepine inhibited the increase in pulmonary inflation pressure more than atropine.

ExcerptReferenceRelevance
"Pirenzepine reduces lower esophageal sphincter pressure (LESP), amplitude, and duration of esophageal contractions, but it increases velocity of propagation of esophageal contractions."( The effect of pirenzepine on esophageal motility.
Berges, W; Erckenbrecht, E; Erckenbrecht, J; Sonnenberg, A; Wienbeck, M, 1982
)
1.35
"Pirenzepine was found to cause a significant increase in the R-R interval from 903+/-112 to 956+/-129 ms in the control group (P<0.0001) and from 927+/-141 to 958+/-168 ms in patients with chronic heart failure (P<0.01)."( Paradoxical effects of pirenzepine on parasympathetic activity in chronic heart failure and control.
Furutani, Y; Hayano, T; Ikeda, Y; Matsuzaki, M; Shimizu, A; Ueyama, T; Yamagata, T; Yamamoto, T, 1999
)
1.34
"Pirenzepine inhibited the increase in pulmonary inflation pressure more than atropine."( [Effect of atropine and pirenzepine on bronchoconstriction during vagus nerve stimulation in dogs].
Kawamoto, M; Kawasaki, H; Shiraishi, S; Takasaki, M, 1992
)
1.31
"Pirenzepine did, however, enhance the antisecretory effect of ranitidine after both sham feeding and food ingestion."( The cephalic and gastric phases of gastric secretion during H2-antagonist treatment.
Halter, F; Merki, HS; Walt, RP; Wilder-Smith, CH, 1991
)
1
"Pirenzepine at lower doses (0.3-3 microgram/kg i.v.) attenuated the stimulation of the negative chronotropic response to the intracardiac parasympathetic nerves to the sinoatrial nodal region to 80% of the control response significantly but did not affect the negative dromotropic one."( Functional participation in M1 receptor subtype on chronotropic and dromotropic responses to vagus stimulation in anesthetized dogs.
Chiba, S; Furukawa, Y; Karasawa, Y; Murakami, M; Narita, M; Ren, LM; Takei, M, 1991
)
1

Treatment

Pirenzepine treatment in traumatized rats displayed similar anxiety indices of non-traumatized rats treated with physiological saline. Pretreatment with pirenZepine (40 mg given iv 10 min before TRH) suppressed the TRH-induced GH rise.

ExcerptReferenceRelevance
"Pirenzepine pretreatment reduced while AF-DX116 enhanced expression of SOCS3 at mRNA level."( Muscarinic M1 and M2 receptor subtypes play opposite roles in LPS-induced septic shock.
Geng, B; Li, M; Liu, L; Wang, Z, 2019
)
1.24
"Pirenzepine treatment in traumatized rats displayed similar anxiety indices of non-traumatized rats treated with physiological saline."( Increased noradrenaline levels in the rostral pons can be reversed by M1 antagonist in a rat model of post-traumatic stress disorder.
Aydın, B; Cabadak, H; Gören, MZ; Kaleli, M; Ketenci, S; Terzioğlu, B, 2013
)
1.11
"Pirenzepine-treated patients consumed significantly fewer antacid tablets."( Pirenzepine in duodenal ulcer. A six week, double-blind study.
Daniotti, S; Do, D; Martelli, S, 1982
)
2.43
"Pirenzepine treatment did not change the level of gastrin mRNA but significantly increased the level of somatostatin mRNA."( Effects of pirenzepine on omeprazole-induced gastrin gene expression in rat antral tissues.
Fukino, Y; Hamada, M; Kajiyama, G; Kamiyasu, T; Sumii, K; Sumii, M; Tari, A, 1996
)
1.41
"Pirenzepine treatment suppressed omeprazole-induced increases in serum gastrin levels and mRNA levels of H+-K+-ATPase and histidine decarboxylase. "( Effects of omeprazole and pirenzepine on enterochromaffin-like cells and parietal cells in rat stomach.
Kajiyama, G; Kuruhara, Y; Okahara, S; Sumii, K; Tari, A; Yamauchi, R; Yonei, Y, 2001
)
2.05
"Pirenzepine pretreatment effectively blocked the carbachol-induced, REM sleep-like state and attendant changes in muscle tone."( State-dependent hypotonia in posterior cricoarytenoid muscles of the larynx caused by cholinoceptive reticular mechanisms.
Baghdoyan, HA; Lydic, R; Zwillich, CW, 1989
)
1
"Pirenzepine treatment prevented any subsequent DEPC inhibitory effect."( Pirenzepine prevents diethyl pyrocarbonate inhibition of central CO2 sensitivity.
Mills, JW; Nattie, EE; Ou, LC, 1988
)
2.44
"Pretreatment with pirenzepine increased the sensitivity of rats with acute massive hemorrhage to circulatory hypoxia."( Selective blockade of central m1 muscarinic cholinergic receptors with pirenzepine impairs cardiovascular and respiratory function in rats with acute hemorrhage.
Kovalenko, NY; Matsievskii, DD, 2006
)
0.89
"Pretreatment with pirenzepine (40 mg given iv 10 min before TRH) suppressed the TRH-induced GH rise."( The growth hormone response to thyrotropin-releasing hormone in insulin-dependent diabetics involves a cholinergic mechanism.
Butturini, U; Capretti, L; Chiodera, P; Coiro, V; Muzzetto, P; Speroni, G; Volpi, R, 1984
)
0.59
"Pretreatment with pirenzepine significantly attenuated the GH response to GHRH analogue (552 (64-1274) mU/l/min in controls vs 305 (134-2726) mU/l/min in irradiated group)."( Radiation and neuroregulatory control of growth hormone secretion.
Ogilvy-Stuart, AL; Shalet, SM; Wallace, WH, 1994
)
0.61
"Pretreatment with pirenzepine (100 mg p.o."( Muscarinic cholinergic mediation of the GH response to gamma-hydroxybutyric acid: neuroendocrine evidence in normal and parkinsonian subjects.
Caffarra, P; Chiodera, P; Coiro, V; Malvezzi, L; Saginario, A; Scaglioni, A; Volpi, R, 2000
)
0.63
"Pretreatment with pirenzepine did not modify this response."( Pirenzepine inhibits growth hormone, but not thyrotropin response to thyrotropin-releasing hormone in patients with endogenous depression.
Chiodera, P; Coiro, V; De Ferri, A; Delsignore, R; Gnudi, A; Govi, AM; Marchesi, C; Mosti, A, 1987
)
2.04
"Treatment with pirenzepine neither altered basal blood glucose levels nor affected glucose tolerance after the injection of the glucose load."( Muscarinic cholinergic modulation of insulin response to an intravenous glucose tolerance test in normal man.
Butturini, U; Camellini, L; Chiodera, P; Coiro, V; d'Amato, L; Pignatti, D; Rossi, G; Volpi, R, 1986
)
0.61

Toxicity

Pirenzepine is effective and relatively safe in slowing the progression of myopia during a 1-year treatment period. A side effect encountered was sinus tachycardia in 4 of 27 patients treated with pirenzEpine.

ExcerptReferenceRelevance
" These drugs can also induce toxic effects in the liver."( Side effects of stress bleeding prophylaxis.
Tryba, M, 1989
)
0.28
"8 nmol/mg for pirenzepine and 71 nmol/mg for chloroquine, a compound which has been described as provoking toxic side-effects in melanin-containing tissues and adjacent structures."( Melanosome binding and oxidation-reduction properties of synthetic L-dopa-melanin as in vitro tests for drug toxicity.
Debing, I; Ijzerman, AP; Vauquelin, G, 1988
)
0.64
" A side effect encountered was sinus tachycardia in 4 of 27 patients treated with pirenzepine."( [Prevention of gastroduodenal stress lesions with secretion inhibitors in accident patients needing intensive care: incidence of lesions and adverse effects; consequences].
Barandun, J; Frutiger, A; Kobler, E; Leutenegger, A; Rüedi, T, 1985
)
0.49
" Thus, pirenzepine provides good results in double-contrast studies (equal to SMB), while presenting no adverse effects."( Usefulness and safety of pirenzepine in double-contrast study of upper gastrointestinal tract: comparison with scopolamine methylbromide.
Bartolozzi, C; Boraschi, P; Braccini, G; Falaschi, F; Marraccini, P; Marrucci, A; Testa, R,
)
0.89
" It does not appear to be free of adverse effects on liver function."( First clinical experience with olanzapine (LY 170053): results of an open-label safety and dose-ranging study in patients with schizophrenia.
Baldwin, DS; Montgomery, SA, 1995
)
0.29
" Considerable progress has been made in improving the motor side effect profile with the advent of clozapine and risperidone."( Side effect profiles of new antipsychotic agents.
Casey, DE, 1996
)
0.29
" Significant adverse events included somnolence, weight gain, and asymptomatic treatment-emergent transaminase elevation."( Safety of olanzapine.
Beasley, CM; Tollefson, GD; Tran, PV, 1997
)
0.3
"Most traditional neuroleptics have a narrow therapeutic-to-toxic index, and thus, the novel antipsychotics are the result of a search to substantially widen the distance between the dose that treats psychosis and the one that produces adverse effects."( The relationship of pharmacology to side effects.
Casey, DE, 1997
)
0.3
" Neutrophils from two patients with a history of clozapine-induced agranulocytosis seemed to be more sensitive to the toxic effects of the clozapine reactive metabolite; however, the numbers are too small to draw any definite conclusions."( A comparison of the oxidation of clozapine and olanzapine to reactive metabolites and the toxicity of these metabolites to human leukocytes.
Gardner, I; MacCrimmon, D; Uetrecht, JP; Zahid, N, 1998
)
0.3
" Thus, clinicians should address patients' concerns about adverse effects and attempt to choose medications that will improve their patients' quality of life as well as overall health."( Adverse effects of the atypical antipsychotics. Collaborative Working Group on Clinical Trial Evaluations.
, 1998
)
0.3
" The side effects associated with traditional antipsychotic treatment are generally minimal in patients who take risperidone, a combined 5-HT2/D2 antagonist, but the literature is sparse on adverse events among the newer atypical antipsychotics."( Risperidone side effects.
Conley, RR, 2000
)
0.31
" Compared with traditional agents, olanzapine shows only a few adverse events such as dry mouth, sedation, and increase in appetite."( Adverse events related to olanzapine.
Conley, RR; Meltzer, HY, 2000
)
0.31
" Their adverse effects, which include extrapyramidal side effects, tardive dyskinesia, weight gain, sedation, and sexual dysfunction, often lead to non-compliance; their use may have a negative impact on the overall course of illness; and they may not be as effective as lithium in treating the core manic symptoms over the long term."( Antipsychotic drug side effect issues in bipolar manic patients.
Zarate, CA, 2000
)
0.31
" Safety was evaluated through the collection of spontaneous adverse events and a specific questionnaire for extrapyramidal symptoms."( The safety of olanzapine compared with other antipsychotic drugs: results of an observational prospective study in patients with schizophrenia (EFESO Study). Pharmacoepidemiologic Study of Olanzapine in Schizophrenia.
Antón Saiz, C; Breier, A; Fontova Carbonell, E; Gómez, JC; Hernández, J; Ruiz Carrasco, P; Sacristán, JA, 2000
)
0.31
" Overall incidence of adverse events was significantly lower in the olanzapine group compared with the control group (p < ."( The safety of olanzapine compared with other antipsychotic drugs: results of an observational prospective study in patients with schizophrenia (EFESO Study). Pharmacoepidemiologic Study of Olanzapine in Schizophrenia.
Antón Saiz, C; Breier, A; Fontova Carbonell, E; Gómez, JC; Hernández, J; Ruiz Carrasco, P; Sacristán, JA, 2000
)
0.31
"These results show that olanzapine is safe and effective in nonselected schizophrenic outpatients and are consistent with the efficacy and safety profile that olanzapine has shown in previous controlled clinical trials."( The safety of olanzapine compared with other antipsychotic drugs: results of an observational prospective study in patients with schizophrenia (EFESO Study). Pharmacoepidemiologic Study of Olanzapine in Schizophrenia.
Antón Saiz, C; Breier, A; Fontova Carbonell, E; Gómez, JC; Hernández, J; Ruiz Carrasco, P; Sacristán, JA, 2000
)
0.31
" Olanzapine seems to be safe in this patient, since no major decreases of haematological parameters were observed."( Olanzapine appears haematologically safe in patients who developed blood dyscrasia on clozapine and risperidone.
Dernovsek, MZ; Tavcar, R, 2000
)
0.31
" Although the incidence of serious adverse cardiac events in response to antipsychotic medications is relatively low, any possibility for the occurrence of cardiotoxicity warrants continued study."( Cardiac safety parameters of olanzapine: comparison with other atypical and typical antipsychotics.
Beasley, CM; Czekalla, J; Kollack-Walker, S, 2001
)
0.31
" These findings suggest that intramuscular olanzapine is a safe and effective treatment for reducing acute agitation in patients with bipolar mania."( A double-blind, randomized comparison of the efficacy and safety of intramuscular injections of olanzapine, lorazepam, or placebo in treating acutely agitated patients diagnosed with bipolar mania.
Breier, A; David, S; Janicak, P; Koch, M; Meehan, K; Rizk, R; Small, J; Tohen, M; Tran, P; Walker, D; Zhang, F, 2001
)
0.31
" We conducted a survey of Spanish psychiatrists in mental health centers and outpatient treatment units to assess the severity scores that they would assign to a list of the most common adverse events (AEs) that usually occur with antipsychotic treatment."( Global index of safety (GIS): a new instrument to assess drug safety.
Badía, X; Gómez, JC; Kind, P; Sacristán, JA, 2001
)
0.31
"In vitro receptor characterization methods, when done using physiologically relevant conditions allow accurate prediction of the relatively low rate of anticholinergic-like adverse events, extrapyramidal symptoms, and cardiovascular adverse events during treatment with OLZ."( A current review of olanzapine's safety in the geriatric patient: from pre-clinical pharmacology to clinical data.
Baker, RW; Beasley, CM; Bernauer, M; Breier, A; Bymaster, FP; Calligaro, DO; Dossenbach, M; Effron, MB; Felder, CC; Hay, D; Holcombe, JH; Kaiser, C; Kennedy, JS; Kinon, BJ; Nomikos, G; Roth, HJ; Schuh, L, 2001
)
0.31
"Converging evidence indicates that, in controlled drug trials, individuals receiving novel antipsychotic medications have fewer adverse effects than those receiving conventional antipsychotic medications."( Short report: comparison of patient satisfaction and burden of adverse effects with novel and conventional neuroleptics: a naturalistic study.
Bromet, EJ; Davidson, M; Rabinowitz, J, 2001
)
0.31
"Psychopharmacology research aims to expand the therapeutic ratio between efficacy, on the one hand, and adverse events and safety, on the other."( Psychotropic drugs and adverse events in the treatment of bipolar disorders revisited.
McIntyre, RS, 2002
)
0.31
" Relatively little information on adverse events (AEs), specifically in children or adolescents taking atypical antipsychotics, is available."( Effects of development on olanzapine-associated adverse events.
Martin, A; McGlashan, TH; Spector, SG; Woods, SW, 2002
)
0.31
" Safety was assessed through the collection of spontaneous adverse events and a specific extrapyramidal symptoms questionnaire (EPS)."( Safety of olanzapine versus conventional antipsychotics in the treatment of patients with acute schizophrenia. A naturalistic study.
Alvarez, E; Bobes, J; Cañas, F; Carrasco, JL; Gascón, J; Gibert, J; Gómez, JC; Gutiérrez, M; Sacristán, JA, 2003
)
0.32
" Other safety and tolerability endpoints included spontaneous adverse event reporting and changes from baseline in laboratory measures and vital signs."( A comparison of the efficacy, safety, and tolerability of divalproex sodium and olanzapine in the treatment of bipolar disorder.
Sachs, G; Sommerville, KW; Swann, AC; Weisler, R; Wozniak, P; Zajecka, JM, 2002
)
0.31
"05) greater proportion of olanzapine-treated subjects experienced somnolence, weight gain, edema, rhinitis, and speech disorder (slurred speech); no adverse events were significantly greater in the divalproex group."( A comparison of the efficacy, safety, and tolerability of divalproex sodium and olanzapine in the treatment of bipolar disorder.
Sachs, G; Sommerville, KW; Swann, AC; Weisler, R; Wozniak, P; Zajecka, JM, 2002
)
0.31
" Divalproex was associated with a more favorable adverse event profile and significantly less weight gain than olanzapine."( A comparison of the efficacy, safety, and tolerability of divalproex sodium and olanzapine in the treatment of bipolar disorder.
Sachs, G; Sommerville, KW; Swann, AC; Weisler, R; Wozniak, P; Zajecka, JM, 2002
)
0.31
" Olanzapine is one of the atypical antipsychotics with efficacy for psychotic symptoms and a safer side-effect profile than typical antipsychotics."( The efficacy and safety of olanzapine for the treatment of geriatric psychosis.
Hwang, JP; Lee, TW; Tsai, SJ; Yang, CH, 2003
)
0.32
" Safety was evaluated in terms of the spontaneous adverse events reported and a specific questionnaire for extrapyramidal symptoms (EPS)."( Safety and effectiveness of olanzapine versus conventional antipsychotics in the acute treatment of first-episode schizophrenic inpatients.
Alvarez, E; Bobes, J; Cañas, F; Carrasco, JL; Ciudad, A; Gascón, J; Gibert, J; Gómez, JC; Gutiérrez, M, 2003
)
0.32
"The results of this observational, naturalistic study show that olanzapine is safe and effective in a nonselected sample of acute, first-episode schizophrenic inpatients."( Safety and effectiveness of olanzapine versus conventional antipsychotics in the acute treatment of first-episode schizophrenic inpatients.
Alvarez, E; Bobes, J; Cañas, F; Carrasco, JL; Ciudad, A; Gascón, J; Gibert, J; Gómez, JC; Gutiérrez, M, 2003
)
0.32
" This is because of their efficacy in the treatment of several psychiatric disorders, ease of administration, and absence of the well-known extrapyramidal adverse effects long-attributed to the standard dopamine blocking anti-psychotic medications."( Atypical psychotropic medications and their adverse effects: a review for the African-American primary care physician.
Bailey, RK, 2003
)
0.32
"To assess the adverse events associated with the appropriate use of oral risperidone and oral olanzapine in long-term care patients with behavioral and psychotic disturbances associated with dementia."( Safety profile assessment of risperidone and olanzapine in long-term care patients with dementia.
Cornacchione, MJ; Deymann, S; Martin, H; Slyk, MP,
)
0.13
" Adverse events of particular significance in the elderly population, including agitation/anxiety, laxative use, dry eyes, and falls, were collected from audited medical records."( Safety profile assessment of risperidone and olanzapine in long-term care patients with dementia.
Cornacchione, MJ; Deymann, S; Martin, H; Slyk, MP,
)
0.13
"Among long-term care residents with dementia who received low doses of risperidone or olanzapine, the incidence of adverse events was low."( Safety profile assessment of risperidone and olanzapine in long-term care patients with dementia.
Cornacchione, MJ; Deymann, S; Martin, H; Slyk, MP,
)
0.13
" Adverse events and scores on EPS rating scales were assessed."( A comparison of the efficacy and safety of olanzapine versus haloperidol during transition from intramuscular to oral therapy.
Birkett, M; Breier, A; Lindborg, SR; Meehan, K; Morris, P; Taylor, CC; Wright, P, 2003
)
0.32
" Although the nature of adverse events differed between the two agents, retention in the study was greater with olanzapine."( Comparative efficacy and safety of atypical and conventional antipsychotic drugs in first-episode psychosis: a randomized, double-blind trial of olanzapine versus haloperidol.
Green, AI; Gur, RE; Hamer, RM; Kahn, R; Lieberman, JA; McEvoy, J; Perkins, D; Sharma, T; Tohen, M; Tollefson, G; Wei, H; Zipursky, R, 2003
)
0.32
"Available toxicity data concerning olanzapine were obtained from the Offices of the Medical Examiners of Canada, the Canadian Adverse Drug Reaction Monitoring Program and a review of the literature."( A review of olanzapine-associated toxicity and fatality in overdose.
Chue, P; Singer, P, 2003
)
0.32
" Early signal detection and effective notification processes are crucial in the event that serious adverse effects do occur."( A review of olanzapine-associated toxicity and fatality in overdose.
Chue, P; Singer, P, 2003
)
0.32
" Divalproex loading was as well tolerated or better tolerated than the other active treatments as measured by adverse events and changes in laboratory parameters."( The safety and early efficacy of oral-loaded divalproex versus standard-titration divalproex, lithium, olanzapine, and placebo in the treatment of acute mania associated with bipolar disorder.
Baker, JD; Hirschfeld, RM; Sommerville, KW; Tracy, K; Wozniak, P, 2003
)
0.32
" Statistically significant differences of mean change of BAS total score from baseline to endpoint were noted between treatment groups Treatment--emergent adverse events occurred more frequently in patients receiving perphenazine (46%), than in patients receiving olanzapine (17%)."( [Safety and efficacy of olanzapine versus perphenazine in patients with schizophrenia: results of multicenter, 18-week, double-blind clinical trial].
Araszkiewicz, A; Bilikiewicz, A; Bomba, J; Chrzanowski, W; Debowska, G; Jarema, M; Landowski, J; Olajossy, M; Rybakowski, J,
)
0.13
" Safety was assessed via adverse events, vital signs, laboratory analytes, electrocardiography, and extrapyramidal symptom measures."( Long-term antidepressant efficacy and safety of olanzapine/fluoxetine combination: a 76-week open-label study.
Andersen, SW; Corya, SA; Detke, HC; Dubé, S; Kelly, LS; Sanger, TM; Van Campen, LE; Williamson, DJ, 2003
)
0.32
" The most frequently reported adverse events were somnolence, weight gain, dry mouth, increased appetite, and headache."( Long-term antidepressant efficacy and safety of olanzapine/fluoxetine combination: a 76-week open-label study.
Andersen, SW; Corya, SA; Detke, HC; Dubé, S; Kelly, LS; Sanger, TM; Van Campen, LE; Williamson, DJ, 2003
)
0.32
"Hypersalivation is known as a frequent, disturbing, and socially stigmatizing side effect of therapy with the atypical antipsychotic clozapine."( Reduction of clozapine-induced hypersalivation by pirenzepine is safe.
Fritze, J; Hiemke, C; Schneider, B; Weber, B; Weigmann, H, 2004
)
0.58
" No patients in the placebo group and 13 (11%) of 117 patients in the pirenzepine group discontinued participation in the study because of adverse effects (5 [4%] of 117 due to excessive antimuscarinic effects)."( Safety and efficacy of 2% pirenzepine ophthalmic gel in children with myopia: a 1-year, multicenter, double-masked, placebo-controlled parallel study.
Cotter, S; Crockett, RS; Miller, JM; Novack, GD; Scher, CA; Siatkowski, RM, 2004
)
0.86
"Pirenzepine is effective and relatively safe in slowing the progression of myopia during a 1-year treatment period."( Safety and efficacy of 2% pirenzepine ophthalmic gel in children with myopia: a 1-year, multicenter, double-masked, placebo-controlled parallel study.
Cotter, S; Crockett, RS; Miller, JM; Novack, GD; Scher, CA; Siatkowski, RM, 2004
)
2.07
" Discontinued from the study for adverse events were 11% (31/282) of pirenzepine-treated subjects."( One-year multicenter, double-masked, placebo-controlled, parallel safety and efficacy study of 2% pirenzepine ophthalmic gel in children with myopia.
Chua, WH; Crockett, RS; Lam, DS; Shu-Ping, DF; Tan, DT, 2005
)
0.78
"Gel (2% twice daily) was effective and relatively safe in slowing the progression of myopia over a 1-year treatment period."( One-year multicenter, double-masked, placebo-controlled, parallel safety and efficacy study of 2% pirenzepine ophthalmic gel in children with myopia.
Chua, WH; Crockett, RS; Lam, DS; Shu-Ping, DF; Tan, DT, 2005
)
0.55
" Thirteen (11%) pirenzepine patients dropped out due to adverse effects in the first year, and 1 did so in the second year."( Two-year multicenter, randomized, double-masked, placebo-controlled, parallel safety and efficacy study of 2% pirenzepine ophthalmic gel in children with myopia.
Cotter, SA; Crockett, RS; Miller, JM; Novack, GD; Siatkowski, RM; Zadnik, K, 2008
)
0.9

Pharmacokinetics

Pirenzepine had no significant effect on plasma paracetamol Cmax. renal clearance, total clearance and terminal (dominant) half-life were found to be correlated with the creatinine clearance (CLCR)

ExcerptReferenceRelevance
"This paper gives a brief review of the pharmacokinetic studies performed on pirenzepine (L S 519 Cl2, Gastrozepin hitherto."( The pharmacokinetic profile of pirenzepine.
Hammer, R; Koss, FW, 1979
)
0.78
" Pirenzepine had no significant effect on plasma paracetamol Cmax (17."( The effect of pirenzepine on gastric emptying and salivary flow rate: constraints on the use of saliva paracetamol concentrations for the determination of paracetamol pharmacokinetics.
Edwards, C; Kamali, F; Rawlins, MD, 1992
)
1.55
" tmax and cmax remained unchanged."( [Pharmacokinetics and tolerability of telenzepine in patients with compensated liver cirrhosis].
Dammann, HG; Müller, P; Reinicke, A; Simon, B, 1990
)
0.28
"The individual variations in the blood concentrations of gastrocepine, the period of its half-life and clearance in patients with peptic ulcers of the stomach and the duodenal bulb were determined."( [The characteristics of gastrozepin pharmacokinetics in patients with gastric and duodenal peptic ulcers].
Bendikov, EA; Giliadova, LA; Loginov, AS; Sil'vestrova, SIu,
)
0.13
"The pharmacokinetic properties of pirenzepine following administration of a single, 50 mg oral dose were evaluated in three groups of subjects: group I, end stage renal disease requiring maintenance haemodialysis (CLCR 0 to 10 ml."( Oral pharmacokinetics of pirenzepine in patients with chronic renal insufficiency, failure, and maintenance haemodialysis.
Chonko, A; Keirns, J; MacGregor, T; Matzek, K; Vinocur, M, 1990
)
0.86
"The pharmacokinetic parameters of muscarinic cholinergic drugs after intravenous (IV) and oral administration to mice was determined with ex vivo (3H)-oxotremorine-M (3H-Oxt) binding to the brain."( Pharmacokinetics of muscarinic cholinergic drugs as determined by ex vivo (3H)-oxotremorine-M binding.
Francis, JW; Sethy, VH, 1990
)
0.28
" Pirenzepine renal clearance, total clearance and terminal (dominant) half-life were found to be correlated with the creatinine clearance (CLCR), but this was not the case for the volume of distribution and the nonrenal clearance."( Steady-state intravenous pharmacokinetics of pirenzepine in patients with differing degrees of renal dysfunction.
Bozler, G; Krakamp, B; Tanswell, P; Vogel, H, 1989
)
1.45
"The possible pharmacokinetic interactions between pirenzepin and theophylline were investigated in an open single blind trial."( Pirenzepin does not alter the pharmacokinetics of theophylline.
Meryn, S; Rameis, H; Sertl, K, 1987
)
0.27
"0 ng/ml), and decreased bi-phasically with an elimination half-life (t1/2 beta) of 13."( Pharmacokinetics of pirenzepine in patients with gastric or duodenal ulcers.
Bozler, G; Hayakawa, A; Kobayashi, S; Misawa, T; Nishihara, S, 1987
)
0.6
" A 3-compartment model was taken as a basis for the calculation of the plasma concentration curves and the pharmacokinetic parameters."( Pharmacokinetics and bioequivalence of different formulations of pirenzepine.
Mascher, H; Nitsche, V; Strobel, K; Vergin, H, 1986
)
0.51
" The possibility of a pharmacokinetic interaction between these drugs was examined in eight patients who received cimetidine and PRZ alone and in combination in a crossover fashion."( Lack of pharmacokinetic interaction between cimetidine and pirenzepine.
Jamali, F; Mahachai, V; Reilly, PA; Thomson, AB, 1985
)
0.51
" The mean terminal half-life of disposition was 11 hours."( An international pharmacokinetic study on pirenzepine following a single oral dose.
Bozler, G; Hammer, R, 1980
)
0.53
"The pharmacodynamic properties of meloxicam, a new nonsteroidal antiinflammatory drug (NSAID), that go beyond those typical of an NSAID were examined."( General pharmacology of meloxicam--Part II: Effects on blood pressure, blood flow, heart rate, ECG, respiratory minute volume and interactions with paracetamol, pirenzepine, chlorthalidone, phenprocoumon and tolbutamide.
Engelhardt, G; Homma, D; Schlegel, K; Schnitzler, C; Utzmann, R, 1996
)
0.49
" The purpose of the present study was to assess the potential for a pharmacokinetic interaction between olanzapine and carbamazepine, since these agents are likely to be used concomitantly in the treatment of manic psychotic disorder."( A pharmacokinetic interaction between carbamazepine and olanzapine: observations on possible mechanism.
Bergstrom, RF; Gilfillan, DJ; Lucas, RA, 1998
)
0.3
" Olanzapine pharmacokinetic values for Cmax and AUC were significantly lower after the second dose, the elimination half-life was significantly shorter, and the clearance and volume of distribution were significantly increased."( A pharmacokinetic interaction between carbamazepine and olanzapine: observations on possible mechanism.
Bergstrom, RF; Gilfillan, DJ; Lucas, RA, 1998
)
0.3
" Its mean half-life in healthy individuals was 33 hours, ranging from 21 to 54 hours."( Olanzapine. Pharmacokinetic and pharmacodynamic profile.
Beasley, CM; Bergstrom, RF; Callaghan, JT; Ptak, LR, 1999
)
0.3
" Blood samples, collected during dose titration and at a steady state provided pharmacokinetic data."( Olanzapine pharmacokinetics in pediatric and adolescent inpatients with childhood-onset schizophrenia.
Bergstrom, RF; Calis, KA; DeVane, CL; Grothe, DR; Jacobsen, L; Kumra, S; Kurtz, DL; Rapoport, JL, 2000
)
0.31
" Its pharmacokinetic properties are comparable to those of classical antipsychotics."( [Olanzapine: pharmacology, pharmacokinetics and therapeutic drug monitoring].
Baumann, P; Grasmäder, K; Hiemke, C; Rao, ML, 2001
)
0.31
" The purpose of this study was to assess the potential for pharmacokinetic interaction between olanzapine and fluoxetine, a popular antidepressant that is a selective serotonin reuptake inhibitor."( Influence of fluoxetine on olanzapine pharmacokinetics.
de Suray, JM; Gangji, D; Gossen, D; Onkelinx, C; Vandenhende, F, 2002
)
0.31
" We compared olanzapine noncompartmental pharmacokinetic parameter values before and after ritonavir with a paired Student t test."( Influence of ritonavir on olanzapine pharmacokinetics in healthy volunteers.
Hon, YY; Jann, MW; Lawhorn, WD; Penzak, SR; Shirley, KL; Spratlin, V, 2002
)
0.31
" In this study, pharmacokinetic interactions and clinical effects of adding the CYP1A2 inhibitor fluvoxamine to steady-state olanzapine was examined in patients suffering from schizophrenia."( Fluvoxamine augmentation of olanzapine in chronic schizophrenia: pharmacokinetic interactions and clinical effects.
Hadjez, J; Härtter, S; Hiemke, C; Jabarin, M; Modai, I; Peled, A; Ritsner, M; Silver, H; Weigmann, H, 2002
)
0.31
"To compare the pharmacokinetic profiles and dose proportionality of olanzapine in Chinese and Caucasian subjects."( Olanzapine pharmacokinetics are similar in Chinese and Caucasian subjects.
Bergstrom, RF; Chan, C; Sathirakul, K; Teng, L; Wise, SD; Yeo, KP, 2003
)
0.32
" Noncompartmental pharmacokinetic parameters were derived."( Olanzapine pharmacokinetics are similar in Chinese and Caucasian subjects.
Bergstrom, RF; Chan, C; Sathirakul, K; Teng, L; Wise, SD; Yeo, KP, 2003
)
0.32

Compound-Compound Interactions

Serum gastrin levels in 44 peptic ulcer patients were determined after they had been treated with omeprazole. Ulceration healed up within 2 weeks in 40% of patients treated with cimetidine combined with pirenzepine.

ExcerptReferenceRelevance
" Ulceration healed up within 2 weeks in 40% of patients treated with cimetidine combined with pirenzepine and in 31."( [Comparison of the results of the treatment with pirenzepine combined with cimetidine and sucralfate of stomach ulcer resistant to cimetidine].
Janke, A; Kozuszyńska, M; Namiot, Z; Stasiewicz, J; Szałaj, W,
)
0.6
"Serum gastrin levels in 44 peptic ulcer patients (26 gastric ulcer patients and 18 duodenal ulcer patients) were determined after they had been treated with omeprazole (OPZ) (20 mg/day) alone or in combination with pirenzepine (PZP) (100 mg/day)."( Serum gastrin levels following administration of omeprazole alone or in combination with pirenzepine.
Arakawa, Y; Ito, K; Iwasaki, A; Kawamura, Y; Matsuo, Y; Miyazawa, K; Sakai, Y; Tashiro, Y, 1994
)
0.7
"To understand the mechanism of the clinical efficacy of olanzapine and fluoxetine combination therapy for treatment-resistant depression (TRD), we studied the effects of olanzapine and other antipsychotics in combination with the selective serotonin uptake inhibitors fluoxetine or sertraline on neurotransmitter release in rat prefrontal cortex (PFC) using microdialysis."( Synergistic effects of olanzapine and other antipsychotic agents in combination with fluoxetine on norepinephrine and dopamine release in rat prefrontal cortex.
Bao, J; Bymaster, FP; Perry, KW; Potts, BD; Tollefson, GD; Wong, DT; Zhang, W, 2000
)
0.31
"This study examined the short-term efficacy of electroconvulsive therapy (ECT) combined with antipsychotic medication in treatment-resistant schizophrenia (TRS)."( Efficacy of electroconvulsive therapy combined with antipsychotic medication in treatment-resistant schizophrenia: a prospective, open trial.
Tang, WK; Ungvari, GS, 2002
)
0.31
" Treatment with divalproex in combination with an atypical antipsychotic agent resulted in earlier improvements in a range of psychotic symptoms among acutely hospitalized patients with schizophrenia."( Effect of divalproex combined with olanzapine or risperidone in patients with an acute exacerbation of schizophrenia.
Casey, DE; Daniel, DG; Sommerville, KW; Tracy, KA; Wassef, AA; Wozniak, P, 2003
)
0.32

Bioavailability

The effect of an antacid on the bioavailability of orally administered pirenzepine (Gastricur) was evaluated in 10 subjects in a double-blind single dose cross-over study. The antacid had no influence on theBioavailability of amoxicillin, cephalexin, and am toxicillin-clavulanic acid.

ExcerptReferenceRelevance
"The absolute bioavailability (f) of pirenzepine was determined in 27 intensive care patients receiving the drug for prophylaxis and therapy of upper gastrointestinal tract bleeding."( Absolute bioavailability of pirenzepine in intensive care patients.
Allmendinger, G; Bozler, G; Giesler, H; Hofgärtner, F; Schmid, E; Tanswell, P, 1990
)
0.85
" atropine and pirenzepine) and the results were compared with the bioavailability (i."( The mean cumulative fraction absorbed-time profiles of paracetamol as an index of gastric emptying.
Meyer, EC; Moncrieff, J; Sommers, DK; van Wyk, M, 1990
)
0.64
" The antacid, pirenzepine, and ranitidine had no influence on the bioavailability of amoxicillin, cephalexin, and amoxicillin-clavulanic acid."( Influence of ranitidine, pirenzepine, and aluminum magnesium hydroxide on the bioavailability of various antibiotics, including amoxicillin, cephalexin, doxycycline, and amoxicillin-clavulanic acid.
Deppermann, KM; Höffken, G; Kalz, C; Koeppe, P; Lode, H; Tschink, G, 1989
)
0.94
"The effect of an antacid containing aluminium-hydroxide, magnesium-hydroxide and calcium carbonate (Trigastril) on the bioavailability of orally administered pirenzepine (Gastricur) was evaluated in 10 subjects in a double-blind single dose cross-over study."( Effect of an aluminium-hydroxide containing antacid on the oral bioavailability of pirenzepine.
Gugler, R; Herrlinger, C; Vergin, H, 1989
)
0.7
"An intraindividual comparative single-dose study was carried out under carefully controlled conditions on 12 healthy volunteers in order to establish the bioavailability of 5,11-dihydro-11-[(4-methyl-piperazin-1- -yl)acetyl]-6H-pyrido[2,3b][1,4]benzodiazepin-6-one dihydrochloride (pirenzepine), the active principle of newly developed tablets (Gastricur) and suspension containing 10 mg."( Pharmacokinetics and bioequivalence of different formulations of pirenzepine.
Mascher, H; Nitsche, V; Strobel, K; Vergin, H, 1986
)
0.69
" It is often accepted that drugs or drug formulations with low bioavailability show high variations in the rates and extent of absorption."( An international pharmacokinetic study on pirenzepine following a single oral dose.
Bozler, G; Hammer, R, 1980
)
0.53
" Pyridostigmine had a higher elimination (2 h-1) than the absorption rate constant (0."( Renal clearance of pyridostigmine in myasthenic patients and volunteers under the influence of ranitidine and pirenzepine.
Breyer-Pfaff, U; Eiermann, B; Maier, U; Schumm, F; Sommer, N; Winne, D, 1993
)
0.5
" After oral administration, OLZ was well absorbed in dogs (absolute bioavailability of 73%) and to the extent of at least 55% in monkeys and 32% in mice."( Disposition and metabolism of olanzapine in mice, dogs, and rhesus monkeys.
Bernstein, J; Chiu, A; Franklin, R; Gillespie, T; Hotten, T; Kassahun, K; Mattiuz, E; Murphy, A, 1997
)
0.3
" The drug is well absorbed from the GI tract; food has no effect."( Olanzapine: a serotonin-dopamine-receptor antagonist for antipsychotic therapy.
Bever, KA; Perry, PJ, 1998
)
0.3
"The quantitative structure-bioavailability relationship of 232 structurally diverse drugs was studied to evaluate the feasibility of constructing a predictive model for the human oral bioavailability of prospective new medicinal agents."( QSAR model for drug human oral bioavailability.
Topliss, JG; Yoshida, F, 2000
)
0.31
" It may be less well absorbed and/or less effective than Clozaril, although evidence is conflicting."( Advances in atypical antipsychotics for the treatment of schizophrenia: new formulations and new agents.
Albert, MJ; Baldessarini, RJ; Centorrino, F; Kelleher, JP, 2002
)
0.31
" To assess the ocular bioavailability of pirenzepine, a HPLC method for determination of pirenzepine in rabbit aqueous humor was developed."( HPLC determination of pirenzepine dihydrochloride in rabbit aqueous humor.
Li, P; Pang, H; Tu, J; Yang, X, 2005
)
0.91
" To show the importance of physicochemical properties, the classic QSAR and CoMFA of neonicotinoids and prediction of bioavailability of pesticides in terms of membrane permeability in comparison with drugs are described."( Importance of physicochemical properties for the design of new pesticides.
Akamatsu, M, 2011
)
0.37
" We hypothesized that the inhibition of cholinesterase activity might increase acetylcholine bioavailability and consequently cholinoceptor activation, leading to concomitant adenosine release from nerve endings and skeletal muscle fibers."( Paradoxical neostigmine-induced TOFfade: on the role of presynaptic cholinergic and adenosine receptors.
Alves-Do-Prado, W; Ambiel, CR; Antônio, MB; Correia-de-Sá, P; de Paula Ramos, E, 2014
)
0.4
", 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
"5 times higher bioavailability was achieved by the addition of sorbic acid at a 1:1 ratio."( Ion-paired pirenzepine-loaded micelles as an ophthalmic delivery system for the treatment of myopia.
Li, P; Li, Y; Mi, G; Shen, Y; Sun, L; Tu, J; Webster, TJ; Zhang, Y, 2017
)
0.84
"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

Dosage Studied

Pirenzepine and N-methylatropine have antimuscarinic potencies. Dose-response curves were shifted to the right by muscarinic antagonists in the following order of affinity: darifenacin (M)>methocramine (M(2) >pirenzepine (1)

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
" To see if this increase in LESP is due to upregulation of mAChR, we evaluated both mAChR binding and dose-response curves for bethanechol and atropine-induced changes in LESP before and after acute and chronic ethanol exposure."( Chronic ethanol feeding produces a muscarinic receptor upregulation, but not a muscarinic supersensitivity in lower esophageal sphincter muscle.
Fields, JZ; Gordon, JH; Keshavarzian, A; Urban, G; Willson, C, 1992
)
0.28
" Telenzepine (3 x 10(-8)-10(-5) M) concentration-dependently shifted to the right the dose-response curves of bethanechol, acetylcholine and McN-A343, and partially depressed the electrically-evoked twitch responses."( Antimuscarinic activity of telenzepine on isolated human urinary bladder: no role for M1-muscarinic receptors.
Bertaccini, G; Monica, B; Poli, E; Pozzoli, C; Zappia, L, 1992
)
0.28
" The muscarinic antagonists pirenzepine, (+-)-5,11-dihydro-11-[[[2-[2-((dipropylamino)methyl)-1-piperidinyl] ethyl]amino]-carbonyl]-6H-pyrido(2,3-b)(1,4)-benzodiazepin-6-one (AF-DX 384), 11-[[4-[4-(diethylamino)butyl]-1-piperidinyl]acetyl]-5,11-dihydro- 6H-pyrido(2,3-b)(1,4)-benzodiazepin-6-one (AQ-RA 741), p-fluorohexahydro-sila-difenidol (p-F-HHSiD), 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP) and (R)- and (S)-hexahydro-difenidol [(R)-HHD, (S)-HHD] shifted the muscarine, methacholine or carbachol dose-response curve to the right in a competitive manner."( Characterization of muscarinic receptors mediating vasodilation in guinea-pig ileum submucosal arterioles by the use of computer-assisted videomicroscopy.
Bungardt, E; Feifel, R; Lambrecht, G; Moser, U; Mutschler, E; Surprenant, A; Tacke, R; Vockert, E, 1992
)
0.58
" Log ID50s calculated for the antagonists from the dose-response curves were found to correlate significantly with the log Kis of the antagonists for the muscarinic M3 receptor subtype."( Pressor response to posterior hypothalamic administration of carbachol is mediated by muscarinic M3 receptor.
Martin, JR, 1992
)
0.28
" Dose-response curves showed that the parietal sheet was more sensitive to the physiological agonist (acetylcholine) than to carbachol."( Cholinergic effects on intracellular free calcium concentration in renal corpuscle: role of parietal sheet.
Lebrun, F; Marchetti, J; Morel, F; Vassent, G, 1992
)
0.28
" To obtain dose-response curves to inhaled pirenzepine, we measured partial and full flow-volume curves before and 30 min after inhalation of each concentration of pirenzepine (3."( Effect of a M1-selective muscarinic receptor antagonist (pirenzepine) on basal bronchomotor tone in young women.
Fujimura, M; Kamio, Y; Matsuda, T, 1992
)
0.79
" In tissues precontracted with methacholine, 11-([[2-(diethylamino)methyl]-1-piperidinyl]acetyl)5,11- dihydro-6H-pyrido[2,3-6][1,4]benzodiazepine-6-one (AF-DX 116), a selective M2 antagonist, shifted dose-response curves to both isoproterenol and forskolin significantly to the left."( M2 muscarinic receptors inhibit isoproterenol-induced relaxation of canine airway smooth muscle.
Fernandes, LB; Fryer, AD; Hirshman, CA, 1992
)
0.28
" Addition of the muscarinic antagonists atropine or pirenzepine shifted the carbachol dose-response curves to the right, without decreasing the carbachol maximal stimulatory effects."( Effects of muscarinic agonists and depolarizing agents on inositol monophosphate accumulation in the rabbit vagus nerve.
Dunant, Y; Sierro, CD; Vitus, J, 1992
)
0.53
" The dose-response relations of carbachol-induced cAMP synthesis and carbachol-induced rise in intracellular free Ca2+ were similar."( Muscarinic receptor-linked elevation of cAMP in SH-SY5Y neuroblastoma cells is mediated by Ca2+ and protein kinase C.
Akerman, KE; Jansson, CC; Kukkonen, J, 1991
)
0.28
"3 microM) shifted the dose-response curve to the right in a parallel manner."( Muscarinic receptor is coupled with a cation channel through a GTP-binding protein in guinea-pig chromaffin cells.
Inoue, M; Kuriyama, H, 1991
)
0.28
" Low concentrations of pirenzepine (10(-8) M), produced a rightward shift in the dose-response curve to McN, without inhibiting responses to carbachol."( Functional subtyping of muscarinic receptors on canine esophageal mucosa.
Donoff, B; Lad, R; Rangachari, PK, 1991
)
0.59
" Alinidine (10(-6) M) shifted the dose-response curves of acetylcholine and carbachol to the right, but it did not affect those for isosorbide dinitrate, isoproterenol and adenosine."( Anti-muscarinic effect of alinidine on acetylcholine-induced vasodilation in isolated and perfused dog coronary arteries.
Chiba, S; Furukawa, Y; Nakane, T, 1991
)
0.28
" Dose-response lines in response to the two agonists, expressed as percent maximal contraction, did not differ among the groups."( Muscarinic-receptor functioning in tracheas from normal and ovalbumin-sensitive guinea pigs.
Biggs, DF; Yang, ZJ, 1991
)
0.28
" Omeprazole, which suppresses acid very effectively, may be problematic in the critically ill, limited by its oral dosage form, acid-labile properties, and potential drug interactions."( Controlling gastric pH: the impact of newer agents on the critically ill patient.
Earnest, DL, 1990
)
0.28
" Characteristic dose-response curves for acetylcholine showing greater negative inotropic response with dose were seen."( The effects of AF-DX 116, a cardioselective muscarinic antagonist, on the negative inotropic action of acetylcholine.
Baskin, SI; Thomsen, RH, 1991
)
0.28
" Dose-response curves were constructed, and the IC50s determined for 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP), pirenzepine (PRZ) and 11-2[[2-[(diethylamino)methyl]-1-piperidinyl]acetyl]-5,11,-dihydro- 6H-pyrido[2,3-b] [1,4]benzodiazepin-6-one (AF-DX 116) were 72 nM, 385 nM, and 24 microM, respectively."( Activation of the pharmacologically defined M3 muscarinic receptor depolarizes hippocampal pyramidal cells.
Alger, BE; Pitler, TA, 1990
)
0.48
" After repeated dosing 3 patients displayed different kinetic behaviour resulting in higher values of AUC on day 14/15 in comparison to day 1/2."( [Pharmacokinetics and tolerability of telenzepine in patients with compensated liver cirrhosis].
Dammann, HG; Müller, P; Reinicke, A; Simon, B, 1990
)
0.28
" Therefore, we investigated in a dose-response fashion the inhibitory effect of the muscarinic cholinergic receptor antagonist pirenzepine on the GH responses to arginine infusion (30 g infused intravenously (IV) in 30 minutes), exercise (bicycle ergometer test at an intensity of 75 W for 30 minutes), or 1-44 GH-releasing hormone (GHRH) (1 microgram/kg in an IV bolus)."( Reduced sensitivity to pirenzepine-induced blockade of growth hormone responses to arginine, exercise, and growth hormone-releasing hormone in type I diabetic subjects.
Bianconi, L; Capretti, L; Coiro, V; Davoli, C; Fagnoni, F; Gardini, E; Maffei, ML; Passeri, M; Speroni, G; Volpi, R, 1990
)
0.8
" All the antagonists shifted the methacholine dose-response curve to the right in a parallel and concentration-dependent fashion, yielding Schild plots with slopes not significantly different from unity."( Characterization of the muscarinic receptor subtype involved in phosphoinositide metabolism in bovine tracheal smooth muscle.
Elzinga, CR; Meurs, H; Roffel, AF; Zaagsma, J, 1990
)
0.28
" Assuming that the binding of carbachol to one site (Site 1) increases [14C]aminopyrine accumulation but its binding to the other site (Site 2) reduces [14C]aminopyrine accumulation, we analysed the dose-response curves for the carbachol effects in the absence and presence of different concentrations of atropine, pirenzepine and AF-DX 116."( Carbachol-induced potentiation and inhibition of acid secretion by guinea pig gastric gland.
Haga, T; Honda, N; Ichiyama, A; Kajimura, M; Kaneko, E, 1990
)
0.45
" A multiple oral and intravenous dosage regimen and the times of blood sampling were adapted to individual conditions and treatment."( Absolute bioavailability of pirenzepine in intensive care patients.
Allmendinger, G; Bozler, G; Giesler, H; Hofgärtner, F; Schmid, E; Tanswell, P, 1990
)
0.57
" The dosing was either metoclopramide alone or combined with either neostigmine and pirenzepine or with neostigmine and atropine."( The effect of neostigmine on metoclopramide-induced aldosterone secretion after the administration of muscarinic antagonists in man.
Meyer, EC; Sommers, DK; van Wyk, M, 1990
)
0.5
" A reduction in dose or dosing frequency may be warranted only in end state renal disease (CLCR 0 to 10 ml."( Oral pharmacokinetics of pirenzepine in patients with chronic renal insufficiency, failure, and maintenance haemodialysis.
Chonko, A; Keirns, J; MacGregor, T; Matzek, K; Vinocur, M, 1990
)
0.58
" This inhibition resulted in a rightward shift in the dose-response curve for carbamylcholine-stimulated amylase secretion without altering the maximal increase in amylase secretion."( Comparative inhibitory effects of pirenzepine and atropine on cholinergic stimulation of exocrine and endocrine rat pancreas.
Baba, S; Fujii, M; Nakamura, T; Oka, T; Okabayashi, Y; Otsuki, M, 1985
)
0.55
" 4-DAMP (10(-9) to 10(-6) M) caused a progressive parallel rightward shift in the acetylcholine dose-response curve without a change in maximal amylase release."( Muscarinic receptor subtypes on rat pancreatic acini: secretion and binding studies.
Louie, DS; Owyang, C, 1986
)
0.27
" In the isolated acini, pirenzepine caused a concentration-dependent rightward shift in the dose-response curve for carbamylcholine-stimulated amylase secretion without altering the maximal increase."( Pirenzepine inhibits pancreatic exocrine secretion in the rat.
Baba, S; Fujii, M; Nakamura, T; Oka, T; Okabayashi, Y; Otsuki, M, 1986
)
2.02
" 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
)
0.89
" The shifts caused by atropine and pirenzepine in the dose-response curves for ACh were not parallel after in vitro treatment of the muscle with DFP."( Contractile responses of tracheal smooth muscle in organophosphate-treated swine: 2. Effects of antagonists.
Dwyer, TM; Farley, JM; Murali Mohan, P; Yang, CM, 1988
)
0.55
" Both slopes of the dose-response regression line are parallel in effect."( Effect of the radioprotector WR-2721 on operant behavior in the rat.
Lee, JD; Lee, SF; Lin, CH; Liu, WF; Ma, C; Shih, JH,
)
0.13
" In spite of the fact that there was a doubling of the density of M2 sites, no significant differences in dose-response curves for carbachol-induced inhibition of [3H]cAMP accumulation were observed in slices of CTX plus DH from control and l-atropine-treated rats."( Regulation of muscarinic receptor subtypes and their responsiveness in rat brain following chronic atropine administration.
Lee, W; Wolfe, BB, 1989
)
0.28
" The present study shows for the first time that the newly developed antimuscarinic drug telenzepine is in a single nocturnal dosage regimen (3 mg nocte) as effective as pirenzepine (50 mg bid) in the treatment of duodenal ulcer."( [Single evening administration of a new antimuscarinic agent telenzepine in therapy of acute duodenal ulcer. Results of a randomized double-blind comparative study versus pirenzepine].
Dammann, HG; Dreyer, M; Merk-Härtelt, B; Müller, P; Simon, B; Wolf, N, 1989
)
0.67
" It is concluded that once daily administration of 3 mg in the evening must be regarded as the optimal dosage regimen of telenzepine."( [Dose finding study of telenzepine (1.5 vs. 3 vs 5 mg once daily) in acute treatment of duodenal ulcer. A double-blind, randomized, multicenter parallel group comparison].
Hüttemann, W; Schneider, A, 1989
)
0.28
"The dose-response curve for the muscarine-induced depolarisation of the rat isolated superior cervical ganglion, studied over the concentration range of 3 nM-1 mM, was biphasic."( Biphasic dose-response curve to muscarine on the rat superior cervical ganglion.
Gilbert, MJ; Newberry, NR, 1989
)
0.28
" 4-DAMP, atropine, and pirenzepine caused a progressive parallel rightward shift in the dose-response curve of pancreatic secretion for bethanechol."( Subtypes of muscarinic receptors in pancreatic exocrine secretion in anesthetized dog.
Chiba, S; Haruta, K; Homma, N; Horiuchi, A; Iwatsuki, K; Yonekura, H, 1989
)
0.59
" Dose-response curves to carbachol, muscarine and oxotremorine were shifted to the right by gallamine and pirenzepine in a parallel manner with no change in maximal response ostensibly indicating simple competitive inhibition."( Pharmacologic discrimination between receptor heterogeneity and allosteric interaction: resultant analysis of gallamine and pirenzepine antagonism of muscarinic responses in rat trachea.
Boselli, C; Kenakin, T, 1989
)
0.7
" The dose-response relations for the increase in inositol phosphates closely paralleled the binding of carbachol to muscarinic receptors with a Km of 17 microM."( Stimulation of acid secretion and phosphoinositol production by rat parietal cell muscarinic M2 receptors.
Herz, A; Paumgartner, G; Pfeiffer, A; Rochlitz, H, 1988
)
0.27
" Pirenzepine caused a progressive parallel rightward shift in the dose-response curves for SLI inhibition and gastrin stimulation by carbachol, suggesting competitive inhibition."( Pirenzepine-sensitive muscarinic receptors regulate gastric somatostatin and gastrin.
Soll, AH; Sue, R; Todisco, A; Toomey, ML; Yamada, T, 1985
)
2.62
" The other five patients, who were free of complication, initially received a standard regimen of omeprazole 60 mg orally once a day; dosage was subsequently adjusted until the basal acid output, measured 1 hr before the next dose of the drug, was less than 10 mmol/hr."( Effectiveness of omeprazole in seven patients with Zollinger-Ellison syndrome resistant to histamine H2-receptor antagonists.
Bader, JP; Cortot, A; Delchier, JC; Goldfain, D; Isal, JP; Mignon, M; Soule, JC; Travers, B, 1986
)
0.27
" Addition of the acetylcholinesterase inhibitor, physostigmine, caused a leftward shift in the GABA dose-response curve and increased by 10-fold the sensitivity of the antral preparation to GABA stimulation."( Cholinergic mediation of gamma-aminobutyric acid-induced gastrin and somatostatin release from rat antrum.
Franklin, PA; Harty, RF, 1986
)
0.27
" Plasma concentrations remained in the therapeutic range and the dosage regimen was well tolerated."( Steady-state intravenous pharmacokinetics of pirenzepine in patients with hepatic insufficiency and combined renal- and hepatic insufficiency.
Bozler, G; Krakamp, B; Leidig, P; Schmitz, R; Tanswell, P; Vogel, H, 1989
)
0.54
" Dosage adjustment need only be considered in patients with CLCR less than 25 ml/min in order to reduce the frequency of minor side-effects."( Steady-state intravenous pharmacokinetics of pirenzepine in patients with differing degrees of renal dysfunction.
Bozler, G; Krakamp, B; Tanswell, P; Vogel, H, 1989
)
0.54
" Because it has been suggested that the lower relapse rate for duodenal ulcer following colloidal bismuth subcitrate (CBS) is due to suppression of C pylori we investigated different formulations and dosing of CBS for their efficacy in clearing C pylori."( Treatment of Campylobacter pylori gastritis: a pilot study using pirenzepine dihydrochloride (Gastrozepin) and three formulations of colloidal bismuth subcitrate (De-Nol).
Ali, MR; Brown, P; Lane, M; Morris, A; Palmer, R, 1988
)
0.51
" This bivalent dose-response relationship was also observed after beta-blockade."( Dose-response curves of pirenzepine in man in relation to M1- and M2-cholinoceptor occupancy.
Pitschner, HF; Wellstein, A, 1988
)
0.58
"In the present study we set out to explain the complex atropine dose-response curves in man in relation to M-cholinoceptor subtype occupancy."( Complex dose-response curves of atropine in man explained by different functions of M1- and M2-cholinoceptors.
Pitschner, HF; Wellstein, A, 1988
)
0.27
" The dose-response curves showed that AF102B was far less potent than oxotremorine at the hippocampal presynaptic muscarinic receptors (autoreceptors)."( Heterogeneity of muscarinic autoreceptors and heteroreceptors in the rat brain: effects of a novel M1 agonist, AF102B.
Kawanishi, G; Mizobe, F; Ohgane, N; Ono, S; Saito, Y, 1988
)
0.27
" Dose-response experiments indicate that norepinephrine is approximately 10,000 times more potent on a molar basis than carbachol in stimulating antral gastrin release."( Comparison of adrenergic and cholinergic receptor-mediated stimulation of gastrin release from rat antral fragments.
Harty, RF; Maico, DG; McGuigan, JE,
)
0.13
" Thus: (a) Dose-response relationships between IP3 accumulation, MLC phosphorylation and muscle contraction for CCh suggest a fairly good correlation between the biochemical and pharmacological responses."( Muscarinic-receptor induced myo-inositol trisphosphate accumulation, myosin light chain phosphorylation and contraction in the rabbit iris sphincter smooth muscle.
Abdel-Latif, AA; Akhtar, RA; Howe, PH, 1987
)
0.27
"The relationships between occupancy of muscarinic acetylcholine receptors on iris sphincter muscle, measured by [3H]quinuclidinylbenzylate (QNB) binding, carbachol (CCh)-stimulated phosphatidylinositol 4,5-bisphosphate hydrolysis, measured as myo-inositol trisphosphate (IP3) accumulation, myosin light chain (MLC) phosphorylation and contraction were analyzed by examination of the dose-response relationships and the effects of the muscarinic antagonists, atropine and pirenzepine (PZ)."( M2 muscarinic receptor subtype is associated with inositol trisphosphate accumulation, myosin light chain phosphorylation and contraction in sphincter smooth muscle of rabbit iris.
Abdel-Latif, AA; Akhtar, RA; Honkanen, RE; Howe, PH, 1987
)
0.44
" The cimetidine dose-response curves and the calculated ED50 values were similar in the different experimental situations."( Effects of cimetidine, atropine and pirenzepine on basal and stimulated gastric acid secretion in the rat.
Ekelund, M; Håkanson, R; Vallgren, S, 1987
)
0.55
" For drug-treated BALB mice, the dose-response curves for both measures were parallel to those for saline-treated mice, while for DBA and C3H mice the slopes of the dose-response curves were significantly less for treated mice than they were for controls."( Genetic influences on tolerance development with chronic oxotremorine infusion.
Collins, AC; Marks, MJ; Romm, E, 1987
)
0.27
" The treatment with full dosage (100 mg/day) did not increase the rate of positive responsiveness compared to that of standard dosage (50 mg/day)."( [Pharmacologic treatment of duodenal ulcer. Short and long-term results with pirenzepine in ambulatory patients].
Barberani, F; Carpinelli, D; D'Ambrosio, C; Della Spoletina, A; Fiorini, MA; Nicolao, V; Schiaroli, G; Valentini, P, 1986
)
0.5
" The antisecretory dosage of pirenzepine caused a significant reduction in the surface area of the ulcer by the seventh postoperative day, whereas neither the antisecretory dosage of atropine nor the nonantisecretory dosage of pirenzepine significantly affected the size of the ulcer."( Effects of atropine and pirenzepine on healing of gastric ulcer induced by mucosal excision in rats.
Fujiwara, M; Kitagawa, H; Sano, M, 1985
)
0.87
" Serum samples were serially drawn during each dosing interval for determination of cimetidine and PRZ concentrations by HPLC and RIA, respectively."( Lack of pharmacokinetic interaction between cimetidine and pirenzepine.
Jamali, F; Mahachai, V; Reilly, PA; Thomson, AB, 1985
)
0.51
" In hexamethonium, pirenzepine shifted the acetylcholine dose-response curve to the right with an equilibrium dissociation constant of 200 nM, indicating an interaction with a m2-type of muscarinic receptor."( Acetylcholine acts on m2-muscarinic receptors to excite rat locus coeruleus neurones.
Egan, TM; North, RA, 1985
)
0.6
" The calcium dose-response curve paralleled those of lipase and chymotrypsin outputs."( Action of pirenzepine, a new muscarinic antagonist drug, on human pancreatic secretion.
Laugier, R; Nishimura, S; Sarles, H, 1985
)
0.67
" A beneficial effect of pirenzepine in the prevention of duodenal ulcer recurrence was apparent in preliminary studies in small numbers of patients, but its efficacy in this regard needs further confirmation and the optimum dosage determined."( Pirenzepine. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in peptic ulcer disease and other allied diseases.
Brogden, RN; Carmine, AA, 1985
)
2.02
" Atropine caused a dose-dependent rightward shift in the dose-response curves of inhibitory and excitatory effects of the two muscarinic agonists."( Pharmacologic identification, activation and antagonism of two muscarine receptor subtypes in the lower esophageal sphincter.
Gilbert, R; Goyal, RK; Rattan, S, 1984
)
0.27
" To characterize the antimuscarinic potencies of pirenzepine and N-methylatropine, for both antagonists doses were calculated that produce a 10-fold shift to the right of the dose-response curves for A) the pressor response to McN-A-343 (i."( A comparison of the antimuscarinic effects of pirenzepine and N-methylatropine on ganglionic and vascular muscarinic receptors in the rat.
Lambrecht, G; Moser, U; Mutschler, E; Wess, J, 1984
)
0.78
" The results show that pirenzepine was as effective as cimetidine in the prevention of duodenal ulcer relapses when administered at a dosage of 75 mg daily (of which 50 mg at bedtime) for one year."( Long-term management of duodenal ulcer with pirenzepine and cimetidine: a double-blind controlled clinical trial.
Cacioli, D; Galeone, M; Giorgi-Conciato, M; Moise, G; Stock, F; Toti, GL, 1983
)
0.84
"A study has been made on the modifications that appear after acute dosage of pirenzepine in a series of eight healthy subjects of both sexes who had shown, by radioisotopic evaluation, a physiological pattern of gastric kinetics."( Antimuscarinic compounds and gastric kinetics: a study with pirenzepine on healthy subjects.
Alberti, R; Colombi Zinelli, L; Ferretti, PP; Rinetti, M; Ugolotti, G, 1984
)
0.74
" In 12 prospective randomized double-blind placebo controlled studies pirenzepine was administered to 475 duodenal ulcer patients with an incidence of endoscopically proven healing of 74% when the daily dosage of the drug was 100 or 150 mg but of only 55% if the dosage of the drug was 75 mg or less."( Pirenzepine in the treatment of peptic ulcer disease. Review and commentary.
Bianchi Porro, G; Petrillo, M, 1982
)
1.94
" Selectivity is dose limited and has so far been demonstrated only at a daily dosage of 100 mg, in 2 divided doses."( The efficacy and selectivity of pirenzepine. Review and commentary.
Reilly, PA; Texter, EC, 1982
)
0.55
" Pirenzepine, however, shows consistently uniform plasma level profiles, well within the therapeutic range after multiple dosing (50 mg, twice daily)."( An international pharmacokinetic study on pirenzepine following a single oral dose.
Bozler, G; Hammer, R, 1980
)
1.44
" Oxotremorine generated dose-response curves that were similar in both the circular and longitudinal vectors and intermediate to those previously reported for carbachol and aceclidine."( The effect of muscarinic agonists and selective receptor subtype antagonists on the contractile response of the isolated rhesus monkey ciliary muscle.
Gabelt, BT; Kaufman, PL; Poyer, JF, 1994
)
0.29
" The dose-response curves for haloperidol to changes in the evoked DA release were found to be biphasic (small doses increased the release and large doses inhibited), which were shifted to the left by longer periods of superfusion with haloperidol."( [Inhibitory effect of haloperidol on evoked dopamine release from striatal slices of the rat].
Takaki, T; Tanaka, M; Yamada, S; Yokoo, H, 1995
)
0.29
"To answer the questions if the type of continuous dose-response technique influences the pancreatic secretory response to intraduodenal tryptophan and if the M1-receptor antagonist telenzepine influences the intestinal absorption of tryptophan, we determined, in 12 conscious dogs with chronic gastric and duodenal fistulas, pancreatic bicarbonate and protein secretion and tryptophan plasma concentrations following intraduodenal tryptophan perfusion using two dose-response techniques."( Comparison of two dose-response techniques to study the pancreatic secretory response to intraduodenal tryptophan in the absence and presence of the M1-receptor antagonist telenzepine.
Chari, ST; Niebergall, E; Singer, MV; Teyssen, S, 1995
)
0.29
" Our results suggest that adaptation of physiological mechanisms governing the exocrine pancreas may occur after one week of receptor blockade by a therapeutic dosage of telenzepine, to the extent that M1-blockade no longer inhibits secretion."( Exocrine pancreatic secretion in man following one week of M1-muscarinic receptor blockade.
Ditschuneit, H; Glasbrenner, B; Kemmer, TP; Malfertheiner, P; Nelson, DK; Schneider, A, 1993
)
0.29
" They were obtained by the chi-square (chi 2) goodness-of-fit test, recently applied for the evaluation of dose-response curves."( Modern approach to the evaluation of combined effects of single-dose trials and clinical time-course studies, exemplified by combinations of pirenzepine and H2-receptor antagonists.
Londong, W; Pöch, G, 1993
)
0.49
" A standardized dosage of cyclosporine was given orally, and the duration was calculated for the maximum whole blood level of cyclosporine to be achieved; the dosage/level quotient was calculated."( The influence of gastrointestinal agents on resorption and metabolism of cyclosporine after heart transplantation: experimental and clinical results.
Markewitz, A; Meiser, BM; Muschiol, F; Nollert, G; Pfeiffer, M; Reichart, B; Reichenspurner, H; Uberfuhr, P; Wagner, F,
)
0.13
" The mean IC50 values for ACh and oxotremorine methiodide (oxo-M), obtained from non-cumulative dose-response curves, were 204 and 363 nM respectively."( M2 muscarinic receptor-mediated inhibition of the Ca2+ current in rat magnocellular cholinergic basal forebrain neurones.
Allen, TG; Brown, DA, 1993
)
0.29
" However, risperidone induced a U-shaped dose-response curve."( Differential effects of repeated administration of novel antipsychotic drugs on the activity of midbrain dopamine neurons in the rat.
Skarsfeldt, T, 1995
)
0.29
" The aim of the present investigation was to establish dose-response curves for intravitreal and subconjunctivally injected pirenzepine and to determine receptor specificity."( Pirenzepine prevents form deprivation myopia in a dose dependent manner.
Cottriall, CL; Leech, EM; McBrien, NA, 1995
)
1.94
" Inhibitors of phospholipase C, protein kinase C, calcium/calmodulin, nitric oxide synthase and guanylate cyclase, shifted the dose-response curve of carbachol on contractility to the right."( Endogenous nitric oxide signalling system and the cardiac muscarinic acetylcholine receptor-inotropic response.
Borda, E; Echagüe, AV; Genaro, A; Leiros, CP; Sterin-Borda, L, 1995
)
0.29
" The dose-response curves of 2-butynyloxy, cyclopropylmethyloxy and hexyloxy compound together was the same as the response of each separately."( 1,2,5-Thiadiazole derivatives of arecoline stimulate M1 receptors coupled to phosphoinositide turnover.
Hoss, W; Messer, WS; Periyasamy, S; Roknich, S; Sauerberg, P, 1995
)
0.29
"1 microM), shifted the dose-response curve for muscarine-induced adrenaline secretion to the right."( Muscarinic receptor subtypes mediating catecholamine secretion and increase in intracellular Ca2+ concentration in adrenal chromaffin cells of the guinea pig.
Asano, T; Ito, S; Nakazato, Y; Ohta, T; Otsuguro, K, 1995
)
0.29
" In the presence of chlorisondamine, McN-A-343 increased both RNA and BP in dose-related fashion, and the dose-response curves of McN-A-343 shifted to the right in the presence of pirenzepine."( Role of muscarinic receptors in ganglionic transmission in rabbits.
Kim, JH; Ro, YB, 1996
)
0.49
" The in vivo dose-response effects of "selective" muscarinic antagonists on changes in lung resistance (RL) and heart rate (HR) in response to electrical stimulation of the vagus nerves were obtained in four groups of newborns."( Cardiopulmonary actions of muscarinic receptor subtypes in the newborn dog.
Anderson, JW; Brundage, KL; Fisher, JT, 1996
)
0.29
" Detailed evaluation of the dose-response characteristics of olanzapine and direct clinical comparison to clozapine will thus provide valuable leads to the clarification of atypical antipsychotic action."( A PET study of 5-HT2 and D2 dopamine receptor occupancy induced by olanzapine in healthy subjects.
Farde, L; Halldin, C; Nyberg, S, 1997
)
0.3
" Analyses indicated that an increasing dose-response curve was observed across the range of all olanzapine dose groups."( Olanzapine versus haloperidol: acute phase results of the international double-blind olanzapine trial.
Beasley, CM; Beuzen, JN; Blin, O; Crawford, AM; Dellva, MA; Hamilton, SH; Tollefson, GD; Tran, PV, 1997
)
0.3
" Dose-response curves were constructed using the putatively selective antagonists pirenzepine (M1), gallamine (M2) and 4-DAMP (M3: 4-diphenyl-acetoxy-N-methylpiperidine) and compared with the non-selective blocker, atropine."( Functional characterization of peripheral muscarinic subtypes in anesthetized cats.
Koss, MC, 1997
)
0.52
" Olanzapine exhibits linear kinetics over the dosage range studied and is extensively metabolized in humans."( Olanzapine: a new antipsychotic agent with efficacy in the management of schizophrenia.
Green, AI; Kando, JC; Patel, JK; Reams, SG; Satterlee, W; Shepski, JC, 1997
)
0.3
" After a 2- to 9-day placebo lead-in, 79 inpatients with schizophrenia according to DSM-III-R criteria were placed on an olanzapine dosage of 10 mg/day or 1 mg/day for up to 6 weeks."( Olanzapine plasma concentrations and clinical response in acutely ill schizophrenic patients.
Beasley, C; Perry, PJ; Sanger, T, 1997
)
0.3
" In conclusion, the present studies demonstrate that in the case of sequential dosing olanzapine more effectively enhances DA and NE release in the Pfc than in the subcortical areas, which may have an impact on its atypical antipsychotic actions."( Olanzapine increases in vivo dopamine and norepinephrine release in rat prefrontal cortex, nucleus accumbens and striatum.
Bymaster, FP; Li, XM; Perry, KW; Wong, DT, 1998
)
0.3
"The pharmacology, pharmacokinetics, clinical efficacy, adverse effects, drug interactions, dosage and administration, and cost of olanzapine are reviewed."( Olanzapine: a serotonin-dopamine-receptor antagonist for antipsychotic therapy.
Bever, KA; Perry, PJ, 1998
)
0.3
"The 14 patients received olanzapine at a mean (SD dosage of 14."( Olanzapine in treatment-resistant bipolar disorder.
Altshuler, L; Denicoff, K; Frye, M; Keck, PE; Kmetz, GF; Kupka, R; Leverich, GS; McElroy, SL; Nolen, W; Post, RM; Suppes, T, 1998
)
0.3
" Pirenzepine was administered intramuscularly at a dosage of 20 mg/kg twice daily; and lansorprazole, subcutaneously at 50 mg/kg once daily, both every day for 4 weeks."( Effect of pirenzepine on gastric endocrine cell kinetics during lansoprazole administration.
Aoki, T; Gang, C; Kashiwagi, H; Omura, K; Omura, N, 1998
)
1.61
" There are others who are unable to tolerate a high dosage of clozapine."( Olanzapine augmentation of clozapine.
Frank, B; Gupta, S; Sonnenberg, SJ, 1998
)
0.3
"Olanzapine was given to five patients with idiopathic Parkinson's disease and the dosage was titrated until a clinically meaningful reduction in hallucinosis was achieved."( Olanzapine in the treatment of hallucinosis in idiopathic Parkinson's disease: a cautionary note.
Ford, KS; Graham, JM; Sagar, HJ; Sussman, JD, 1998
)
0.3
" Proper dosing has emerged as a vital factor in the effective use of these newer drugs."( Risperidone and olanzapine: optimal dosing for efficacy and tolerability in patients with schizophrenia.
Kasper, S, 1998
)
0.3
" Dosing requirements for elderly patients tend to be much lower than those for younger adults."( Conventional vs. newer antipsychotics in elderly patients.
Harris, MJ; Jeste, DV; Lacro, J; Lohr, JB; Rockwell, E, 1999
)
0.3
" Muscarine shifted the GABA dose-response curve to the left, with the GABA EC50 decreased from 45 +/- 2 to 13 +/- 2 microM."( Enhancement of GABA-activated current by muscarine in rat dorsal root ganglion neurons.
Hu, HZ; Li, ZW; Shao, M, 1999
)
0.3
" To provide the therapeutic benefits of maintenance medication without its drawbacks, intermittent dosing and long-term therapy with reduced doses of conventional medications have been explored."( Olanzapine in the long-term treatment of schizophrenia.
Kane, J, 1999
)
0.3
" The atypical properties of first-line atypical antipsychotics as well as clozapine are reviewed here, with clinical pearls and dosing tips for each based upon a consensus of information from both clinical trials and clinical practice."( Selecting an atypical antipsychotic by combining clinical experience with guidelines from clinical trials.
Stahl, SM, 1999
)
0.3
" In the isolated AV node preparation, dose-response curves for negative dromotropic effects (prolongation of Atrio-His interval) of carbachol (CCh) injected into the posterior septal artery were shifted to the right in parallel by AF-DX, pirenzepine, and atropine with apparent pA2-values of 13, 27."( Comparison of anti-M2-muscarinic effect of AF-DX 116 on atrioventricular nodal conduction with those of pirenzepine and atropine as antibradyarrhythmic drugs.
Motomura, S; Sasaki, S, 1999
)
0.7
" Published studies have drawn criticism in terms of inappropriate titration schedules, nonequivalent dosing between treatment groups, short treatment duration, and inadequate sample sizes."( Clozapine: a comparison with other novel antipsychotics.
Fleischhacker, WW, 1999
)
0.3
" The decreased D(2)/D(3) receptor availability revealed an exponential dose-response relationship (r=-0."( In vivo effects of olanzapine on striatal dopamine D(2)/D(3) receptor binding in schizophrenic patients: an iodine-123 iodobenzamide single-photon emission tomography study.
Dresel, S; Hahn, K; Mager, T; Meisenzahl, E; Möller, HJ; Rossmüller, B; Tatsch, K, 1999
)
0.3
" The withdrawal symptoms disappeared rapidly with an increase in olanzapine dosage and with anticholinergic started at the beginning of the switch."( Clozapine-olanzapine: a potentially dangerous switch. A report of two cases.
Delassus-Guenault, N; Jegouzo, A; Odou, P; Robert, H; Seguret, T; Vignole, E; Zangerlin, H, 1999
)
0.3
" Assessments of attention, memory and motor control were made prior to dosing on each day, at 2, 4, 6 and 8 h after dosing on days 1 and 4, and at 24 and 48 h following the last dose."( A comparison of the effects of olanzapine, haloperidol and placebo on cognitive and psychomotor functions in healthy elderly volunteers.
Beuzen, JN; Taylor, N; Wesnes, K; Wood, A, 1999
)
0.3
" The pharmacokinetics of olanzapine are linear and dose-proportional within the approved dosage range."( Olanzapine. Pharmacokinetic and pharmacodynamic profile.
Beasley, CM; Bergstrom, RF; Callaghan, JT; Ptak, LR, 1999
)
0.3
" We have evaluated the consequences of HFD on heart rate (HR) and blood pressure (BP) circadian cycles and methylscopolamine dose-response curves."( Impaired atrial M(2)-cholinoceptor function in obesity-related hypertension.
Berlan, M; Galitzky, J; Merial, C; Montastruc, JL; Pelat, M; Senard, JM; Verwaerde, P, 1999
)
0.3
" Dosing was 12."( Differential olanzapine plasma concentrations by sex in a fixed-dose study.
Conley, RR; Kelly, DL; Tamminga, CA, 1999
)
0.3
" Surprisingly, there has been little relationship between the pivotal trials designed for FDA approval and current dosing strategies in broader clinical settings."( New antipsychotic medications: more than old wine and new bottles.
Schulz, SC, 2000
)
0.31
" Without such data, clinicians have difficulty designing appropriate dosage regimens for patients in these age groups."( Olanzapine pharmacokinetics in pediatric and adolescent inpatients with childhood-onset schizophrenia.
Bergstrom, RF; Calis, KA; DeVane, CL; Grothe, DR; Jacobsen, L; Kumra, S; Kurtz, DL; Rapoport, JL, 2000
)
0.31
"Thirty adult patients with acute schizophrenia were included into six-week open-labelled, non-comparative trial of olanzapine with free dosing from 5 to 20 mg per day."( [The experience of application of olanzapine: an atypical neuroleptic in acute schizophrenia].
Beniashvili, AG; Morozova, MA; Zharkova, NB, 2000
)
0.31
" Cases admitted in the first semester received a significantly higher daily dosage of antipsychotic drugs and more frequently received anticholinergics."( Second-generation antipsychotics in the emergency care setting. A prospective naturalistic study.
Azzoni, A; Raja, M,
)
0.13
" Longitudinal study is required because this relationship may have implications for dosing strategies."( Subjective experience and striatal dopamine D(2) receptor occupancy in patients with schizophrenia stabilized by olanzapine or risperidone.
Booij, J; de Haan, L; Dingemans, PM; Lavalaye, J; Linszen, D, 2000
)
0.31
" Initial dosage was 10 mg/day with a maximum dosage of 20 mg/day."( Effective open-label treatment of tourette's disorder with olanzapine.
Aschauer, HN; De Zwaan, M; Kasper, S; Resinger, E; Schindler, SD; Stamenkovic, M; Willinger, U, 2000
)
0.31
" A dose-response relationship was not consistently confirmed with any of the drug treatments."( The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia.
Breier, A; David, SR; Kinon, BJ; Taylor, CC, 2000
)
0.31
" No consistent dose-response relationship was observed, and the time course and sex-dependency of the response differed between the 3 agents."( The effects of olanzapine, risperidone, and haloperidol on plasma prolactin levels in patients with schizophrenia.
Breier, A; David, SR; Kinon, BJ; Taylor, CC, 2000
)
0.31
" In addition, psychiatrists' clinical preference of antipsychotic medication and dosage for patient subtypes were examined by the national survey."( Comparison of cost, dosage and clinical preference for risperidone and olanzapine.
Kaplan, Z; Lichtenberg, P; Rabinowitz, J, 2000
)
0.31
" Taking into account drug costs and dosage requirements, the average daily retail price was US $6."( Comparison of cost, dosage and clinical preference for risperidone and olanzapine.
Kaplan, Z; Lichtenberg, P; Rabinowitz, J, 2000
)
0.31
"In this open case series, the dose-response relationship of atypical antipsychotic augmentation in the treatment of obsessive compulsive disorder (OCD), and the dose-severity relationship in atypical anti psychotic-induced OC symptoms were examined."( Serotonin and dopamine antagonism in obsessive-compulsive disorder: effect of atypical antipsychotic drugs.
Lapierre, Y; Ramasubbu, R; Ravindran, A, 2000
)
0.31
"Case 1: A linear dose-response relationship between increasing doses of olanzapine and improvement in OC symptoms was observed in an OCD patient resistant to 5-HT reuptake inhibitors."( Serotonin and dopamine antagonism in obsessive-compulsive disorder: effect of atypical antipsychotic drugs.
Lapierre, Y; Ramasubbu, R; Ravindran, A, 2000
)
0.31
"Controlled studies are needed to investigate the dose-response or dose-severity relationships between OCD and atypical antipsychotics."( Serotonin and dopamine antagonism in obsessive-compulsive disorder: effect of atypical antipsychotic drugs.
Lapierre, Y; Ramasubbu, R; Ravindran, A, 2000
)
0.31
" Olanzapine concentrations were found to be a function of olanzapine dose (in milligrams per day) and gender such that prospective olanzapine dosing is feasible."( Olanzapine plasma concentrations and clinical response: acute phase results of the North American Olanzapine Trial.
Beasley, C; Lund, BC; Perry, PJ; Sanger, T, 2001
)
0.31
" clozapine, Clo) in 3 aspects: 1) the multiple receptor pharmacodynamics involving D1/D2, 5-HT2 and M-ACh receptors; 2) dose-response separation between the block of conditioned avoidance response and catalepsy induction; and 3) the specificity of action sites of firing rates upon acute drug challenge."( Behavioral characteristics of olanzapine: an atypical neuroleptic.
Chen, LJ; Fu, Y; Jin, GZ; Yu, LP; Zhu, ZT, 2000
)
0.31
"Ten adult patients aged 20 to 44 years with Tourette's disorder were treated using an open-label, flexible dosing schedule for 8 weeks."( An open-label study of the treatment efficacy of olanzapine for Tourette's disorder.
Bruun, RD; Budman, CL; Gayer, A; Lesser, M; Shi, Q, 2001
)
0.31
" The initial dosage was 5 mg/day and was titrated to a maximum of 20 mg/day."( Olanzapine in the treatment of post-traumatic stress disorder: a pilot study.
Becker, ME; Butterfield, MI; Churchill, LE; Connor, KM; Davidson, JR; Sutherland, S, 2001
)
0.31
" Olanzapine typically alleviated pain within 20 minutes after oral dosing and treatment response was consistent across multiple treated attacks."( Olanzapine as an abortive agent for cluster headache.
Rozen, TD, 2001
)
0.31
" The trial was divided into two periods: eight weeks during which the dosage was escalated and then fixed, and six weeks during which variable dosages were used."( Effects of clozapine, olanzapine, risperidone, and haloperidol on hostility among patients with schizophrenia.
Chakos, M; Citrome, L; Cooper, TB; Czobor, P; Lieberman, JA; Lindenmayer, JP; McEvoy, J; Sheitman, B; Volavka, J, 2001
)
0.31
" Subjective impairment, as assessed with the subscale 'mental functioning', was significantly correlated with greater conventional neuroleptic dosage after controlling for psychopathology (P<0."( Relationship between neuroleptic dosage and subjective cognitive dysfunction in schizophrenic patients treated with either conventional or atypical neuroleptic medication.
Krausz, M; Moritz, S; Naber, D; Woodward, TS, 2002
)
0.31
" Among the group receiving novel antipsychotics, dosage was not related to satisfaction or burden of adverse effects."( Short report: comparison of patient satisfaction and burden of adverse effects with novel and conventional neuroleptics: a naturalistic study.
Bromet, EJ; Davidson, M; Rabinowitz, J, 2001
)
0.31
" Risk factors are a high dosage of antipsychotics, akathisia in a previous treatment, and diabetes mellitus."( [Drug-induced akathisia].
van Harten, PN, 2002
)
0.31
"A 27-year-old white woman was observed to have a seizure while receiving a stable dosage of olanzapine 15 mg/d, with the addition of quetiapine 100 mg in the evening 1 day before the occurrence of the seizure."( New-onset seizure associated with quetiapine and olanzapine.
Hedges, DW; Jeppson, KG, 2002
)
0.31
"Current dosing regimens of psychotropic drugs are based on plasma kinetic considerations, although it is unclear whether plasma levels faithfully reflect brain kinetics of drugs."( Significant dissociation of brain and plasma kinetics with antipsychotics.
Jones, C; Kapur, S; Remington, G; Tauscher, J; Zipursky, RB, 2002
)
0.31
" The manuscript describes the pharmacology, efficacy and tolerability studies, adverse effects and dosing considerations in the elderly."( Use of olanzapine for elderly patients with psychotic disorders: a review.
Bogunovic, O; Brenner, R; Gupta, S; Madhusoodanan, S; Sinha, S, 2001
)
0.31
" No serious side effects were reported at the maximum dosage reached (7."( Treatment of patients with tardive dystonia with olanzapine.
Bellini, G; Bernardini, S; Bonuccelli, U; Dell'Agnello, G; Lucetti, C; Maggi, L; Manca, L; Nuti, A; Piccinni, A,
)
0.13
" A dose-response relationship for IM olanzapine in the reduction of agitation was assessed by measuring the reduction in Positive and Negative Syndrome Scale Excited Component (PANSS-EC) scores 2 hours after the first injection."( A double-blind, placebo-controlled dose-response comparison of intramuscular olanzapine and haloperidol in the treatment of acute agitation in schizophrenia.
Birkett, M; Breier, A; Brook, S; David, S; Dossenbach, M; Ferchland, I; Kiesler, G; Meehan, K; Palmer, R; Sutton, V; Taylor, CC; Wright, P, 2002
)
0.31
"Olanzapine exhibited a dose-response relationship for reduction in agitation (F(1,179)= 14."( A double-blind, placebo-controlled dose-response comparison of intramuscular olanzapine and haloperidol in the treatment of acute agitation in schizophrenia.
Birkett, M; Breier, A; Brook, S; David, S; Dossenbach, M; Ferchland, I; Kiesler, G; Meehan, K; Palmer, R; Sutton, V; Taylor, CC; Wright, P, 2002
)
0.31
"0 mg per injection exhibits a dose-response relationship in the rapid treatment of acute agitation in patients with schizophrenia and demonstrates a favorable safety profile."( A double-blind, placebo-controlled dose-response comparison of intramuscular olanzapine and haloperidol in the treatment of acute agitation in schizophrenia.
Birkett, M; Breier, A; Brook, S; David, S; Dossenbach, M; Ferchland, I; Kiesler, G; Meehan, K; Palmer, R; Sutton, V; Taylor, CC; Wright, P, 2002
)
0.31
" In the case presented, the good efficacy of olanzapine in low dosage over an extended period of time is described."( [Delusional ectoparasitic infestation in multiple system atrophy].
Kornhuber, M; Kumbier, E, 2002
)
0.31
"A 3-week, randomized, double-blind trial compared flexibly dosed olanzapine (5-20 mg/day) to divalproex (500-2500 mg/day in divided doses) for the treatment of patients hospitalized for acute bipolar manic or mixed episodes."( Olanzapine versus divalproex in the treatment of acute mania.
Altshuler, LL; Baker, RW; Breier, A; Gilmore, JA; Ketter, TA; Milton, DR; Risser, R; Suppes, T; Tohen, M; Tollefson, GA; Zarate, CA, 2002
)
0.31
" When olanzapine was discontinued or the dosage decreased, 78% of patients had improved glycemic control."( Olanzapine-associated diabetes mellitus.
Doraiswamy, PM; Koller, EA, 2002
)
0.31
" The present TDM-based follow-up suggests that the influence of gender, smoking habits, and certain drug interactions may need to be considered for optimal dosage of OLA."( Therapeutic drug monitoring data on olanzapine and its N-demethyl metabolite in the naturalistic clinical setting.
Bengtsson, F; Dahl, ML; Lundmark, J; Reis, M; Skogh, E, 2002
)
0.31
" Whole brain and plasma P and 3alpha,5alpha-THP concentrations were increased with olanzapine or P dosing and were greatest with coadministration."( Olanzapine and progesterone have dose-dependent and additive effects to enhance lordosis and progestin concentrations of rats.
Frye, C; Seliga, A, 2002
)
0.31
" This double-blind, randomized controlled trial, comparing flexible dosing of olanzapine (5-20 mg/day, n = 234) to haloperidol (3-15 mg/day, n = 219), consisted of a 6-week acute phase, followed by a 6-week continuation phase."( Olanzapine versus haloperidol in the treatment of acute mania: clinical outcomes, health-related quality of life and work status.
Breier, A; Edgell, ET; Gandhi, G; Haro, JM; Namjoshi, MA; Shi, L; Tohen, M; Zhang, F, 2002
)
0.31
"Eleven patients with schizophrenia stabilized on oral olanzapine (mean dosage 12."( Dissolution profile, tolerability, and acceptability of the orally disintegrating olanzapine tablet in patients with schizophrenia.
Chue, P; Dickson, R; Jones, B; Taylor, CC, 2002
)
0.31
" Divalproex was initiated at 15 mg/kg/day and titrated over 12 days to a maximum dosage of 30 mg/kg/day."( Effect of divalproex combined with olanzapine or risperidone in patients with an acute exacerbation of schizophrenia.
Casey, DE; Daniel, DG; Sommerville, KW; Tracy, KA; Wassef, AA; Wozniak, P, 2003
)
0.32
" The mean daily dosage of olanzapine in the fourth week was 10."( The efficacy and safety of olanzapine for the treatment of geriatric psychosis.
Hwang, JP; Lee, TW; Tsai, SJ; Yang, CH, 2003
)
0.32
" The patients were treated with conventional antipsychotics for seven days after admission and were then randomised to the treatment arms with risperidone (4 mg/day) or with olanzapine (10 mg/day) at a fixed dosage in the first week and thereafter in flexible dosages for the remaining seven weeks."( Measurement of simple reaction time in antipsychotic treatment of patients with schizophrenia.
Kores Plesnicar, B; Krajnc, I; Tomori, M; Zalar, B, 2003
)
0.32
"This 47-week, randomized, double-blind study compared flexibly dosed olanzapine (5-20 mg/day) to divalproex (500-2500 mg/day) for manic or mixed episodes of bipolar disorder (N=251)."( Olanzapine versus divalproex sodium for the treatment of acute mania and maintenance of remission: a 47-week study.
Altshuler, L; Baker, RW; Brown, E; Frye, M; Ketter, TA; Risser, RC; Schuh, LM; Suppes, T; Tohen, M; Zajecka, J; Zarate, CA, 2003
)
0.32
" At a higher dosage (0."( The atypical antipsychotics risperidone, clozapine and olanzapine differ regarding their sedative potency in rats.
Ahnaou, A; Drinkenburg, WH; Megens, AA, 2003
)
0.32
"This was a double-blind, randomized, parallel-groups, placebo-controlled trial with fixed-flexible dosing conducted at four sites."( Randomized trial of olanzapine versus placebo in the symptomatic acute treatment of the schizophrenic prodrome.
Addington, J; Breier, A; Hawkins, KA; Lindborg, SR; Marquez, E; McGlashan, TH; Miller, TJ; Perkins, DO; Tohen, M; Woods, SW; Zipursky, RB, 2003
)
0.32
" A new approach to olanzapine dosing that expands the initial dose range up to 40 mg/d may offer superior efficacy in rapidly and effectively controlling the symptoms of agitation."( Effectiveness of rapid initial dose escalation of up to forty milligrams per day of oral olanzapine in acute agitation.
Baker, RW; Hill, AL; Kinon, BJ; Liu, H; Maguire, GA, 2003
)
0.32
" Daily dosage was subsequently adjusted between 5 and 20 mg/d based on individual clinical status."( A Canadian multicenter trial assessing memory and executive functions in patients with schizophrenia spectrum disorders treated with olanzapine.
Chokka, PR; Dickson, RA; Dursun, SM; Jones, B; MacEwan, GW; Reiss, JP; Remington, GJ; Rotstein, E; Stip, E, 2003
)
0.32
"Previous studies have examined the safety and tolerability of oral-loaded divalproex sodium in the treatment of acute mania, but not the early efficacy of this dosing strategy."( The safety and early efficacy of oral-loaded divalproex versus standard-titration divalproex, lithium, olanzapine, and placebo in the treatment of acute mania associated with bipolar disorder.
Baker, JD; Hirschfeld, RM; Sommerville, KW; Tracy, K; Wozniak, P, 2003
)
0.32
" However, no correlation between prolactin levels and dosage could be found."( [Plasma prolactin level and incidence of adverse endocrinologic effects during therapy with atypical neuroleptics].
Fric, M; Laux, G, 2003
)
0.32
" The diagnosis of rhabdomyolysis was confirmed by myoglobinemia dosage and ortholuidine test."( [Rhabdomyolysis associated with respiratory infection in chronic psychiatric patients during neuroleptic treatment].
Busiello, L; Cascella, M; De Robertis, E; Di Domenico, MG; Palmese, S; Pezza, M, 2003
)
0.32
" The starting dose was 10 mg/day, with dosage adjustments based on physician judgment."( Switching treatment-resistant patients with schizophrenia or schizoaffective disorder to olanzapine: a one-year open-label study with five-year follow-up.
Karagianis, JL; LeDrew, KK; Walker, DJ, 2003
)
0.32
"Double-blind data on patients age > or =60 randomized to 5 mg/d OLZ (n=83) or 5 mg/d HAL (n=34) (Week 1) then flexibly dosed to 5-20 mg/d over six weeks, with a 48-week extension for responders, were analyzed post-hoc."( Olanzapine vs haloperidol in geriatric schizophrenia: analysis of data from a double-blind controlled trial.
Breier, A; Bymaster, FP; Dossenbach, M; Gilmore, JA; Golshan, S; Jeste, D; Kaiser, CJ; Kennedy, JS; Kinon, BJ; Maguire, GA; Sanger, T; Tollefson, G, 2003
)
0.32
" The mean dosage of olanzapine was 11."( Pilot study: access to fitness facility and exercise levels in olanzapine-treated patients.
Archie, S; Hobbs, H; McNiven, J; Osborne, S; Wilson, JH, 2003
)
0.32
" We suggest that plasma olanzapine monitoring can be used for dose-response optimization, but only to complement the normal clinical evaluation process."( Investigation of target plasma concentration-effect relationships for olanzapine in schizophrenia.
Ahmad, F; Bulsara, MK; Castle, DJ; Dusci, LJ; Fellows, L; Ilett, KF, 2003
)
0.32
" The treating clinician was free to vary or discontinue dosing and use additional medications."( A 1-year open-label trial of olanzapine in school-age children with schizophrenia.
Adler, LE; Farley, GK; Novins, D; Ross, RG, 2003
)
0.32
"Patients were randomly assigned to receive flexibly dosed olanzapine, 5 to 20 mg/d, with prophylactic benztropine, 1 to 4 mg/d (n = 159); or haloperidol, 5 to 20 mg/d (n = 150), for 12 months."( Effectiveness and cost of olanzapine and haloperidol in the treatment of schizophrenia: a randomized controlled trial.
Allan, E; Bingham, S; Campbell, EC; Caroff, S; Collins, J; Corwin, J; Davis, L; Douyon, R; Dunn, L; Evans, D; Frecska, E; Grabowski, J; Graeber, D; Herz, L; Kwon, K; Lawson, W; Leslie, D; Liu-Mares, W; Mena, F; Perlick, D; Rosenheck, R; Sheikh, J; Smelson, D; Smith-Gamble, V; Warren, S, 2003
)
0.32
"The design consisted of 2 successive, 6-week, double-blind periods and compared flexible dosing of olanzapine (5-20 mg/d, n = 234) with haloperidol (3-15 mg/d, n = 219)."( A 12-week, double-blind comparison of olanzapine vs haloperidol in the treatment of acute mania.
Azorin, JM; Baker, RW; Breier, A; Emsley, RA; Evans, AR; Goldberg, JF; Gonzalez-Pinto Arrillaga, AM; Hardy-Bayle, MC; Lawson, WB; Namjoshi, MA; Risser, RC; Tohen, M; Vieta, E; Zhang, F, 2003
)
0.32
" In the present study, blood samples were collected for 24 h after dosing rats orally with a 5 mg/kg dose of olanzapine (OLAN)."( An automated blood sampler for simultaneous sampling of systemic blood and brain microdialysates for drug absorption, distribution, metabolism, and elimination studies.
Gitzen, JF; Gunaratna, PC; Kissinger, CB; Kissinger, PT,
)
0.13
" The dose-response curves were shifted to the right by muscarinic antagonists in the following order of affinity: darifenacin (M(3))>methocramine (M(2)) >pirenzepine (M(1))."( Mechanisms mediating cholinergic antral circular smooth muscle contraction in rats.
Ouyang, A; Tandon, T; Wrzos, HF, 2004
)
0.52
" That some patients still yielded to acute organophosphate poisoning despite repeated dosing of atropine suggests that cellular mechanisms that are independent of muscarinic receptor activation may also be engaged in organophosphate poisoning."( Muscarinic receptor-independent activation of cyclic adenosine monophosphate-dependent protein kinase in rostral ventrolateral medulla underlies the sympathoexcitatory phase of cardiovascular responses during mevinphos intoxication in the rat.
Chan, SH; Chang, AY; Tsai, CY; Wu, CH, 2007
)
0.34
" Next, training was suspended and the mice received a maintenance dosing regimen in which they were injected twice daily with 10 mg/kg N-desmethylclozapine for 10 days."( The metabolites N-desmethylclozapine and N-desmethylolanzapine produce cross-tolerance to the discriminative stimulus of the atypical antipsychotic clozapine in C57BL/6 mice.
Meltzer, HY; Porter, JH; Webster, KA; Wiebelhaus, JM, 2011
)
0.37
" The method was successfully used for the analysis of samples from nonsmoking patients (n = 48) treated with OLZ in the dosage range of 5-20 mg per day."( Determination of olanzapine and N-desmethyl-olanzapine in plasma using a reversed-phase HPLC coupled with coulochemical detection: correlation of olanzapine or N-desmethyl-olanzapine concentration with metabolic parameters.
Chen, YC; Lin, CH; Lu, ML; Wu, TH; Yang, HC, 2013
)
0.39
" In order to test the hypothesis that the differential blockade of the muscarinic receptor subtypes would influence their potency and efficacy to prevent EPS, here we tested four anticholinergics with varying order of affinities for the muscarinic receptor subtypes, and compared their dose-response curves to inhibit haloperidol-induced catalepsy in male rats."( The potency and efficacy of anticholinergics to inhibit haloperidol-induced catalepsy in rats correlates with their rank order of affinities for the muscarinic receptor subtypes.
Alvarez-Cervera, FJ; Bata-García, JL; Erosa-Rivero, HB; Góngora-Alfaro, JL; Heredia-López, FJ, 2014
)
0.4
" TDM of both OLZ and DMO levels could assist clinical practice when individualizing OLZ dosage adjustments for patients with schizophrenia."( Application of Plasma Levels of Olanzapine and N-Desmethyl-Olanzapine to Monitor Clinical Efficacy in Patients with Schizophrenia.
Chen, CH; Chen, YH; Kuo, PT; Lin, CH; Lu, ML; Wu, TH; Wu, YX, 2016
)
0.43
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (3)

RoleDescription
anti-ulcer drugOne of various classes of drugs with different action mechanisms used to treat or ameliorate peptic ulcer or irritation of the gastrointestinal tract.
muscarinic antagonistA drug that binds to but does not activate muscarinic cholinergic receptors, thereby blocking the actions of endogenous acetylcholine or exogenous agonists.
antispasmodic drugA drug that suppresses spasms. These are usually caused by smooth muscle contraction, especially in tubular organs. The effect is to prevent spasms of the stomach, intestine or urinary bladder.
[role 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]

Drug Classes (1)

ClassDescription
pyridobenzodiazepineAny three-ring heterocyclic compound with a skeleton consisting of a pyridine ring ortho-fused to a benzodiazepine.
[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]

Pathways (1)

PathwayProteinsCompounds
Pirenzepine Action Pathway1012

Protein Targets (36)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
dopamine D1 receptorHomo sapiens (human)Potency3.66260.00521.30228.1995AID624455
ATAD5 protein, partialHomo sapiens (human)Potency2.59180.004110.890331.5287AID493107
GALC proteinHomo sapiens (human)Potency0.070828.183828.183828.1838AID1159614
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency25.11890.011212.4002100.0000AID1030
regulator of G-protein signaling 4Homo sapiens (human)Potency1.33710.531815.435837.6858AID504845
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency29.93490.035520.977089.1251AID504332
cytochrome P450 2D6 isoform 1Homo sapiens (human)Potency31.62280.00207.533739.8107AID891
D(1A) dopamine receptorHomo sapiens (human)Potency1.63590.02245.944922.3872AID488982
chromobox protein homolog 1Homo sapiens (human)Potency63.09570.006026.168889.1251AID488953
potassium voltage-gated channel subfamily H member 2 isoform dHomo sapiens (human)Potency8.91250.01789.637444.6684AID588834
ubiquitin carboxyl-terminal hydrolase 2 isoform aHomo sapiens (human)Potency12.58930.65619.452025.1189AID927
histone acetyltransferase KAT2A isoform 1Homo sapiens (human)Potency39.81070.251215.843239.8107AID504327
muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Potency0.11300.00106.000935.4813AID943; AID944
lamin isoform A-delta10Homo sapiens (human)Potency0.12590.891312.067628.1838AID1487
Disintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)Potency12.58931.584913.004325.1189AID927
Inositol monophosphatase 1Rattus norvegicus (Norway rat)Potency4.67961.000010.475628.1838AID1457
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency15.10140.060110.745337.9330AID485368
[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)
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
Muscarinic acetylcholine receptor M2Homo sapiens (human)IC50 (µMol)0.68910.00001.23267.7930AID142392; AID142779
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.37440.00000.690210.0000AID141156; AID142111; AID342990; AID723861
Muscarinic acetylcholine receptor M4Homo sapiens (human)IC50 (µMol)0.58560.00001.15467.5858AID1167257; AID1167263; AID1167267; AID141874
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.21630.00000.79519.1201AID141156; AID342992; AID723860
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)IC50 (µMol)0.61340.00052.773925.1700AID141543; AID141544; AID142622; AID142625; AID142626; AID142627; AID142629; AID142637; AID142639; AID142640; AID142645; AID142757; AID142758; AID142759; AID142760; AID142762; AID142763; AID142764; AID142767; AID142768; AID142772; AID142774; AID142776; AID142777; AID142779; AID142780; AID142781; AID142782; AID142886; AID142887; AID142889; AID142890; AID142892
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.05240.00010.579710.0000AID104026; AID141077; AID141834; AID142727
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)IC50 (µMol)0.62220.00052.891925.1700AID141543; AID141544; AID141606; AID142622; AID142625; AID142626; AID142627; AID142629; AID142637; AID142639; AID142640; AID142645; AID142757; AID142758; AID142759; AID142760; AID142762; AID142763; AID142764; AID142767; AID142768; AID142772; AID142774; AID142776; AID142777; AID142779; AID142780; AID142781; AID142782; AID142886; AID142887; AID142889; AID142890; AID142892
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.15330.00011.48339.1400AID141077; AID141727
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)IC50 (µMol)0.62270.00052.747825.1700AID141543; AID141544; AID142622; AID142625; AID142626; AID142627; AID142629; AID142637; AID142639; AID142640; AID142645; AID142757; AID142758; AID142759; AID142760; AID142762; AID142763; AID142764; AID142767; AID142768; AID142772; AID142774; AID142776; AID142777; AID142779; AID142780; AID142781; AID142782; AID142886; AID142887; AID142889; AID142890; AID142892
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.14620.00010.68688.2600AID101871; AID141077; AID142012
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)IC50 (µMol)0.62270.00052.780225.1700AID141543; AID141544; AID142622; AID142625; AID142626; AID142627; AID142629; AID142637; AID142639; AID142640; AID142645; AID142757; AID142758; AID142759; AID142760; AID142762; AID142763; AID142764; AID142767; AID142768; AID142772; AID142774; AID142776; AID142777; AID142779; AID142780; AID142781; AID142782; AID142886; AID142887; AID142889; AID142890; AID142892
Muscarinic acetylcholine receptor M5Rattus norvegicus (Norway rat)Ki0.11000.00010.66618.2600AID141077
Muscarinic acetylcholine receptor M5Homo sapiens (human)IC50 (µMol)0.34060.00010.99178.0000AID142149
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.23050.00000.72926.9183AID141156; AID302023; AID723858
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)IC50 (µMol)0.62810.00053.314249.5000AID141543; AID141544; AID142622; AID142625; AID142626; AID142627; AID142629; AID142637; AID142639; AID142640; AID142645; AID142757; AID142758; AID142759; AID142760; AID142762; AID142763; AID142764; AID142767; AID142768; AID142772; AID142774; AID142776; AID142777; AID142779; AID142780; AID142781; AID142782; AID142798; AID142865; AID142886; AID142887; AID142889; AID142890; AID142892
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki4.82860.00010.58908.2600AID141077; AID142876; AID34453
Muscarinic acetylcholine receptor M1Homo sapiens (human)IC50 (µMol)0.02910.00001.403910.0000AID1167235; AID1167243; AID1167251; AID1285636; AID1336331; AID141050; AID142291; AID1433976; AID255294; AID340252; AID346429; AID566265; AID751878; AID752238
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.05660.00000.59729.1201AID1152692; AID1196321; AID1196337; AID141156; AID1433976; AID1458653; AID238833; AID257195; AID302019; AID342989; AID346429; AID723863; AID751878
Muscarinic acetylcholine receptor M1Mus musculus (house mouse)IC50 (µMol)0.75000.00333.21788.9000AID141403
Muscarinic acetylcholine receptor DM1Drosophila melanogaster (fruit fly)Ki0.41000.00051.42495.2000AID1090601; AID1090602
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.04790.00010.739610.0000AID342991
Muscarinic acetylcholine receptor M3Homo sapiens (human)IC50 (µMol)0.95560.00011.01049.9280AID141348
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.24530.00000.54057.7600AID141156; AID342991; AID723862
Muscarinic acetylcholine receptor M4Mus musculus (house mouse)IC50 (µMol)0.75000.00333.21788.9000AID141403
Muscarinic acetylcholine receptorCavia porcellus (domestic guinea pig)Ki0.06570.00010.61203.8019AID141077; AID302019
Muscarinic acetylcholine receptor M5Mus musculus (house mouse)IC50 (µMol)0.75000.00333.21788.9000AID141403
Muscarinic acetylcholine receptor M3Mus musculus (house mouse)IC50 (µMol)0.75000.00333.21788.9000AID141403
Muscarinic acetylcholine receptor M2Mus musculus (house mouse)IC50 (µMol)0.51000.00333.22478.9000AID141403; AID142637; AID142639
[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)
Muscarinic acetylcholine receptor M1Homo sapiens (human)Kd0.02000.00090.98292.6915AID238154
[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)
Muscarinic acetylcholine receptor M1Homo sapiens (human)KA0.01100.01102.28076.8100AID141437
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (100)

Processvia Protein(s)Taxonomy
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of heart contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
response to virusMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M2Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M2Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M2Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M4Homo sapiens (human)
cell surface receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M4Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M4Homo sapiens (human)
gastric acid secretionMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
dopamine transportMuscarinic acetylcholine receptor M5Homo sapiens (human)
transmission of nerve impulseMuscarinic acetylcholine receptor M5Homo sapiens (human)
regulation of phosphatidylinositol dephosphorylationMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M5Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M5Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M5Homo sapiens (human)
positive regulation of monoatomic ion transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein kinase C-activating G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
neuromuscular synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of locomotionMuscarinic acetylcholine receptor M1Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M1Homo sapiens (human)
cognitionMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of postsynaptic membrane potentialMuscarinic acetylcholine receptor M1Homo sapiens (human)
regulation of glial cell proliferationMuscarinic acetylcholine receptor M1Homo sapiens (human)
positive regulation of intracellular protein transportMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M1Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M1Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M1Homo sapiens (human)
calcium-mediated signalingMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of monoatomic ion transmembrane transporter activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
signal transductionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
synaptic transmission, cholinergicMuscarinic acetylcholine receptor M3Homo sapiens (human)
nervous system developmentMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of insulin secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein modification processMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
saliva secretionMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ion channel modulating, G protein-coupled receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
ligand-gated ion channel signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
regulation of smooth muscle contractionMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messengerMuscarinic acetylcholine receptor M3Homo sapiens (human)
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathwayMuscarinic acetylcholine receptor M3Homo sapiens (human)
chemical synaptic transmissionMuscarinic acetylcholine receptor M3Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to hypoxiaDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
neutrophil mediated immunityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
germinal center formationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of leukocyte chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane protein ectodomain proteolysisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch receptor processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell population proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to xenobiotic stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of T cell chemotaxisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein processingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
signal releaseDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
B cell differentiationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell growthDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
response to lipopolysaccharideDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of chemokine productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor productionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
regulation of mast cell apoptotic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
T cell differentiation in thymusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell adhesion mediated by integrinDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
wound healing, spreading of epidermal cellsDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of blood vessel endothelial cell migrationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of cyclin-dependent protein serine/threonine kinase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor-activated receptor activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of epidermal growth factor receptor signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
spleen developmentDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell motilityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
defense response to Gram-positive bacteriumDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cellular response to high density lipoprotein particle stimulusDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
commissural neuron axon guidanceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
negative regulation of cold-induced thermogenesisDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of G1/S transition of mitotic cell cycleDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch signaling pathwayDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (27)

Processvia Protein(s)Taxonomy
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
arrestin family protein bindingMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M2Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M4Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M5Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M1Homo sapiens (human)
phosphatidylinositol phospholipase C activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
protein bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled acetylcholine receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
signaling receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
acetylcholine bindingMuscarinic acetylcholine receptor M3Homo sapiens (human)
G protein-coupled serotonin receptor activityMuscarinic acetylcholine receptor M3Homo sapiens (human)
endopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Notch bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
interleukin-6 receptor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
integrin bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
protein bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
peptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metallopeptidase activityDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
SH3 domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytokine bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
PDZ domain bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
tumor necrosis factor bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metal ion bindingDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
metalloendopeptidase activity involved in amyloid precursor protein catabolic processDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (35)

Processvia Protein(s)Taxonomy
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
clathrin-coated endocytic vesicle membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
asymmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
symmetric synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
neuronal cell bodyMuscarinic acetylcholine receptor M2Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M2Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M2Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M2Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M2Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M4Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M4Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M5Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M5Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
presynaptic membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
axon terminusMuscarinic acetylcholine receptor M1Homo sapiens (human)
Schaffer collateral - CA1 synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
postsynaptic density membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
glutamatergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
cholinergic synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M1Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M1Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M1Homo sapiens (human)
endoplasmic reticulum membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basal plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
basolateral plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
postsynaptic membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
synapseMuscarinic acetylcholine receptor M3Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Homo sapiens (human)
dendriteMuscarinic acetylcholine receptor M3Homo sapiens (human)
cell-cell junctionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
focal adhesionDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
ruffle membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
Golgi membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytoplasmDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
endoplasmic reticulum lumenDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cytosolDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
cell surfaceDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
actin cytoskeletonDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
apical plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
membrane raftDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneDisintegrin and metalloproteinase domain-containing protein 17Homo sapiens (human)
plasma membraneMuscarinic acetylcholine receptor M3Mus musculus (house mouse)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (322)

Assay IDTitleYearJournalArticle
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))1994FEBS letters, Sep-19, Volume: 352, Issue:1
A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
AID1345286Human M1 receptor (Acetylcholine receptors (muscarinic))1991British journal of pharmacology, Jan, Volume: 102, Issue:1
Selectivity profile of the novel muscarinic antagonist UH-AH 37 determined by the use of cloned receptors and isolated tissue preparations.
AID1345465Human M4 receptor (Acetylcholine receptors (muscarinic))2001AAPS pharmSci, , Volume: 3, Issue:4
Receptor binding studies of soft anticholinergic agents.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))1998The Journal of pharmacology and experimental therapeutics, Feb, Volume: 284, Issue:2
Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
AID1345465Human M4 receptor (Acetylcholine receptors (muscarinic))1991British journal of pharmacology, Jan, Volume: 102, Issue:1
Selectivity profile of the novel muscarinic antagonist UH-AH 37 determined by the use of cloned receptors and isolated tissue preparations.
AID1345343Human M3 receptor (Acetylcholine receptors (muscarinic))1994FEBS letters, Sep-19, Volume: 352, Issue:1
A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
AID1345511Rat M5 receptor (Acetylcholine receptors (muscarinic))1992Life sciences, , Volume: 51, Issue:12
Cloning of the rat M3, M4 and M5 muscarinic acetylcholine receptor genes by the polymerase chain reaction (PCR) and the pharmacological characterization of the expressed genes.
AID1345465Human M4 receptor (Acetylcholine receptors (muscarinic))1997British journal of pharmacology, Apr, Volume: 120, Issue:8
Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo.
AID1345286Human M1 receptor (Acetylcholine receptors (muscarinic))1989Molecular pharmacology, Apr, Volume: 35, Issue:4
Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
AID1345699Rat M3 receptor (Acetylcholine receptors (muscarinic))1992Life sciences, , Volume: 51, Issue:12
Cloning of the rat M3, M4 and M5 muscarinic acetylcholine receptor genes by the polymerase chain reaction (PCR) and the pharmacological characterization of the expressed genes.
AID1345364Rat M2 receptor (Acetylcholine receptors (muscarinic))1992Life sciences, , Volume: 51, Issue:12
Cloning of the rat M3, M4 and M5 muscarinic acetylcholine receptor genes by the polymerase chain reaction (PCR) and the pharmacological characterization of the expressed genes.
AID1345343Human M3 receptor (Acetylcholine receptors (muscarinic))1997British journal of pharmacology, Apr, Volume: 120, Issue:8
Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo.
AID1345364Rat M2 receptor (Acetylcholine receptors (muscarinic))1988The EMBO journal, Oct, Volume: 7, Issue:10
Cloned M1 muscarinic receptors mediate both adenylate cyclase inhibition and phosphoinositide turnover.
AID1345343Human M3 receptor (Acetylcholine receptors (muscarinic))1989Molecular pharmacology, Apr, Volume: 35, Issue:4
Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
AID1345465Human M4 receptor (Acetylcholine receptors (muscarinic))1991The Journal of pharmacology and experimental therapeutics, Feb, Volume: 256, Issue:2
Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
AID1345543Human M5 receptor (Acetylcholine receptors (muscarinic))1994FEBS letters, Sep-19, Volume: 352, Issue:1
A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))1989Molecular pharmacology, Apr, Volume: 35, Issue:4
Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))2006The Journal of pharmacology and experimental therapeutics, Jan, Volume: 316, Issue:1
Constitutive activity and inverse agonism at the M2 muscarinic acetylcholine receptor.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))1997British journal of pharmacology, Apr, Volume: 120, Issue:8
Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo.
AID1345465Human M4 receptor (Acetylcholine receptors (muscarinic))1994FEBS letters, Sep-19, Volume: 352, Issue:1
A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
AID1345543Human M5 receptor (Acetylcholine receptors (muscarinic))1991British journal of pharmacology, Jan, Volume: 102, Issue:1
Selectivity profile of the novel muscarinic antagonist UH-AH 37 determined by the use of cloned receptors and isolated tissue preparations.
AID1345343Human M3 receptor (Acetylcholine receptors (muscarinic))1991British journal of pharmacology, Jan, Volume: 102, Issue:1
Selectivity profile of the novel muscarinic antagonist UH-AH 37 determined by the use of cloned receptors and isolated tissue preparations.
AID1345435Rat M4 receptor (Acetylcholine receptors (muscarinic))1992Life sciences, , Volume: 51, Issue:12
Cloning of the rat M3, M4 and M5 muscarinic acetylcholine receptor genes by the polymerase chain reaction (PCR) and the pharmacological characterization of the expressed genes.
AID1345286Human M1 receptor (Acetylcholine receptors (muscarinic))2001AAPS pharmSci, , Volume: 3, Issue:4
Receptor binding studies of soft anticholinergic agents.
AID1345286Human M1 receptor (Acetylcholine receptors (muscarinic))1991The Journal of pharmacology and experimental therapeutics, Feb, Volume: 256, Issue:2
Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
AID1345286Human M1 receptor (Acetylcholine receptors (muscarinic))1994FEBS letters, Sep-19, Volume: 352, Issue:1
A toxin from the green mamba Dendroaspis angusticeps: amino acid sequence and selectivity for muscarinic m4 receptors.
AID1345189Rat M1 receptor (Acetylcholine receptors (muscarinic))1992Life sciences, , Volume: 51, Issue:12
Cloning of the rat M3, M4 and M5 muscarinic acetylcholine receptor genes by the polymerase chain reaction (PCR) and the pharmacological characterization of the expressed genes.
AID1345343Human M3 receptor (Acetylcholine receptors (muscarinic))2001AAPS pharmSci, , Volume: 3, Issue:4
Receptor binding studies of soft anticholinergic agents.
AID1345364Rat M2 receptor (Acetylcholine receptors (muscarinic))1998The Journal of pharmacology and experimental therapeutics, Feb, Volume: 284, Issue:2
Pharmacological comparison of the cloned human and rat M2 muscarinic receptor genes expressed in the murine fibroblast (B82) cell line.
AID1345543Human M5 receptor (Acetylcholine receptors (muscarinic))1997British journal of pharmacology, Apr, Volume: 120, Issue:8
Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo.
AID1345189Rat M1 receptor (Acetylcholine receptors (muscarinic))1989Molecular pharmacology, Apr, Volume: 35, Issue:4
Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells.
AID1345286Human M1 receptor (Acetylcholine receptors (muscarinic))1997British journal of pharmacology, Apr, Volume: 120, Issue:8
Functional role of M2 and M3 muscarinic receptors in the urinary bladder of rats in vitro and in vivo.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))2001AAPS pharmSci, , Volume: 3, Issue:4
Receptor binding studies of soft anticholinergic agents.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))1991British journal of pharmacology, Jan, Volume: 102, Issue:1
Selectivity profile of the novel muscarinic antagonist UH-AH 37 determined by the use of cloned receptors and isolated tissue preparations.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))1991The Journal of pharmacology and experimental therapeutics, Feb, Volume: 256, Issue:2
Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
AID1345343Human M3 receptor (Acetylcholine receptors (muscarinic))1991The Journal of pharmacology and experimental therapeutics, Feb, Volume: 256, Issue:2
Antagonist binding profiles of five cloned human muscarinic receptor subtypes.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID504836Inducers of the Endoplasmic Reticulum Stress Response (ERSR) in human glioma: Validation2002The Journal of biological chemistry, Apr-19, Volume: 277, Issue:16
Sustained ER Ca2+ depletion suppresses protein synthesis and induces activation-enhanced cell death in mast cells.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID588378qHTS for Inhibitors of ATXN expression: Validation
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID588349qHTS for Inhibitors of ATXN expression: Validation of Cytotoxic Assay
AID1347045Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot counterscreen GloSensor control cell line2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347049Natriuretic polypeptide receptor (hNpr1) antagonism - Pilot screen2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347050Natriuretic polypeptide receptor (hNpr2) antagonism - Pilot subtype selectivity assay2019Science translational medicine, 07-10, Volume: 11, Issue:500
Inhibition of natriuretic peptide receptor 1 reduces itch in mice.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID135327BBB penetration classification2000Journal of medicinal chemistry, Jun-01, Volume: 43, Issue:11
Predicting blood-brain barrier permeation from three-dimensional molecular structure.
AID142291Compound was tested for its binding affinity against M1 human recombinant muscarinic receptor in CHO cells.1999Bioorganic & medicinal chemistry letters, Oct-04, Volume: 9, Issue:19
Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID142644Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of dorsomedial hypothalamus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142638Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of cuneiform nucleus region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID91833Binding affinity against imipramine receptor was determined in homogenized rat cortex tissue using [3H]-imipramine as radioligand1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Tricyclic compounds as selective antimuscarinics. 1. Structural requirements for selectivity toward the muscarinic acetylcholine receptor in a series of pirenzepine and imipramine analogues.
AID474278Selectivity for muscarinic M1 receptor over muscarinic M5 receptor2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
AID142636Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of cerebral cortex layers VI of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142761Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of lateral hypothalamus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID342992Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M4 receptor expressed in CHOK1 cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
AID1167268Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID723861Binding affinity to human M2 muscarinic receptor2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID28681Partition coefficient (logD6.5)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID142764Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of medial geniculate region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1167263Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID142629Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of central medial thalamic nucleus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1090601Displacement of [3H]QNB from Drosophila melanogaster mAChR by scintillation counting2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID566265Inhibition of human muscarinic M1 receptor2010Bioorganic & medicinal chemistry, Nov-01, Volume: 18, Issue:21
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: de
AID142625Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of basolateral amygdaloid nucleus region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID723863Binding affinity to human M1 muscarinic receptor2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID141403Ability (10 ug/kg) to inhibit binding of [125I]iododexetimide to muscarinic receptor in mice1989Journal of medicinal chemistry, May, Volume: 32, Issue:5
Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.
AID238002Apparent dissociation constant for human muscarinic receptor M1 from FRET binding assay2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.
AID320528Selectivity for rat muscarinic M1 receptor over rat muscarinic M2 receptor by calcium mobilization assay2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
AID342993Antagonist activity at peripheral muscarinic M2 receptor in guinea pig left atrium assessed as effect on arecaidin propargyl ester-induced contraction after 1 hr2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
AID142798Binding affinity to the rat cardiac muscarinic acetylcholine receptor M2 using 0.3 nM [3H]N-methylscopolamine as radioligand1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Tricyclic compounds as selective muscarinic receptor antagonists. 3. Structure-selectivity relationships in a series of cardioselective (M2) antimuscarinics.
AID141050Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M1 using membranes from transfected CHO cells1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Identification and characterization of m1 selective muscarinic receptor antagonists1.
AID1090593Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 0.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID142634Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of cerebral cortex layers I-III of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142781Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of superior coliculus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142392Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M2 using membranes from transfected CHO cells1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Identification and characterization of m1 selective muscarinic receptor antagonists1.
AID101728Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Synthesis and biodistribution of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate. A new ligand for the potential imaging of muscarinic receptors by single photon emission computed tomography.
AID1895280Displacement of [3H]-QNB from Wistar rat brain membrane mAChR assessed as inhibition constant incubated for 30 mins by radioligand competitive binding assay2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Rational Design of Photochromic Analogues of Tricyclic Drugs.
AID27167Delta logD (logD6.5 - logD7.4)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID142762Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of medial amygdaloid nucleus region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID455986Permeability across human Caco-2 cells2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID257195Displacement of [3H]QNB from EGFP(delta-17)human M1 receptor expressed in HEK cells2005Journal of medicinal chemistry, Dec-01, Volume: 48, Issue:24
On the use of nonfluorescent dye labeled ligands in FRET-based receptor binding studies.
AID474281Selectivity ratio of muscarinic M1 receptor over muscarinic M3 receptor2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
AID342990Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M2 receptor expressed in CHOK1 cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
AID142876Tested for affinity constant against M2 muscarinic receptor rat heart using [3H]-NMS1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Design, synthesis, and biological activity of methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4] benzodiazepin-6-one moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed b
AID1090594Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 24 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID346429Displacement of radiolabeled pirenzepine from human muscarinic M1 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.
AID142955Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M2 of rat heart tissue membrane.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID142892Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of zona inserta region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID141023Tested for affinity constant against M4 muscarinic receptor in NG 108-15 cell homogenates using [3H]NMS1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Design, synthesis, and biological activity of methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4] benzodiazepin-6-one moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed b
AID1090598Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 0.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID1895287Anticholinergic activity in isolated CD1 mouse CCh-induced bradycardia atrium assessed as recovery of CCh-indued contraction frequency at 100 uM2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Rational Design of Photochromic Analogues of Tricyclic Drugs.
AID142631Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of cerebellum, lobe 2 region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID340252Inhibition of human muscarinic M1 receptor2008Journal of medicinal chemistry, Jul-24, Volume: 51, Issue:14
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID142774Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of reticular thalamic nucleus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142950Displacement of [3H](-)-quinuclidinyl benzilate(QNB) from muscarinic (M2) receptor in rat heart homogenates1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
Muscarinic receptor binding profile of para-substituted caramiphen analogues.
AID1167244Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID1090590Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 2.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID255294Percent inhibition against Muscarinic acetylcholine receptor M1 at 1 uM2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
AID232600Ratio of IC50 (gastric fundus) to IC50 (cortex)1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine.
AID142622Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of Primary olfactory cortex region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142630Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of cerebellum, lobe 1 region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID288185Permeability coefficient through artificial membrane in presence of stirred water layer2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID142889Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of ventral posterior thalamic nucleus region of brain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142641Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of dorsal parabrachial nucleus region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID234497Ratio IC50 values of Muscarinic M2 receptor and muscarinic M1 receptor1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1458653Displacement of [3H]-pyrilamine from human recombinant M1 receptor expressed in CHO cells after 60 mins by scintillation counting2017Journal of medicinal chemistry, 09-14, Volume: 60, Issue:17
Novel 3-(1,2,3,6-Tetrahydropyridin-4-yl)-1H-indole-Based Multifunctional Ligands with Antipsychotic-Like, Mood-Modulating, and Procognitive Activity.
AID141009Displacement of [3H]methylscopolamine binding to muscarinic M3 receptor in submaxillary salivary glands of rats.1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.
AID234498Ratio IC50 values of Muscarinic M3 receptor and muscarinic M1 receptor1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.
AID29359Ionization constant (pKa)2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID1167257Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID1895281Displacement of [3H]-QNB from Wistar rat brain membrane mAChR incubated for 30 mins by radioligand competitive binding assay2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Rational Design of Photochromic Analogues of Tricyclic Drugs.
AID142765Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of medial raphe nucleus region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID1285636Displacement of [3H]pirenzepine from human recombinant muscarinic M1 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.
AID140922Inhibition of carbachol-induced release of alpha-amylase from pancreatic acinar cells from that of rat ileum contained the muscarinic acetylcholine receptor M2 subtypes1989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
AID141858Binding affinity to Muscarinic acetylcholine receptor M1 by measuring its ability to displace [3H]pirenzepine from rat cerebral cortex1998Journal of medicinal chemistry, Aug-13, Volume: 41, Issue:17
Synthesis and pharmacological characterization of O-alkynyloximes of tropinone and N-methylpiperidinone as muscarinic agonists.
AID142012Inhibition of binding of [3H]N-Methyl-scopolamine to muscarinic acetylcholine receptor M4 of rat heart NG108-15 cells1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.
AID29812Oral bioavailability in human2000Journal of medicinal chemistry, Jun-29, Volume: 43, Issue:13
QSAR model for drug human oral bioavailability.
AID233598Ratio of Ki (M1 receptor) to Ki (M2 receptor) was determined1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
Muscarinic receptor binding profile of para-substituted caramiphen analogues.
AID185122The antiulcer activity against stress-induced ulcer in rats by 30 mg/kg peroral administration.1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID238833Inhibition of [3H]QNB binding to human muscarinic receptor M12004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.
AID142129Antimuscarinic activity on the acetylcholine-induced inhibition of contraction of guinea pig ileum which has Muscarinic acetylcholine receptor M21989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
AID751878Binding affinity to human muscarinic M1 receptor by radioligand displacement assay2013European journal of medicinal chemistry, May, Volume: 63Synthesis and structure-activity relationship studies in serotonin 5-HT(1A) receptor agonists based on fused pyrrolidone scaffolds.
AID142639Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of dentate gyrus region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID142149Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M5 using membranes from transfected CHO cells1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Identification and characterization of m1 selective muscarinic receptor antagonists1.
AID1090602Displacement of [3H]AF-DX 384 from Drosophila melanogaster mAChR by scintillation counting2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID142628Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of central gray, pons region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142624Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of anterior hypothalamus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID142779Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of subiculum region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID141141In vitro functional activity in isolated urinary bladder strips from Guinea Pig; Not determined1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.
AID744641Inhibition of muscarinic acetylcholine receptor in rat cortex2013Bioorganic & medicinal chemistry, May-01, Volume: 21, Issue:9
Discovery of subtype selective muscarinic receptor antagonists as alternatives to atropine using in silico pharmacophore modeling and virtual screening methods.
AID141453Binding affinity towards Muscarinic acetylcholine receptor M1 of cerebral cortex1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine.
AID1167243Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID142778Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of rhomboid thalamic nucleus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID141544In vitro inhibition of [3H]QNB binding to Muscarinic receptor from rat cortical homogenates1992Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7
Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.
AID142921Binding affinity against Muscarinic acetylcholine receptor M1 by displacement of [3H]pirenzepine in bovine striatum1988Journal of medicinal chemistry, Jul, Volume: 31, Issue:7
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.
AID302019Displacement of [3H]QNB from human muscarinic M1 receptor expressed in CHO cells2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID142627Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of central amygdaloid nucleus region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID141348Displacement of [3H]-NMS binding to human Muscarinic acetylcholine receptor M3 using membranes from transfected CHO cells1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Identification and characterization of m1 selective muscarinic receptor antagonists1.
AID1193905Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and biological evaluation of isoxazoline derivatives as potent M₁ muscarinic acetylcholine receptor agonists.
AID1091958Hydrophobicity, log P of the compound in octanol-water by shaking-flask method2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID142626Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of bed nucleus stria terminalis region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID141156Binding affinity for muscarinic acetylcholine receptor by measuring displacement of [3H]QNB from guinea pig urinary bladder1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.
AID142727Tested for affinity constant against M1 muscarinic receptor in rat cortex using [3H]pirenzepine1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Design, synthesis, and biological activity of methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4] benzodiazepin-6-one moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed b
AID288184Permeability coefficient through artificial membrane in presence of unstirred water layer by PAMPA2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID141011Tested for affinity constant against M3 muscarinic receptor in rat submaxillary gland using [3H]NMS1994Journal of medicinal chemistry, Sep-30, Volume: 37, Issue:20
Design, synthesis, and biological activity of methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4] benzodiazepin-6-one moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed b
AID141543In vitro inhibition of [3H]OXO-M binding to Muscarinic receptor from rat cortical homogenates1992Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7
Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.
AID1196321Inhibition of muscarinic M1 receptor (unknown origin) assessed as reduction in control ligand binding2015European journal of medicinal chemistry, Mar-06, Volume: 92Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.
AID342991Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M3 receptor expressed in CHOK1 cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
AID232369Ratio of Compound (IC50(nM) of QNB/ IC50(nM) of OXO-M)1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands.
AID320530Selectivity for rat muscarinic M1 receptor over rat muscarinic M4 receptor by calcium mobilization assay2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
AID1167258Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID142637Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of cudate nucleus region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142769Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of pontine nuclei region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID101871Affinity constant measured against M4 muscarinic receptor rat NG108-15 cells1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
AID1090596Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 1.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID1167235Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID141955Percentage inhibition for muscarinic acetylcholine receptor at concentration 10e-6 M.1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.
AID231529Ratio of binding affinity towards M2 (bovine striatum) to M1 (rat myocardium) receptor1988Journal of medicinal chemistry, Jul, Volume: 31, Issue:7
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.
AID142803Binding affinity towards muscarinic receptor of gastric fundus containing Muscarinic acetylcholine receptor M21988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine.
AID141874Displacement of [3H]NMS binding to human Muscarinic acetylcholine receptor M4 using membranes from transfected CHO cells1999Journal of medicinal chemistry, Feb-11, Volume: 42, Issue:3
Identification and characterization of m1 selective muscarinic receptor antagonists1.
AID142640Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of dorsal lateral geniculate region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID142772Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of posterior thalamic nucleus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID141834Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M1 of transfected rat A9L cells.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.
AID104026Affinity constant measured against M1 muscarinic receptor in rat cortex1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
AID141534In vitro displacement of [3H]quinuclidinyl benzilate (QNB) from rat cerebral cortex muscarinic receptor.1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands.
AID231933Ratio for Ki for M2 (inhibition of adenylate cyclase of rat heart) to Ki for M1 (phosphatidyl inositol turnover in rat cortex)1988Journal of medicinal chemistry, Jul, Volume: 31, Issue:7
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.
AID140891Inhibition of [3H]NMS binding to cerebral cortex membranes which contain predominantly the muscarinic acetylcholine receptor M11989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
AID142750Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of hippocampus CA1 region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID101707Affinity constant measured against M2 muscarinic receptor in rat heart r1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
AID723862Binding affinity to human M3 muscarinic receptor2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID1091957Apparent permeability of the compound by PAMPA2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID320531Selectivity for rat muscarinic M1 receptor over rat muscarinic M5 receptor by calcium mobilization assay2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
AID1193907Antagonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as inhibition of acetylcholine-induced calcium mobilization at 10 microM by FLIPR assay2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and biological evaluation of isoxazoline derivatives as potent M₁ muscarinic acetylcholine receptor agonists.
AID142758Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of lateral dorsal thalamic nucleus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142759Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of lateral posterior thalamic nucleus region of mid brain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1091955Dissociation constant, pKa of the compound at pH 7.32011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID1167264Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID752238Binding affinity to human muscarinic M1 receptor by radioligand displacement assay2013Bioorganic & medicinal chemistry, May-15, Volume: 21, Issue:10
Synthesis and biological evaluation of 2-(5-methyl-4-phenyl-2-oxopyrrolidin-1-yl)-acetamide stereoisomers as novel positive allosteric modulators of sigma-1 receptor.
AID19424Partition coefficient (logD7.4)2001Journal of medicinal chemistry, Jul-19, Volume: 44, Issue:15
ElogD(oct): a tool for lipophilicity determination in drug discovery. 2. Basic and neutral compounds.
AID142642Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of dorsal raphe nucleus region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID185121Inhibition of stress-induced ulcer formation in rats by 10 mg/kg p.o. administration.1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.
AID141734Selectivity ratio for glandular muscarinic receptor 3 and cardiac muscarinic receptor 2 in rat1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Tricyclic compounds as selective muscarinic receptor antagonists. 3. Structure-selectivity relationships in a series of cardioselective (M2) antimuscarinics.
AID1196337Displacement of [3H]pirenzepine from human muscarinic M1 receptor expressed in CHO cells2015European journal of medicinal chemistry, Mar-06, Volume: 92Novel 5-HT6 receptor antagonists/D2 receptor partial agonists targeting behavioral and psychological symptoms of dementia.
AID142865Displacement of [3H]methylscopolamine binding to muscarinic M2 receptor in rat heart.1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.
AID141437Displacement of [3H]pirenzepine from Muscarinic acetylcholine receptor M1 in rabbit sympathetic ganglia homogenate1992Journal of medicinal chemistry, Jul-24, Volume: 35, Issue:15
Amide, urea, and carbamate analogues of the muscarinic agent [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride.
AID302023Displacement of [3H]QNB from human muscarinic M5 receptor expressed in CHO cells2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Novel oxotremorine-related heterocyclic derivatives: Synthesis and in vitro pharmacology at the muscarinic receptor subtypes.
AID233269Selectivity ratio between heart (M2) and cortex (M1) was determined1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
AID1193906Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells by calcium mobilization assay at 10 microM by FLIPR assay relative to 100 nM acetylcholine response2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and biological evaluation of isoxazoline derivatives as potent M₁ muscarinic acetylcholine receptor agonists.
AID142751Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of hippocampus CA3 region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID141727Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Functionalized congener approach to muscarinic antagonists: analogues of pirenzepine.
AID1090589Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 24 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID288192Partition coefficient, log P of the compound2007Bioorganic & medicinal chemistry, Jun-01, Volume: 15, Issue:11
QSAR study on permeability of hydrophobic compounds with artificial membranes.
AID142768Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of periaqueductal region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID474279Selectivity ratio of muscarinic M1 receptor over muscarinic M4 receptor2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
AID142886Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of ventral dentate gyrus region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID142752Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of hippocampus CA4 region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142888Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of ventral parabrachial nucleus region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142935Binding affinity against Muscarinic acetylcholine receptor M2 by displacement of [3H]QNB in rat myocardium1988Journal of medicinal chemistry, Jul, Volume: 31, Issue:7
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.
AID23248Partition coefficient (log P) at pH 7.41988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
Tricyclic compounds as selective antimuscarinics. 2. Structure-activity relationships of M1-selective antimuscarinics related to pirenzepine.
AID140897Binding affinity for muscarinic acetylcholine receptor M1 by measuring displacement of [3H]QNB from guinea pig cerebral cortex1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.
AID1090597Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 1 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID77620Antimuscarinic activity was assayed for its ability to block the acetyl-choline induced contraction of the guinea pig ileum1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.
AID1336331Displacement of [3H]pirenzepine from human recombinant M1 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
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID1090591Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 1.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID142891Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of ventromedial hypothalamus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142776Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of retrosplenial cortex region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID104018Ability to displace [3H]pirenzepine (PZ) from M1 receptor in rat cortex homogenate1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Synthesis and biodistribution of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate. A new ligand for the potential imaging of muscarinic receptors by single photon emission computed tomography.
AID233261Selectivity ratio between Heart (M2) and gland (M3) was determined1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
AID141077Binding affinity for muscarinic acetylcholine receptor M3 by measuring displacement of [3H]QNB from guinea pig parotid gland1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.
AID196390Evaluated for the phosphatidyl inositol turnover at Muscarinic acetylcholine receptor M1 in rat cortex1988Journal of medicinal chemistry, Jul, Volume: 31, Issue:7
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.
AID1090595Toxicity to Musca domestica (house fly) assessed as mortality at 25 ug/fly measured after 2.5 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID320529Selectivity for rat muscarinic M1 receptor over rat muscarinic M3 receptor by calcium mobilization assay2008Bioorganic & medicinal chemistry letters, Feb-01, Volume: 18, Issue:3
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
AID1167236Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID233259Selectivity ratio between Heart (M2) and NG108-15 (M4) was determined1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
AID1167251Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based beta-arrestin engagement assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID142220Binding affinity against Muscarinic acetylcholine receptor was determined in homogenized rat cortex tissue using [3H]N-methylscopolamine as radioligand1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Tricyclic compounds as selective antimuscarinics. 1. Structural requirements for selectivity toward the muscarinic acetylcholine receptor in a series of pirenzepine and imipramine analogues.
AID142773Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of raphe pontis region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID101556Ability to displace [3H](-)-quinuclidinyl benzilate(QNB) from M2 receptor in rat heart homogenate1993Journal of medicinal chemistry, Apr-02, Volume: 36, Issue:7
Synthesis and biodistribution of iodine-125-labeled 1-azabicyclo[2.2.2]oct-3-yl alpha-hydroxy-alpha-(1-iodo-1-propen-3-yl)-alpha-phenylacetate. A new ligand for the potential imaging of muscarinic receptors by single photon emission computed tomography.
AID142635Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of cerebral cortex layers IV and V of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID101736Affinity constant measured against M3 muscarinic receptor in rat submaxillary gland1993Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
AID1091956Apparent hydrophobicity, log D of the compound in Octanol-buffer2011Journal of agricultural and food chemistry, Apr-13, Volume: 59, Issue:7
Importance of physicochemical properties for the design of new pesticides.
AID142782Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of superior coliculus, infragranular region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142715Displacement of [3H]pirenzepine binding to muscarinic M1 receptor in brain cortex of rat.1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.
AID142632Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of cerebellum, lobe 3 region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID229750Ratio of inhibition of QNB to OXO-M binding to Muscarinic receptor1992Journal of medicinal chemistry, Apr-03, Volume: 35, Issue:7
Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.
AID141829Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 in rat cortex homogenates1991Journal of medicinal chemistry, Oct, Volume: 34, Issue:10
Muscarinic receptor binding profile of para-substituted caramiphen analogues.
AID1433976Displacement of [3H]pirenzepine from human recombinant Muscarinic acetylcholine receptor M1 expressed in CHO cells after 60 mins by scintillation counting2017Journal of medicinal chemistry, 01-12, Volume: 60, Issue:1
Pyrimidine-Based Inhibitors of Dynamin I GTPase Activity: Competitive Inhibition at the Pleckstrin Homology Domain.
AID142770Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of posterior cingulate cortex region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID141606Binding affinity for glandular muscarinic acetylcholine receptor M3 in rat assayed using 0.3 nM [3H]N-methylscopolamine as radioligand1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Tricyclic compounds as selective muscarinic receptor antagonists. 3. Structure-selectivity relationships in a series of cardioselective (M2) antimuscarinics.
AID142756Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of inferior coliculus region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID723858Binding affinity to human M5 muscarinic receptor2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID142766Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of neostriatum region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID238154Apparent dissociation constant for human muscarinic receptor M1 from FRET based binding assay2004Journal of medicinal chemistry, Aug-12, Volume: 47, Issue:17
Fluorescent pirenzepine derivatives as potential bitopic ligands of the human M1 muscarinic receptor.
AID342989Displacement of [3H]N-methylscopolamine chloride from human cloned muscarinic M1 receptor expressed in CHOK1 cells2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
AID142757Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of lateral amygdaloid nucleus region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142106Antimuscarinic activity on the acetylcholine-induced inhibition of contraction of guinea pig ileum which has muscarinic acetylcholine receptor M21989Journal of medicinal chemistry, Jul, Volume: 32, Issue:7
Binary antidotes for organophosphate poisoning: aprophen analogues that are both antimuscarinics and carbamates.
AID142633Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of cerebellum, lobe 4 region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1167267Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID141953Percentage inhibition for muscarinic acetylcholine receptor at concentration 10 e-5M.1988Journal of medicinal chemistry, Apr, Volume: 31, Issue:4
Synthesis and antiulcer activity of 5,11-dihydro[1]benzoxepino[3,4-b]pyridines.
AID157520Inhibition of carbachol-induced release of alpha-amylase from pancreatic acini from rat was determined1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.
AID342994Antagonist activity at peripheral muscarinic M3 receptor in guinea pig longitudinal ileum assessed as effect on arecaidin propargyl ester-induced contraction after 1 hr2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
AID142623Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of anterior cingulate cortex region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142777Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of reuniens thalamic nucleus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142887Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of ventral lateral geniculate region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142780Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of substantia nigra region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID474280Selectivity ratio of muscarinic M1 receptor over muscarinic M2 receptor2010Bioorganic & medicinal chemistry letters, Apr-01, Volume: 20, Issue:7
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
AID141531In vitro ability to displace [3H]oxotremorine-M (OXO-M) from rat cerebral cortex muscarinic receptor.1992Journal of medicinal chemistry, Jun-26, Volume: 35, Issue:13
Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands.
AID1090592Toxicity to Musca domestica (house fly) assessed as mortality at 75 ug/fly measured after 1 hr2007Journal of agricultural and food chemistry, Mar-21, Volume: 55, Issue:6
Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists.
AID342995Antagonist activity at peripheral muscarinic M4 receptor in rabbit vas deferens assessed as effect on McN-A-343-induced contraction after 1 hr2008Bioorganic & medicinal chemistry, Aug-01, Volume: 16, Issue:15
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
AID142763Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of medial dorsal thalamic nucleus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142111Binding affinity for muscarinic acetylcholine receptor M2 by measuring displacement of [3H]QNB from guinea pig heart1995Journal of medicinal chemistry, Feb-03, Volume: 38, Issue:3
3-Heteroaryl-substituted quinuclidin-3-ol and quinuclidin-2-ene derivatives as muscarinic antagonists. Synthesis and structure-activity relationships.
AID142771Inhibition of binding of [3H]L-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of posterior hypothalamus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142760Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]-l-QNB) to muscarinic acetylcholine receptor of lateral septal nucleus of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142890Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of ventral subiculum region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID1152692Displacement of [3H]pirenzepine from human recombinant M1 receptor expressed in CHO cells2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel arylsulfonamide derivatives with 5-HT₆/5-HT₇ receptor antagonism targeting behavioral and psychological symptoms of dementia.
AID34453Evaluated for the inhibition of adenylate cyclase at M2 receptor in rat heart1988Journal of medicinal chemistry, Jul, Volume: 31, Issue:7
Affinity and selectivity of the optical isomers of 3-quinuclidinyl benzilate and related muscarinic antagonists.
AID142645Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of entorhinal cortex region of forebrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID142767Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of paraventricular thalamic nucleus region of midbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID723860Binding affinity to human M4 muscarinic receptor2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
AID142643Inhibition of binding of [3H]l-quinuclidinyl benzilate ([3H]L-QNB) to muscarinic acetylcholine receptor of dorsal tegmentum region of hindbrain1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Regional differences in the binding of selective muscarinic receptor antagonists in rat brain: comparison with minimum-energy conformations.
AID79352Antimuscarinic activity was assayed for its ability to block the acetyl-choline induced contraction of the guinea pig ileum1987Journal of medicinal chemistry, May, Volume: 30, Issue:5
6-Methyl-6-azabicyclo[3.2.1]octan-3 alpha-ol 2,2-diphenylpropionate (azaprophen), a highly potent antimuscarinic agent.
AID1167252Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based beta-arrestin engagement assay relative to untreated control2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Synthesis and biological evaluation of a novel series of heterobivalent muscarinic ligands based on xanomeline and 1-[3-(4-butylpiperidin-1-yl)propyl]-1,2,3,4-tetrahydroquinolin-2-one (77-LH-28-1).
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
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.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
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.
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.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (3,595)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990907 (25.23)18.7374
1990's1315 (36.58)18.2507
2000's1214 (33.77)29.6817
2010's138 (3.84)24.3611
2020's21 (0.58)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 59.52

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

MetricThis Compound (vs All)
Research Demand Index59.52 (24.57)
Research Supply Index8.39 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index105.55 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (59.52)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials587 (15.40%)5.53%
Reviews280 (7.35%)6.00%
Case Studies451 (11.83%)4.05%
Observational0 (0.00%)0.25%
Other2,494 (65.42%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized, Double-blind, Placebo-controlled, Parallel, 12-week, Phase 2a Study of Topical Pirenzepine (WST-057) or Placebo in Type 2 Diabetes Mellitus Patients With Painful Peripheral Neuropathy [NCT04786340]Phase 258 participants (Actual)Interventional2020-11-20Completed
A Randomized, Double-Blind, Placebo-Controlled, Parallel, 24-Week, Phase 2a Study of Topical Pirenzepine (WST-057) or Placebo in Type 2 Diabetic Patients With Peripheral Neuropathy [NCT04005287]Phase 258 participants (Actual)Interventional2019-10-15Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]