Page last updated: 2024-12-07

tripitramine

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Description

tripitramine: structure given in first source; preferentially binds to M2 receptors [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID132947
CHEMBL ID265256
SCHEMBL ID20584784
MeSH IDM0224415

Synonyms (16)

Synonym
6h-pyrido(2,3-b)(1,4)benzodiazepin-6-one, 11,11'-(3-(2-(5,6-dihydro-6-oxo-11h-pyrido(2,3-b)(1,4)benzodiazepin-11-yl)-2-oxoethyl)-10,19-dimethyl-1,28-dioxo-3,10,19,26-tetraazaoctacosane-1,28-diyl)bis(5,11-dihydro-
152429-64-6
11-[2-[6-[methyl-[8-[methyl-[6-[[2-oxo-2-(6-oxo-5h-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]amino]hexyl]amino]octyl]amino]hexyl-[2-oxo-2-(6-oxo-5h-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]amino]acetyl]-5h-pyrido[2,3-b][1,4]benzodiazepin-6-one
gtpl361
PDSP1_000934
tripitramine
PDSP2_000920
L000604
CHEMBL265256
11-[2-[6-[8-[6-[bis[2-oxo-2-(6-oxo-5h-pyrido[2,3-b][1,4]benzodiazepin-11-yl)ethyl]amino]hexyl-methylamino]octyl-methylamino]hexylamino]acetyl]-5h-pyrido[2,3-b][1,4]benzodiazepin-6-one
bdbm82423
cas_132947
nsc_132947
DTXSID30165030
SCHEMBL20584784
Q27089026

Research Excerpts

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

Protein Targets (11)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Muscarinic acetylcholine receptor M2Homo sapiens (human)Ki0.00030.00000.690210.0000AID142646; AID342990
Muscarinic acetylcholine receptor M4Homo sapiens (human)Ki0.00900.00000.79519.1201AID142001; AID342992
Muscarinic acetylcholine receptor M1Rattus norvegicus (Norway rat)Ki0.01680.00010.579710.0000AID104026; AID141857; AID142727
Muscarinic acetylcholine receptor M3Rattus norvegicus (Norway rat)Ki0.14790.00011.48339.1400AID141738
Muscarinic acetylcholine receptor M4Rattus norvegicus (Norway rat)Ki0.01160.00010.68688.2600AID101871; AID142017
Muscarinic acetylcholine receptor M5Homo sapiens (human)Ki0.03390.00000.72926.9183AID142273
Muscarinic acetylcholine receptor M2Rattus norvegicus (Norway rat)Ki0.00030.00010.58908.2600AID140935; AID142876
Muscarinic acetylcholine receptor M1Homo sapiens (human)Ki0.00260.00000.59729.1201AID141302; AID342989
Muscarinic acetylcholine receptor M1Mus musculus (house mouse)Ki0.00160.00160.41173.1623AID141302
5-hydroxytryptamine receptor 1ARattus norvegicus (Norway rat)Ki0.14790.00010.739610.0000AID342991
Muscarinic acetylcholine receptor M3Homo sapiens (human)Ki0.09300.00000.54057.7600AID141590; AID342991
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (39)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (7)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (18)

Processvia Protein(s)Taxonomy
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)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (40)

Assay IDTitleYearJournalArticle
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.
AID141200Antagonist affinity evaluated against Muscarinic acetylcholine receptor M3 in isolated guinea pig longitudinal Ileum.1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
AID140935Inhibition of [3H]NMS binding to rat heart Muscarinic acetylcholine receptor M21998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
AID233262Selectivity 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.
AID142273Affinity for Muscarinic acetylcholine receptor M5 expressed in CHO cells by [3H]NMS displacement.2001Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.
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
AID141590Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.2001Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.
AID101733Antagonistic activity measured in isolated guinea pig left ileum (M3 receptor)1993Journal 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.
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.
AID142124Antagonist affinity evaluated against Muscarinic acetylcholine receptor M2 in isolated guinea pig left atrium1998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
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.
AID233265Selectivity ratio between atrium (M2) and ileum (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.
AID142017Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M41998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
AID141302Affinity for Muscarinic acetylcholine receptor M1 expressed in CHO cells by [3H]NMS displacement.2001Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.
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.
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
AID233270Selectivity 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.
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
AID141738Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M31998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
AID142001Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.2001Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.
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.
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.
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.
AID232491Selectivity ratio is the antilog of the difference between the pA2 values at guinea pig left atrium and ileum muscarinic receptors1994Journal 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
AID101699Antagonistic activity measured in isolated guinea pig left atrium (M2 receptor)1993Journal 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.
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.
AID141857Binding affinity for rat cortex Muscarinic acetylcholine receptor M11998Journal of medicinal chemistry, Oct-08, Volume: 41, Issue:21
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
AID142748Antagonistic activity against M2 muscarinic receptor in guinea pig left atrium derived by plotting log(DR - 1) vs log[antagonist]1994Journal 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
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
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.
AID140997Antagonistic activity against M3 muscarinic receptor in guinea pig left ileum derived by plotting log(DR - 1) vs log[antagonist]1994Journal 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
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.
AID142646Affinity for Muscarinic acetylcholine receptor M2 expressed in CHO cells by [3H]NMS displacement.2001Bioorganic & medicinal chemistry letters, May-07, Volume: 11, Issue:9
Design and pharmacology of quinuclidine derivatives as M2-selective muscarinic receptor ligands.
AID233260Selectivity 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.
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.
AID1345326Human M2 receptor (Acetylcholine receptors (muscarinic))1994European journal of pharmacology, Aug-16, Volume: 268, Issue:3
Binding profile of the selective muscarinic receptor antagonist tripitramine.
AID1345543Human M5 receptor (Acetylcholine receptors (muscarinic))1994European journal of pharmacology, Aug-16, Volume: 268, Issue:3
Binding profile of the selective muscarinic receptor antagonist tripitramine.
AID1345286Human M1 receptor (Acetylcholine receptors (muscarinic))1994European journal of pharmacology, Aug-16, Volume: 268, Issue:3
Binding profile of the selective muscarinic receptor antagonist tripitramine.
AID1345343Human M3 receptor (Acetylcholine receptors (muscarinic))2008Bioorganic & 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.
AID1345465Human M4 receptor (Acetylcholine receptors (muscarinic))2008Bioorganic & 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.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (17)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's14 (82.35)18.2507
2000's3 (17.65)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 27.09

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

MetricThis Compound (vs All)
Research Demand Index27.09 (24.57)
Research Supply Index2.89 (2.92)
Research Growth Index4.19 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (27.09)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other17 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]