Compounds > ml 10375

Page last updated: 2024-11-12

ml 10375

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

Cross-References

ID Source	ID
PubMed CID	9905972
CHEMBL ID	155917
SCHEMBL ID	2943813
MeSH ID	M0302339

Synonyms (11)

Synonym
ml-10375
2-(3,5-dimethylpiperidin-1-yl)ethyl 4-amino-5-chloro-2-methoxybenzoate
gtpl249
ml 10375
L014506
CHEMBL155917 ,
4-amino-5-chloro-2-methoxy-benzoic acid 2-(3,5-dimethyl-piperidin-1-yl)-ethyl ester
bdbm50056392
ml10375
SCHEMBL2943813
Q27086949

Research Excerpts

Dosage Studied

Excerpt	Relevance	Reference
"3 or 1 mg kg(-1)) inhibited contractions of the stomach fundus in anaesthetized rats in response to intravenous dosing of alpha-methyl 5-HT (0."	( The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Armstrong, SR; Beattie, DT; Humphrey, PP; Mai, N; Marquess, D; McCullough, JL; Pulido-Rios, T; Richardson, C; Sandlund, C; Smith, JA; Vickery, RG, 2004)	0.32

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

Protein Targets (2)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
5-hydroxytryptamine receptor 3A	Rattus norvegicus (Norway rat)	Ki	1.0000	0.0002	0.4841	10.0000	AID5880
5-hydroxytryptamine receptor 3B	Rattus norvegicus (Norway rat)	Ki	1.0000	0.0002	0.5023	10.0000	AID5880
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (14)

Assay ID	Title	Year	Journal	Article
AID624238	Antagonists at Human 5-Hydroxytryptamine receptor 5-HT4	1998	Journal of neurochemistry, Jun, Volume: 70, Issue:6	Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
AID624238	Antagonists at Human 5-Hydroxytryptamine receptor 5-HT4	2000	British journal of pharmacology, Oct, Volume: 131, Issue:4	Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
AID1346953	Human 5-HT4 receptor (5-Hydroxytryptamine receptors)	2000	British journal of pharmacology, Feb, Volume: 129, Issue:4	Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
AID624238	Antagonists at Human 5-Hydroxytryptamine receptor 5-HT4	2000	British journal of pharmacology, Jun, Volume: 130, Issue:3	Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling.
AID1346953	Human 5-HT4 receptor (5-Hydroxytryptamine receptors)	2000	British journal of pharmacology, Oct, Volume: 131, Issue:4	Pharmacological characterization of the human 5-HT(4(d)) receptor splice variant stably expressed in Chinese hamster ovary cells.
AID1346953	Human 5-HT4 receptor (5-Hydroxytryptamine receptors)	2000	British journal of pharmacology, Jun, Volume: 130, Issue:3	Exploration of the ligand binding site of the human 5-HT(4) receptor by site-directed mutagenesis and molecular modeling.
AID624238	Antagonists at Human 5-Hydroxytryptamine receptor 5-HT4	2004	British journal of pharmacology, Nov, Volume: 143, Issue:5	The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo.
AID1346953	Human 5-HT4 receptor (5-Hydroxytryptamine receptors)	1998	Journal of neurochemistry, Jun, Volume: 70, Issue:6	Cloning, expression, and pharmacology of four human 5-hydroxytryptamine 4 receptor isoforms produced by alternative splicing in the carboxyl terminus.
AID1346953	Human 5-HT4 receptor (5-Hydroxytryptamine receptors)	2004	British journal of pharmacology, Nov, Volume: 143, Issue:5	The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo.
AID624238	Antagonists at Human 5-Hydroxytryptamine receptor 5-HT4	2000	British journal of pharmacology, Feb, Volume: 129, Issue:4	Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines.
AID6239	Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
AID5880	Binding affinity was measured on 5-hydroxytryptamine 3 receptor using [3H]-BRL 43694 as radioligand in rat posterior cortex.	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
AID6143	5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum; Inactive up to 10E-5 M	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
AID6152	5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum	1997	Journal of medicinal chemistry, Feb-14, Volume: 40, Issue:4	New esters of 4-amino-5-chloro-2-methoxybenzoic acid as potent agonists and antagonists for 5-HT4 receptors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	2 (33.33)	18.2507
2000's	4 (66.67)	29.6817
2010's	0 (0.00)	24.3611
2020's	0 (0.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.24

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

Metric	This Compound (vs All)
Research Demand Index	12.24 (24.57)
Research Supply Index	1.95 (2.92)
Research Growth Index	4.18 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (12.24)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	6 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Trials	Classes	Roles
5-methoxytryptamine 5-Methoxytryptamine: Serotonin derivative proposed as potentiator for hypnotics and sedatives.. 5-methoxytryptamine : A member of the class of tryptamines that is the methyl ether derivative of serotonin.	2.69	3	0	aromatic ether; primary amino compound; tryptamines	5-hydroxytryptamine 2A receptor agonist; 5-hydroxytryptamine 2B receptor agonist; 5-hydroxytryptamine 2C receptor agonist; antioxidant; cardioprotective agent; human metabolite; mouse metabolite; neuroprotective agent; radiation protective agent; serotonergic agonist
alpha-methylserotonin alpha-methylserotonin: potent agonist at M & D receptors of serotonin; RN given refers to parent cpd	2.02	1	0	tryptamines	serotonergic agonist
cisapride Cisapride: A substituted benzamide used for its prokinetic properties. It is used in the management of gastroesophageal reflux disease, functional dyspepsia, and other disorders associated with impaired gastrointestinal motility. (Martindale The Extra Pharmacopoeia, 31st ed). cisapride : The amide resulting from formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with cis-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-amine. It has been used (as its monohydrate or as its tartrate) for the treatment of gastro-oesophageal reflux disease and for non-ulcer dyspepsia, but its propensity to cause cardiac arrhythmias resulted in its complete withdrawal from many countries, including the U.K., and restrictions on its use elsewhere.	2.41	2	0	benzamides
metoclopramide Metoclopramide: A dopamine D2 antagonist that is used as an antiemetic.. metoclopramide : A member of the class of benzamides resulting from the formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with the primary amino group of N,N-diethylethane-1,2-diamine.	1.99	1	0	benzamides; monochlorobenzenes; substituted aniline; tertiary amino compound	antiemetic; dopaminergic antagonist; environmental contaminant; gastrointestinal drug; xenobiotic
sb 206553 SB 206553: a high-affinity 5-HT(2C/2B) antagonist; structure given in first source	2.02	1	0	pyrroloindole
sdz 205-557 [no description available]	1.99	1	0	methoxybenzoic acid
zacopride [no description available]	1.99	1	0	benzamides
gr 113808 GR 113808: structure given in first source; a 5-HT(4) receptor antagonist: GR 125487 is the HCl salt. GR 113808 : An indolyl carboxylate ester obtained by formal condensation between the carboxy group of 1-methylindole-3-carboxylic acid with the hydroxy group of N-{2-[4-(hydroxymethyl)piperidin-1-yl]ethyl}methanesulfonamide.	2.69	3	0	indolyl carboxylate ester; piperidines; sulfonamide	serotonergic antagonist
sb 204070a [no description available]	2.41	2	0
piboserod Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.	2.02	1	0
rs 23597-190 [no description available]	2.69	3	0	methoxybenzoic acid
rs 67333 RS 67333: 5-HT(4) receptor agonist; structure in first source	2.41	2	0	aromatic ketone
brl 24924 [no description available]	2.69	3	0
bw 723c86 [no description available]	2.02	1	0	tryptamines
ml 10302 2-piperidinoethyl 4-amino-5-chloro-2-methoxybenzoate: structure in first source	3.1	5	0
brl 24682 BRL 24682: RN given for (endo)-isomer; structure in first source	1.99	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Glial Cell Tumors [description not available]	0	2	1	0
Glioma Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)	0	2	1	0
Muscle Contraction A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.	0	2.02	1	0