Compounds > br 100

Page last updated: 2024-12-08

br 100

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

Description

BR 100: consists of UTMA-based resin-impregnated glass fibers [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	199230
CHEMBL ID	41779
SCHEMBL ID	11725908
MeSH ID	M0491722

Synonyms (15)

Synonym
br 100
br 100 (pharmaceutical)
1-(4-dimethylaminobut-2-ynyl)pyrrolid-2-one
brn 1527767
2-pyrrolidinone, 1-(4-(dimethylamino)-2-butynyl)-
CHEMBL41779 ,
bdbm50005856
1-(4-dimethylamino-but-2-ynyl)-pyrrolidin-2-one
1-[4-(dimethylamino)but-2-ynyl]pyrrolidin-2-one
AKOS006279847
3854-02-2
SCHEMBL11725908
DTXSID20191868
1-[4-(dimethylamino)but-2-yn-1-yl]pyrrolidin-2-one
1-(4-(dimethylamino)but-2-yn-1-yl)pyrrolidin-2-one

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

Protein Targets (6)

Inhibition Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
Muscarinic acetylcholine receptor M1	Rattus norvegicus (Norway rat)	Ki	4.2204	0.0001	0.5797	10.0000	AID141721; AID142223; AID142224
Muscarinic acetylcholine receptor M3	Rattus norvegicus (Norway rat)	Ki	1.3604	0.0001	1.4833	9.1400	AID101702; AID142223; AID142224
Muscarinic acetylcholine receptor M4	Rattus norvegicus (Norway rat)	Ki	1.3005	0.0001	0.6868	8.2600	AID142223; AID142224
Muscarinic acetylcholine receptor M5	Rattus norvegicus (Norway rat)	Ki	1.3005	0.0001	0.6661	8.2600	AID142223; AID142224
Muscarinic acetylcholine receptor M2	Rattus norvegicus (Norway rat)	Ki	1.1454	0.0001	0.5890	8.2600	AID101702; AID101704; AID142223; AID142224
Muscarinic acetylcholine receptor	Cavia porcellus (domestic guinea pig)	Ki	1.6000	0.0001	0.6120	3.8019	AID101702
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (17)

Assay ID	Title	Year	Journal	Article
AID141859	Intrinsic activity against M1 receptor in rat cortex as percent response relative to carbachol	1992	Journal of medicinal chemistry, May-01, Volume: 35, Issue:9	Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.
AID101700	Binding affinity at [3H]CD radiolabeled muscarinic M2 receptor in rat cortex.	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
AID231701	Relative [3H]QNB and [3H]-CD binding to muscarinic M2 receptor	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
AID101702	Binding affinity at [3H]QNB and GppNHp radiolabeled muscarinic M2 receptor in rat heart.	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
AID230678	Ratio of [3H]QNB+GppNHp/[3H]-QNB	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
AID79212	Relative efficacy calculated from KA and ED50 values	1985	Journal of medicinal chemistry, Dec, Volume: 28, Issue:12	Stereoselectivity of muscarinic receptors in vivo and in vitro for oxotremorine analogues. N-[4-(tertiary amino)-2-butynyl]-5-methyl-2-pyrrolidones.
AID141136	Tested for agonist activity at Muscarinic acetylcholine receptor in guinea pig ileum	1985	Journal of medicinal chemistry, Dec, Volume: 28, Issue:12	Stereoselectivity of muscarinic receptors in vivo and in vitro for oxotremorine analogues. N-[4-(tertiary amino)-2-butynyl]-5-methyl-2-pyrrolidones.
AID142948	Compound was evaluated for its binding affinity towards Muscarinic acetylcholine receptor M2 in rat brainstem	1992	Journal of medicinal chemistry, May-01, Volume: 35, Issue:9	Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.
AID101703	Binding affinity at [3H]QNB radiolabeled muscarinic M2 receptor in rat cortex.	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
AID228329	Ratio of Ki value for QNB to that of Ki value for Oxo-M.	1991	Journal of medicinal chemistry, Aug, Volume: 34, Issue:8	Cholinergic activity of acetylenic imidazoles and related compounds.
AID140938	Intrinsic activity against Muscarinic acetylcholine receptor M2 in rat striatum (activity expressed as % response of that produced by carbachol)	1992	Journal of medicinal chemistry, May-01, Volume: 35, Issue:9	Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.
AID104025	Binding affinity at [3H]PZ radiolabeled muscarinic M1 receptor in rat cortex.	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
AID142224	Binding affinity to muscarinic acetylcholine receptor was determined in presence of [3H]QNB radioligand (in vitro)	1991	Journal of medicinal chemistry, Aug, Volume: 34, Issue:8	Cholinergic activity of acetylenic imidazoles and related compounds.
AID141721	Compound was evaluated for its binding affinity towards Muscarinic acetylcholine receptor M1 in rat cortex	1992	Journal of medicinal chemistry, May-01, Volume: 35, Issue:9	Synthesis and in vitro characterization of novel amino terminally modified oxotremorine derivatives for brain muscarinic receptors.
AID101704	Binding affinity at [3H]QNB radiolabeled muscarinic M2 receptor in rat heart.	1993	Journal of medicinal chemistry, Nov-12, Volume: 36, Issue:23	The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
AID142223	Binding affinity to muscarinic acetylcholine receptor was determined in presence of [3H]OXO-M radioligand (in vitro)	1991	Journal of medicinal chemistry, Aug, Volume: 34, Issue:8	Cholinergic activity of acetylenic imidazoles and related compounds.
AID79209	Percent occupancy for 50% response calculated from (100 x ED50)/(KA+ED50).	1985	Journal of medicinal chemistry, Dec, Volume: 28, Issue:12	Stereoselectivity of muscarinic receptors in vivo and in vitro for oxotremorine analogues. N-[4-(tertiary amino)-2-butynyl]-5-methyl-2-pyrrolidones.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (7)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	1 (14.29)	18.7374
1990's	3 (42.86)	18.2507
2000's	1 (14.29)	29.6817
2010's	2 (28.57)	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: 43.55

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

Metric	This Compound (vs All)
Research Demand Index	43.55 (24.57)
Research Supply Index	2.20 (2.92)
Research Growth Index	4.90 (4.65)
Search Engine Demand Index	105.11 (26.88)
Search Engine Supply Index	3.51 (0.95)

This Compound (43.55)

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	8 (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
oxotremorine Oxotremorine: A non-hydrolyzed muscarinic agonist used as a research tool.	2.89	4	0	N-alkylpyrrolidine
carbachol Carbachol: A slowly hydrolyzed CHOLINERGIC AGONIST that acts at both MUSCARINIC RECEPTORS and NICOTINIC RECEPTORS.	1.98	1	0	ammonium salt; carbamate ester	cardiotonic drug; miotic; muscarinic agonist; nicotinic acetylcholine receptor agonist; non-narcotic analgesic
n-methyl-n-(1-methyl-4-pyrrolidino-2-butynyl)acetamide N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide: RN given refers to parent cpd without isomeric designation	2.38	2	0	N-alkylpyrrolidine
atropine tropan-3alpha-yl 3-hydroxy-2-phenylpropanoate : A tropane alkaloid that is (1R,5)-8-methyl-8-azabicyclo[3.2.1]octane substituted by a (3-hydroxy-2-phenylpropanoyl)oxy group at position 3.	1.96	1	0
aluminum oxide Aluminum Oxide: An oxide of aluminum, occurring in nature as various minerals such as bauxite, corundum, etc. It is used as an adsorbent, desiccating agent, and catalyst, and in the manufacture of dental cements and refractories.	2.02	1	0
urethane tetramethacrylate urethane tetramethacrylate: structure in first source	2.02	1	0

Condition	Indicated	Relationship Strength	Studies	Trials
Action Tremor [description not available]	0	2.37	2	0
Tremor Cyclical movement of a body part that can represent either a physiologic process or a manifestation of disease. Intention or action tremor, a common manifestation of CEREBELLAR DISEASES, is aggravated by movement. In contrast, resting tremor is maximal when there is no attempt at voluntary movement, and occurs as a relatively frequent manifestation of PARKINSON DISEASE.	0	2.37	2	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	1.96	1	0