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AB120144

4-DAMP, Muscarinic receptor antagonist

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(5 Publications)

MW 451.3 Da, Purity >98%. Muscarinic antagonist. (Ki values for human receptors are 0.57 (M1), 7.3 (M2), 0.37 (M3), 0.72 (M4) and 0.55 nM (M5)).

View Alternative Names

7TM receptor, ACM2_HUMAN, ACM3_HUMAN, ACM4_HUMAN, ACM5_HUMAN, AChR, AChR M5, Acetylcholine receptor muscarinic 5, Acetylcholine receptor, muscarinic, 2, CHKM5MR, CHRM 2, CHRM 3, CHRM1, CM2, Cholinergic receptor muscarinic 1, Cholinergic receptor muscarinic 2, Cholinergic receptor muscarinic 4, Cholinergic receptor muscarinic 5, Cholinergic receptor, muscarinic 2, cardiac, Cholinergic receptor, muscarinic 2, isoform a, Cholinergic receptor, muscarinic 2a, Chrm 4, Chrm 5, EGBRS, FLJ43243, HM 2, HM 3, HM 4, HM 5, HM1, M2 muscarinic receptor, M2-mAChR, M3 muscarinic receptor, M4, M5R, MGC120006, MGC120007, MGC41838, Muscarinic M2 receptor, Muscarinic acetylcholine receptor M1, Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M3, Muscarinic acetylcholine receptor M4, Muscarinic acetylcholine receptor M5, cholinergic receptor muscarinic 3, chrm2a, m3 muscarinic acetylcholine receptor, m5, muscarinic 3, muscarinic cholinergic m3 receptor, muscarinic m3 receptor

2 Images
Chemical Structure - 4-DAMP, Muscarinic receptor antagonist (AB120144)
  • Chemical Structure

Lab

Chemical Structure - 4-DAMP, Muscarinic receptor antagonist (AB120144)

2D chemical structure image of ab120144, 4-DAMP, Muscarinic receptor antagonist

Cellular Activation - 4-DAMP, Muscarinic receptor antagonist (AB120144)
  • CellAct

Unknown

Cellular Activation - 4-DAMP, Muscarinic receptor antagonist (AB120144)

(A) rhAQP5 vector-transfected HSG cells were stimulated with CCh (100 μM) in the presence or absence of 4-DAMP (10 μM), prenzepine (10 μM), and mixture of 4-DAMP and prenzepine (M3R or M1R specific antagonist, respectively).
(B) To monitor hAQP5 trafficking, original GFP pictures in (A) were converted into 'Fire' 3D LUT (lookup tables) setting in ImageJ software and only GFP signal above the fluorescent signal threshold (≥80, red or yellow color in converted picture), was captured in (B) as positive GFP signal. Yellow arrows indicate the positive GFP signal on the membrane and green arrows indicates signal in the cytoplasm in HSG cells.

Image from Lee BH, et al. Plos One, 8(1), e53113. Fig 2,; doi: 10.1371/journal.pone.0053113

Key facts

CAS number

1952-15-4

Purity

>98%

Form

Solid

form

Molecular weight

451.3 Da

Molecular formula

C<sub>2</sub><sub>1</sub>H<sub>2</sub><sub>6</sub>INO<sub>2</sub>

PubChem

3014059

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 25 mM

Biochemical name

4-Damp methiodide

Biological description

Muscarinic antagonist. (Ki values for human receptors are 0.57 (M1), 7.3 (M2), 0.37 (M3), 0.72 (M4) and 0.55 nM (M5)).

Canonical smiles

C[N+]1(CCC(CC1)OC(=O)C(C2=CC=CC=C2)C3=CC=CC=C3)C.[I-]

InChi

InChI=1S/C21H26NO2.HI/c1-22(2)15-13-19(14-16-22)24-21(23)20(17-9-5-3-6-10-17)18-11-7-4-8-12-18;/h3-12,19-20H,13-16H2,1-2H3;1H/q+1;/p-1

InChiKey

WWJHRSCUAQPFQO-UHFFFAOYSA-M

IUPAC Name

(1,1-dimethylpiperidin-1-ium-4-yl) 2,2-diphenylacetate;iodide

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
Ambient
Appropriate long-term storage conditions
Ambient
Storage information
The product can be stored for up to 12 months
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Muscarinic acetylcholine receptors also known as mAChRs are a group of G protein-coupled receptors that bind acetylcholine. They include five distinct subtypes: CHRM1 CHRM2 CHRM3 CHRM4 and CHRM5. These receptors have variable molecular masses ranging from approximately 50 to 60 kDa. Expression of muscarinic receptors is widespread present in both central and peripheral nervous systems and in non-neuronal tissues such as heart and smooth muscle. Each subtype has a unique pattern of distribution affecting how the body reacts to stimuli.
Biological function summary

Muscarinic receptors mediate parasympathetic nervous system responses. They do not function in isolation and may form complexes with other membrane proteins. mAChRs play roles in reducing heart rate constricting bronchi increasing secretions and modulating neurochemical activities in the central nervous system. Arecaidine can act as a muscarinic agonist whereas aclidinium serves as a muscarinic antagonist both influencing receptor activity through different pathways.

Pathways

Muscarinic receptors participate in the PI3K/AKT and MAPK signaling pathways. These pathways are key for cellular responses to environmental changes. For example muscarinic receptors in the cardiac tissue influence heart rate through these pathways interacting with proteins like Gi/o proteins. mAChRs also activate pathways involving other G protein receptors like adrenergic receptors to regulate vascular resistance and secretory processes.

Muscarinic receptors are linked to Alzheimer’s disease and chronic obstructive pulmonary disease (COPD). In Alzheimer’s imbalances in muscarinic receptor signaling can disrupt cognitive function. The CHRM1 subtype is particularly implicated in neurotransmission abnormalities associated with this disease. In COPD the CHRM3 subtype’s regulation of bronchoconstriction becomes clinically relevant. Therapeutic targeting of these receptors using antagonists like aclidinium helps manage symptoms and improve patient outcome.
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Product protocols

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Publications (5)

Recent publications for all applications. Explore the full list and refine your search

Nature biomedical engineering 8:808-822 PubMed37945752

2023

Optogenetic stimulation of vagal nerves for enhanced glucose-stimulated insulin secretion and β cell proliferation.

Applications

Unspecified application

Species

Unspecified reactive species

Yohei Kawana,Junta Imai,Yosuke M Morizawa,Yoko Ikoma,Masato Kohata,Hiroshi Komamura,Toshihiro Sato,Tomohito Izumi,Junpei Yamamoto,Akira Endo,Hiroto Sugawara,Haremaru Kubo,Shinichiro Hosaka,Yuichiro Munakata,Yoichiro Asai,Shinjiro Kodama,Kei Takahashi,Keizo Kaneko,Shojiro Sawada,Tetsuya Yamada,Akira Ito,Kuniyasu Niizuma,Teiji Tominaga,Akihiro Yamanaka,Ko Matsui,Hideki Katagiri

The Journal of neuroscience : the official journal of the Society for Neuroscience 43:722-735 PubMed36535767

2022

Differential Regulation of Prelimbic and Thalamic Transmission to the Basolateral Amygdala by Acetylcholine Receptors.

Applications

Unspecified application

Species

Unspecified reactive species

Sarah C Tryon,Joshua X Bratsch-Prince,James W Warren,Grace C Jones,Alexander J McDonald,David D Mott

Frontiers in pharmacology 10:1386 PubMed31849653

2019

Choline Attenuates Cardiac Fibrosis by Inhibiting p38MAPK Signaling Possibly by Acting on M Muscarinic Acetylcholine Receptor.

Applications

Unspecified application

Species

Unspecified reactive species

Lihui Zhao,Tingting Chen,Pengzhou Hang,Wen Li,Jing Guo,Yang Pan,Jingjing Du,Yuyang Zheng,Zhimin Du

Respiratory physiology & neurobiology 205:7-15 PubMed25262584

2014

Evidence for respiratory neuromodulator interdependence after cholinergic disruption in the ventral respiratory column.

Applications

Unspecified application

Species

Unspecified reactive species

Clarissa Muere,Suzanne Neumueller,Justin Miller,Samantha Olesiak,Matthew R Hodges,Lawrence Pan,Hubert V Forster

PloS one 8:e53113 PubMed23382834

2013

Autoantibodies against muscarinic type 3 receptor in Sjögren's syndrome inhibit aquaporin 5 trafficking.

Applications

Unspecified application

Species

Unspecified reactive species

Byung Ha Lee,Adrienne E Gauna,Geidys Perez,Yun-jong Park,Kaleb M Pauley,Toshihisa Kawai,Seunghee Cha
View all publications
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