p-F-HHSiD
p-F-HHSiD (p-Fluorohexahydrosiladifenidol) is a selective M3 muscarinic receptor antagonist. p-F-HHSiD has a Ki of 18 nM for the human M1 receptor. p-F-HHSiD weakly and competitively antagonizes Carbamoylcholine chloride (HY-B1208)-induced inhibition of excitatory neurotransmission. p-F-HHSiD blocks M3-mediated slow inward current and smooth muscle contraction tension, thereby enhancing M1-mediated relaxation. p-F-HHSiD can be used in research on neurogenic bladder dysfunction and Alzheimer's disease.
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- CAS No.: 116679-83-5
- Formule: C20H32FNOSi
- Masse moléculaire:349.56
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Other In-stock Forms of p-F-HHSiD
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
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mAChR1 18 nM (Ki) |
mAChR3 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| Astrocyte | EC50 |
5.815 μM
Compound: 8, p-F-HHSiD
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Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
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[PMID: 17417631] |
| Medulloblastoma cell | EC50 |
1.125 μM
Compound: 8, p-F-HHSiD
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Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
Antiproliferative activity against mouse medulloblastoma cells harboring heterozygous ptch1 gene by MTT assay
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[PMID: 17417631] |
In Vitro
p-F-HHSiD inhibits ACh-induced slow inward current in chicken ciliary ganglion neurons with an IC50 of 1.1 × 10-7 M, supporting mediation by M3 muscarinic receptors[2].
p-F-HHSiD (0.3 μM) enhances McN-A-343 (HY-107648)-induced relaxation and inhibits the subsequent increase in smooth muscle tone of isolated rat jejunum longitudinal segments, consistent with M3 receptor antagonism[3].
p-F-HHSiD competes with [3H]QNB for binding to muscarinic receptors in MDCK membranes, with an IC50 of 280 nM and a Ki of 39 nM[4].
p-F-HHSiD binds to NB-OK1 membrane muscarinic receptors with a Ki of 18 nM[6].
p-F-HHSiD competitively antagonizes Carbamoylcholine chloride-induced intracellular calcium release in NB-OK1 cells, with a pA2 of 7.33[6].
p-F-HHSiD competitively antagonizes Carbamoylcholine chloride-induced PI turnover in NB-OK1 cells, with a pA2 of 7.46[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 116679-83-5
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Masse moléculaire 349.56
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Formule C20H32FNOSi
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SMILES
FC1=CC=C([Si](CCCN2CCCCC2)(C3CCCCC3)O)C=C1
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Synonyms
p-Fluorohexahydrosiladifenidol
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Bagetta G, et al. Muscarinic inhibition of excitatory neurotransmission in guinea-pig olfactory cortex slices: weak antagonism by M3-muscarinic receptor antagonists. European journal of pharmacology. 1991 May 30;198(1):69-75. [Content Brief]
[6]. Boddeke HW, et al. M1 muscarinic receptors mediate intracellular calcium release in NB-OK1 human neuroblastoma cells. Naunyn-Schmiedeberg's archives of pharmacology. 1992 Sep;346(3):255-61. [Content Brief]
[7]. Pontari MA, et al. The M2 muscarinic receptor mediates in vitro bladder contractions from patients with neurogenic bladder dysfunction. Am J Physiol Regul Integr Comp Physiol. 2004 May;286(5):R874-80. [Content Brief]
[8]. Svensson AL, et al. Characterization of muscarinic receptor subtypes in Alzheimer and control brain cortices by selective muscarinic antagonists. Brain research. 1992 Nov 20;596(1-2):142-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
p-F-HHSiD Related Classifications
HY-137388 Related Classifications
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Keywords
- p-F-HHSiD
- 116679-83-5
- p-Fluorohexahydrosiladifenidol
- mAChR
- Muscarinic acetylcholine receptor
- Alzheimer's disease
- M1 muscarinic receptor
- M3 muscarinic receptor
- carbachol
- excitatory neurotransmission
- muscarinic receptor
- neurogenic bladder dysfunction
- phosphoinositide hydrolysis
- slow inward current
- smooth muscle contraction
- Inhibitor
- inhibitor
- inhibit