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dicycloverine

Names

[ CAS No. ]:
77-19-0

[ Name ]:
dicycloverine

[Synonym ]:
Dicyclohexylhydroxyphenylstannane
[1,1'-bicyclohexyl]-1-carboxylic acid 2-(diethylamino)ethyl ester
Stannane,dicyclohexylhydroxyphenyl
dicycloverine
Dicyclohexylphenyltin hydroxide
Bicyclohexyl-1-carbonsaeure-(2-diaethylamino-aethylester)
bicyclohexyl-1-carboxylic acid-(2-diethylamino-ethyl ester)
Dicyclomine

Biological Activity

[Description]:

Dicyclomine (Dicycloverine) is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine (Dicycloverine) shows high affinity for muscarinic M1 receptor subtype (Ki=5.1 nM) and M2 receptor subtype (Ki=54.6 nM) in brush-border membrane and basal plasma membranes, respectively[1]. Dicyclomine is an antispasmodic agent and relieves smooth muscle spasm of the gastrointestinal tract in vivo[2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR
Signaling Pathways >> GPCR/G Protein >> mAChR

[In Vivo]

Dicyclomine (Dicycloverine) (intraperitoneal injection; 8 mg/kg; daily) exacerbates the cognitive impairments in all the measurements. In addition, the memory impairments are worse in dicyclomine-treated 3xTg-AD mice compared to dicyclomine-treated NonTg mice[2]. Dicyclomine (Dicycloverine) (intraperitoneal injection; 2.0, 4.0, and 8.0 mg/kg; 7 days) produces a highly significant effect on performance in the paired-associates learning (PAL) task in mice.And systemic treatment at lower doses show behavioral impairments in mice in spatial tasks[3]. Animal Model: C57Bl/6 mice[1] Dosage: 2.0, 4.0, and 8.0 mg/kg Administration: Intraperitoneal injection; daily; 7 days Result: Produced impairments due to actions of the agent outside of the hippocampus.

[References]

[1]. Antonella Caccamo, et al.  M1 Receptors Play a Central Role in Modulating AD-like Pathology in Transgenic Mice. 2006 Mar 2;49(5):671-82.doi: 10.1016/j.neuron.2006.01.020.

[2]. Antonella Caccamo, et al.  M1 Receptors Play a Central Role in Modulating AD-like Pathology in Transgenic Mice. 2006 Mar 2;49(5):671-82.doi: 10.1016/j.neuron.2006.01.020.

[3]. Susan J Bartko,et al. A Computer-Automated Touchscreen Paired-Associates Learning (PAL) Task for Mice: Impairments Following Administration of Scopolamine or Dicyclomine and Improvements Following Donepezil.Psychopharmacology (Berl). 2011 Mar;214(2):537-48.

Chemical & Physical Properties

[ Molecular Formula ]:
C19H35NO2

[ Molecular Weight ]:
309.48700

[ Exact Mass ]:
309.26700

[ PSA ]:
29.54000

[ LogP ]:
4.40220

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds