Bioactivity | Dicyclomine hydrochloride is a potent and orally active muscarinic cholinergic receptors antagonist. Dicyclomine hydrochloride 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]. |
Target | Ki: 5.1 nM (muscarinic M1 receptor subtype in brush-border membrane)Ki: 54.6 nM (muscarinic M2 receptor subtype in basal plasma membrane |
In Vivo | Dicyclomine hydrochloride (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 hydrochloride (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: |
Name | Dicyclomine hydrochloride |
CAS | 67-92-5 |
Formula | C19H36ClNO2 |
Molar Mass | 345.95 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
Reference | [1]. J Pavía,et al. Pharmacological Characterization and Distribution of Muscarinic Receptors in Human Placental Syncytiotrophoblast Brush-Border and Basal Plasma Membranes. Eur J Pharmacol. . 1997 Feb 12;320(2-3):209-14. [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):537-4 |