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Anthelminthic Agents01:15

Anthelminthic Agents

Anthelmintic drugs differ significantly from antiparasitic therapies targeting protozoa, primarily due to differences in parasite biology. Whereas most protozoal treatments act on proliferating cells, anthelmintics are typically directed against mature, nonproliferative helminths. The therapeutic approach considers the helminth's reliance on neuromuscular coordination, glucose metabolism, and microtubular integrity for survival, reproduction, and localization within the host. Most anthelmintics...
Cholinergic Antagonists: Pharmacokinetics01:24

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Cholinergic antagonists—such as antimuscarinics—are available in oral, topical, ocular, parenteral, and inhalational formulations. Most antimuscarinics are oral formulations,  while scopolamine is available as a topical patch, and ipratropium and tiotropium are available as inhalation aerosols or powders. Atropine, tropicamide, and cyclopentolate are topically instilled in the eye. Most antimuscarinics are lipid-soluble and readily absorbed from the gastrointestinal tract and the conjunctiva.
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Indirect-acting cholinergic agonists are agents that interact with the acetylcholinesterase enzyme in the synaptic cleft, preventing the breakdown of acetylcholine into choline and acetate. Consequently, the concentration of acetylcholine in the synaptic cleft increases. These agonists can be classified into reversible and irreversible inhibitors based on their duration of action.
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Cholinergic antagonists bind to cholinergic receptors and limit the effects of acetylcholine and other cholinergic agonists. Based on the specific cholinergic receptor affinity, these antagonists are classified as muscarinic or nicotinic. Anticholinergics interrupt parasympathetic innervations while sympathetic innervations remain uninterrupted. Muscarinic antagonists are also called 'muscarinic antagonists', 'antimuscarinics', or 'parasympatholytics'. Nicotinic antagonists are called...
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Thermostabilization, Expression, Purification, and Crystallization of the Human Serotonin Transporter Bound to S-citalopram
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Chlorimipraminium picrate.

Jerry P Jasinski, Ray J Butcher, Q N M Hakim Al-Arique

    Acta Crystallographica. Section E, Structure Reports Online
    |May 18, 2011
    PubMed
    Summary
    This summary is machine-generated.

    This study details the crystal structure of chlorimipraminium picrate, revealing specific molecular arrangements and intermolecular interactions. The findings provide insights into the compound's solid-state properties and chemical behavior.

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    Area of Science:

    • Crystallography
    • Chemical Physics
    • Organic Chemistry

    Background:

    • The compound 3-chloro-5-[3-(dimethyl-amino)prop-yl]-10,11-dihydro-5H-dibenz[b,f]azepinium picrate is a salt with potential pharmaceutical relevance.
    • Understanding the crystal structure is crucial for predicting its physical and chemical properties.

    Purpose of the Study:

    • To elucidate the detailed crystal structure of chlorimipraminium picrate.
    • To analyze the molecular conformation of the cation and anion.
    • To investigate intermolecular interactions within the crystal lattice.

    Main Methods:

    • Single-crystal X-ray diffraction was employed to determine the crystal structure.
    • Analysis of bond lengths, bond angles, and torsion angles.
    • Examination of intermolecular interactions such as hydrogen bonding and π-π stacking.

    Main Results:

    • The asymmetric unit contains two independent cation-anion pairs of chlorimipraminium picrate.
    • The chlorimipraminium cation exhibits a V-shaped dibenz[b,f]azepine core with specific dihedral angles between fused rings.
    • The picrate anion shows significant twisting of nitro groups relative to the benzene ring, and phenolate oxygen atoms are slightly out of plane.
    • Crystal packing is characterized by bifurcated N-H⋯(O,O) hydrogen bonds, π-π stacking, and C-H⋯π interactions.

    Conclusions:

    • The crystal structure of chlorimipraminium picrate has been fully characterized.
    • The observed molecular geometry and intermolecular interactions provide a basis for understanding the compound's stability and reactivity.
    • This structural data is valuable for further research in medicinal chemistry and materials science.