Medicinal Chemistry I is a core subject that explores the design, synthesis, and biological activity of drugs. It bridges organic chemistry and pharmacology to enhance understanding of therapeutic agents.
Acetylcholine (ACh) is a neurotransmitter a chemical messenger that plays a key role in both the central nervous system (CNS) and peripheral nervous system (PNS). It is involved in transmitting nerve impulses across synapses, particularly at neuromuscular junctions, autonomic ganglia, and within the brain. Chemical Formula: C₇H₁₆NO₂⁺ Mechanism of Action: Mimics acetylcholine at muscarinic and … Read more
Parasympathomimetic agents, also known as cholinergic agonists, are drugs that mimic the action of the parasympathetic nervous system (PNS) by stimulating cholinergic receptors (muscarinic and/or nicotinic). A. Direct-Acting Parasympathomimetic Agents These agents bind directly to cholinergic receptors, mimicking the effect of acetylcholine. Mechanism Act as agonists at muscarinic (and in some cases nicotinic) Not dependent … Read more
Parasympathomimetic agents are drugs that mimic the actions of acetylcholine (ACh) on parasympathetic nervous system These agents stimulate cholinergic receptors, resulting in increased secretions, smooth muscle contraction, slowed heart rate, and other parasympathetic effects. They are classified into two main groups: Direct-acting cholinergic agonists Indirect-acting cholinesterase inhibitors A third category includes cholinesterase reactivators, used to … Read more
Cholinergic receptors are specialized protein receptors located on the surface of cells that bind acetylcholine (ACh), a key neurotransmitter in the autonomic and somatic nervous systems. Acetylcholine acts on two types of receptors: Nicotinic receptors (ionotropic) Muscarinic receptors (metabotropic) Muscarinic Cholinergic receptors Type G-protein-coupled receptors (GPCRs) Subtypes and Signal Pathways Subtype G-protein Pathway Effect M1 … Read more
Acetylcholine (ACh) is a neurotransmitter a chemical messenger that plays a crucial role in transmitting signals in both the central and peripheral nervous systems. Biosynthesis of acetylcholine Location Synthesized in the cytoplasm of cholinergic neurons, particularly at nerve terminals. Precursors Choline: Obtained from diet and recycled ACh. Acetyl-CoA: Formed in mitochondria from pyruvate (product of … Read more
Metoprolol is a selective beta-1 adrenergic receptor blocker (β1-blocker) used primarily to manage cardiovascular conditions. It reduces the effects of adrenaline on the heart, leading to decreased heart rate, cardiac output, and blood pressure. Chemical Structure & Formula: Comprises an aromatic ring joined to an oxypropanolamine chain and is typically used as a racemic mixture … Read more
Cholinergic neurotransmitters refer specifically to acetylcholine (ACh), a key chemical messenger used by certain neurons to communicate with each other or with muscle cells. These neurons are called cholinergic neurons because they release acetylcholine as their primary neurotransmitter. Function and Importance of Cholinergic Neurotransmitters Acetylcholine is involved in various physiological functions depending on where in … Read more
Labetalol is a dual-action adrenergic antagonist used primarily as an antihypertensive agent. It blocks both α1-adrenergic receptors and β-adrenergic receptors (non-selective β-blocker with selective α1-blocking activity). Chemical Structure & Formula: Unique among beta blockers, it contains dual-acting structural features (aromatic rings and a secondary amine) that allow it to block both beta and α₁ receptors. … Read more
Esmolol is a short-acting, selective beta-1 adrenergic receptor blocker (beta-blocker) primarily used to manage rapid heart rates and hypertension, especially in acute care settings. Its rapid onset and very short half-life, esmolol is typically administered intravenously and allows for precise control of heart rate in situations like supraventricular tachycardia, atrial fibrillation. Chemical Structure & Formula: … Read more
Bisoprolol is a prescription medication that belongs to a class of drugs called beta-blockers (specifically, β₁-selective adrenergic receptor blockers). Chemical Structure & Formula: A selective β₁ blocker with an oxypropanolamine motif and additional lipophilic groups that enhance selectivity. Approximate Formula: C₁₈H₃₁NO₄ Mechanism of Action: Selectively antagonizes β₁ receptors in cardiac tissue, reducing heart rate and … Read more
