Medicinal Chemistry I

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

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

Carvedilol is a non-selective beta-blocker with alpha-1 blocking activity, used primarily to treat high blood pressure (hypertension), heart failure, and left ventricular dysfunction after a heart attack. By blocking beta-adrenergic receptors, it reduces heart rate and contractility, while its alpha-1 blocking effects help relax blood vessels, lowering blood pressure and improving blood flow. Chemical Structure … Read more

Betazolol is a selective beta-1 adrenergic receptor blocker (beta-blocker) used primarily to manage hypertension (high blood pressure) and to treat glaucoma or ocular hypertension when administered as eye drops. Chemical Structure & Formula: Designed for ocular use, it retains the characteristic aryloxypropanolamine structure optimized for topical delivery. Mechanism of Action: Blocks beta receptors in ocular … Read more