SAR of Barbiturates

SAR of Barbiturates

SAR of Barbiturates shows activity depends on substitutions at C5 and heteroatom modifications. SAR of Barbiturates reveals lipophilicity increases potency, while side chains alter duration. Barbiturates act by enhancing GABA-A activity and directly activating the GABA-A receptor at higher doses. Core Structure: Barbituric acid nucleus (pyrimidine ring with keto groups at C-2 and C-4, C-6). … Read more

Sympathomimetic Drugs

Sympathomimetic Drugs

Sympathomimetic drugs stimulate adrenergic receptors, increasing heart rate, blood pressure, and bronchodilation. (Also called Adrenergic Agonists) Definition of Sympathomimetic Drugs: These drugs mimic the effects of the sympathetic nervous system by activating adrenergic receptors (alpha and beta receptors). Classification with MOA: Direct-acting: Act directly on adrenergic receptors (e.g., epinephrine, dobutamine) Indirect-acting: Increase release or prevent … Read more

Parasympatholytic Drugs

Parasympatholytic Drugs

Parasympatholytic Drugs block acetylcholine action in the parasympathetic system, reducing secretions, relaxing smooth muscles, and increasing heart rate (Also called Anticholinergics or Cholinergic Antagonists) Definition of Parasympatholytic Drugs: These drugs block the effects of the parasympathetic nervous system by inhibiting acetylcholine at muscarinic receptors. Examples of Parasympatholytic Drugs: Atropine – prototype drug Scopolamine – used … Read more

SAR of Benzodiazepines (BZDs)

SAR of Benzodiazepines (BZDs)

SAR of Benzodiazepines (BZDs) highlights the importance of the 1,4-benzodiazepine nucleus for activity. SAR of Benzodiazepines (BZDs) shows how ring substitutions modify potency, duration, and receptor affinity. Benzodiazepines act primarily at the GABA-A receptor to enhance inhibitory neurotransmission. Key SAR of Benzodiazepines (BZDs) Points: Aromatic Ring at Position 5 (C-5): A phenyl group at C-5 … Read more

Benztropine Mesylate

Benztropine Mesylate

Benztropine Mesylate treats Parkinson’s disease and drug-induced extrapyramidal symptoms. Benztropine Mesylate works as an anticholinergic, balancing dopamine and acetylcholine activity. Chemical Formula: C₂₁H₂₅NO·CH₄O₃S Mechanism of Action: Centrally acting M1 antagonist Also has weak dopamine reuptake inhibition (antiparkinsonian effect) Therapeutic Uses of Benztropine Mesylate: Parkinson’s disease (adjunct) Drug-induced extrapyramidal symptoms (EPS) Side Effects of Benztropine Mesylate: … Read more

Propantheline Bromide

Propantheline Bromide treats peptic ulcers and IBS by reducing gastric secretions and spasms. Propantheline Bromide is an anticholinergic blocking muscarinic receptors for smooth muscle relaxation. Chemical Formula: C₂₃H₃₀BrNO₃ Mechanism of Action: Non-selective muscarinic blocker Reduces GI and urinary tract motility Therapeutic Uses of Propantheline Bromide: Bladder spasms GI ulcers and hypermotility Side Effects of Propantheline … Read more

Co-transmission

Co-transmission

Co-transmission occurs when neurons release multiple neurotransmitters to regulate complex physiological responses. Definition of Co-transmission: It is the simultaneous release of more than one neurotransmitter from a single neuron, usually from the same synaptic vesicle or nearby vesicles. Key Features: Neurotransmitters can be classical (e.g., acetylcholine) and peptides (e.g., substance P) or amines (e.g., dopamine). … Read more

Parasympathomimetic Drugs (Cholinergic Agonists)

Parasympathomimetic Drugs (Cholinergic Agonists)

Parasympathomimetic Drugs (Cholinergic Agonists) are agents that mimic acetylcholine, stimulating parasympathetic activity to control functions like smooth muscle contraction, gland secretion, and reduced heart rate. Definition of Parasympathomimetic Drugs: Parasympathomimetics are drugs that mimic the action of the parasympathetic nervous system. They enhance the effects of acetylcholine (ACh) at muscarinic or nicotinic Classification with MOA: … Read more

Classification of Neurotransmitters

Classification of Neurotransmitters

Neurotransmitters are classified as excitatory, inhibitory, or modulatory, based on their role in nerve signaling. Excitatory Neurotransmitters These promote depolarization of the postsynaptic membrane, increasing the likelihood of an action potential. Glutamate: Main excitatory neurotransmitter in the CNS Aspartate: Excitatory amino acid in the CNS Acetylcholine: Excitatory at the neuromuscular junction (nicotinic receptors) Norepinephrine (Noradrenaline): … Read more

Neurohumoral Transmission

Neurohumoral Transmission

Neurohumoral transmission is the process where nerve impulses release chemical messengers to transmit signals. Definition: Neurohumoral transmission refers to the process by which a nerve impulse leads to the release of a chemical substance (neurotransmitter), which then acts on a target cell (neuron, muscle, or gland) to produce a specific physiological response. Steps of Neurohumoral … Read more

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