Medicinal Chemistry I

Thioridazine Hydrochloride is a typical antipsychotic, blocking dopamine receptors to reduce psychotic activity in the brain. It treats schizophrenia and psychotic disorders by managing symptoms like agitation and hallucinations. Chemical Formula: C₂₁H₂₇ClN₂S₂·HCl Mechanism of Action: D2 receptor antagonist Also blocks muscarinic, alpha, and H1 receptors Uses of Thioridazine Hydrochloride: Schizophrenia (especially in treatment-resistant or sensitive … Read more

Morphine Sulphate acts on μ-opioid receptors, altering pain perception and producing sedation. It is a potent opioid analgesic for severe acute and chronic pain relief. Chemical Formula: (C₁₇H₁₉NO₃)₂·H₂SO₄ Mechanism of Action: Full agonist at μ-opioid receptors Causes inhibition of adenylate cyclase, ↓ cAMP, ↑ K⁺ efflux, ↓ Ca²⁺ influx → neuronal hyperpolarization → inhibition of … Read more

SAR of Morphine Analogues highlights opioid receptor binding, guiding design of safer pain relievers. SAR of Morphine Analogues shows how structural changes modify analgesic potency and side effects. Morphine has a rigid, pentacyclic ring system with functional groups critical to opioid activity. Key Features of SAR of Morphine Analogues: Phenolic OH at C-3: Essential for … Read more

Narcotic and Non-Narcotic Analgesics relieve pain, ranging from mild headaches to severe postoperative pain. It acts via opioid receptors or peripheral pathways to reduce pain perception. Narcotic (Opioid) Analgesics These drugs act on the opioid receptors (μ, κ, δ) in the central nervous system (CNS). Mechanism: Agonist activity at μ-opioid receptors leads to: Inhibition of … Read more

Ketamine Hydrochloride blocks NMDA receptors, producing dissociative anesthesia with analgesia. It is used for anesthesia, pain relief, and emergency sedation. Chemical Formula: C₁₃H₁₆ClNO·HCl Mechanism of Action: NMDA receptor antagonist Also interacts with opioid, monoaminergic, and muscarinic receptors Increases sympathetic output → ↑ BP, HR, CO Uses of Ketamine Hydrochloride: Induction of anesthesia Short surgical procedures … Read more

Thiopental Sodium is a barbiturate that enhances GABA action, causing rapid CNS depression. It is used for induction of anesthesia and short-term surgical procedures. Chemical Formula: C₁₁H₁₇N₂NaO₂S Mechanism of Action: Enhances GABA-A receptor function Depresses reticular activating system Uses of Thiopental Sodium: Induction of anesthesia Control of seizures Medically induced coma (neuroprotection) Side Effects of … Read more

Thiamylal Sodium enhances GABA action in the CNS, producing rapid sedative and hypnotic effects. It is a barbiturate used for induction of anesthesia and short surgical procedures. Chemical Formula: C₁₁H₁₇N₂NaO₂S Mechanism of Thiamylal Sodium: Potentiates GABA-A receptor Highly lipophilic → rapid onset of CNS depression Uses of Thiamylal Sodium: Anesthesia induction Brief surgical anesthesia Side … Read more

Desflurane enhances GABA effects in the CNS, offering fast onset, easy control, and quick recovery. It is an inhalation anesthetic used for rapid induction and maintenance of general anesthesia. Chemical Formula: C₃H₂F₆O Mechanism of Desflurane: Similar to isoflurane Rapid onset/recovery due to low blood solubility Uses of Desflurane: Outpatient surgery (day-case anesthesia) Maintenance (not ideal … Read more

Methohexital Sodium, a barbiturate, enhances GABA action causing rapid sedation with short duration. It is used for anesthesia induction and short surgical or diagnostic procedures. Chemical Formula: C₁₄H₁₇N₂NaO₃ Mechanism of Action: Potentiates GABA-A receptors Increases Cl⁻ influx → CNS depression Rapid onset due to high lipid solubility Uses of Methohexital Sodium: Induction of anesthesia Brief … Read more

Sevoflurane acts on CNS by enhancing GABA activity, providing smooth onset and quick recovery. It is an inhalation anesthetic used for rapid induction and maintenance of general anesthesia. Chemical Formula: C₄H₃F₇O Mechanism of Sevoflurane: Potentiates GABA-A and glycine receptors Fast onset due to low blood/gas solubility Uses of Sevoflurane: Induction in children (non-pungent) Maintenance Side … Read more