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Related Concept Videos

Nociception01:44

Nociception

Nociception—the ability to feel pain—is essential for an organism’s survival and overall well-being. Noxious stimuli such as piercing pain from a sharp object, heat from an open flame, or contact with corrosive chemicals are first detected by sensory receptors, called nociceptors, located on nerve endings. Nociceptors express ion channels that convert noxious stimuli into electrical signals. When these signals reach the brain via sensory neurons, they are perceived as pain. Thus, pain helps the...
Analgesia and Pain Management01:25

Analgesia and Pain Management

Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates these...
Local Anesthetics: Common Agents and Their Applications01:23

Local Anesthetics: Common Agents and Their Applications

Local anesthetics (LAs) are commonly used for various applications in medical and dental procedures. Some of the common agents used are cocaine, lidocaine, and bupivacaine.
Cocaine is an ester of benzoic acid and methylecgogine. It is used to anesthetize and vasoconstrict locally. Currently, it is used primarily for topical applications. It is beneficial for surgeries on the upper respiratory tract, providing anesthesia and shrinking the mucosa. Cocaine in the form of cocaine hydrochloride is...
Local Anesthetics: Differential Sensitivity of Nerve Fibers01:24

Local Anesthetics: Differential Sensitivity of Nerve Fibers

Local anesthetics (LAs) block the sodium channels of nerve trunks, sensory nerve endings, and neuromuscular junctions. Although LAs can block all kinds of nerves, the sensitivity of nerve fibers differs according to nerve types and structures. LAs are known to block myelinated fibers faster than unmyelinated ones. Also, they block pain or sensory neurons at low concentrations without affecting the motor neurons involved in muscle contractions. This helps relieve labor pain without affecting the...
Local Anesthetics: Adverse Effects01:12

Local Anesthetics: Adverse Effects

While local anesthetics are generally safe and well-tolerated, they can occasionally cause adverse effects that vary in severity. Local anesthetics can induce toxicity at two distinct levels. They can either produce local effects through direct contact with the neural elements or be absorbed into the bloodstream from the injection site, leading to systemic effects.
Once absorbed into the systemic circulation, local anesthetics can affect the organs that depend on the functioning of sodium...

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Related Experiment Video

Updated: Jun 12, 2026

Establishing a Mouse Model of a Pure Small Fiber Neuropathy with the Ultrapotent Agonist of Transient Receptor Potential Vanilloid Type 1
09:39

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Systemically and topically active antinociceptive neurotensin compounds.

Grace C Rossi1, Joshua E Matulonis, Elliott Richelson

  • 1Department of Psychology, C.W. Post Campus of Long Island University, Brookville, New York, USA.

The Journal of Pharmacology and Experimental Therapeutics
|June 26, 2010
PubMed
Summary

New neurotensin analogs show significant pain relief (antinociception) in mice. These stable compounds are potent analgesics, acting systemically or topically, offering potential for novel pain management therapies.

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Published on: October 6, 2022

Area of Science:

  • Neuroscience
  • Pharmacology
  • Analgesic Research

Background:

  • Neurotensin is a neurotransmitter/modulator with diverse physiological actions.
  • Investigating neurotensin's role in pain modulation is crucial for developing new pain therapies.

Purpose of the Study:

  • To synthesize and evaluate stable neurotensin analogs for antinociceptive effects in mice.
  • To assess the systemic and topical activity, potency, and duration of action of these novel compounds.

Main Methods:

  • Synthesis of 10 stable neurotensin analogs incorporating l-neoTrp.
  • Evaluation of antinociception using the radiant heat tail-flick assay in mice.
  • Analysis of time-action and dose-response curves to determine efficacy and potency (ED50).

Main Results:

  • All synthesized analogs demonstrated antinociceptive properties in vivo.
  • Peak effect was observed at 30 minutes, with a duration of 2-4 hours.
  • Compounds showed high potency (ED50 values comparable to opioids) and two analogs were effective topically.

Conclusions:

  • Neurotensin analogs exhibit significant analgesic potential.
  • Systemic and topical administration routes are effective, suggesting a potential to mitigate side effects like hypothermia and hypotension.