analgesia

Parecoxib (SC 69124) is an effective and selective COX-2 inhibitor.

Dexmedetomidine is a Central alpha-2 Adrenergic Agonist. The mechanism of action of dexmedetomidine is as an Adrenergic alpha2-Agonist. The physiologic effect of dexmedetomidine is by means of General Anesthesia.

Dexmedetomidine hydrochloride (Precedex) is a potent, selective, orally active α2-adrenoceptor agonist with a Ki value of 1.08 nM. It shows 1620-fold selectivity over α1-adrenoceptors. Dexmedetomidine hydrochloride (Precedex) can protect against sepsis-induced acute lung injury through anti-inflammatory, anti-oxidative, and anti-apoptotic effects.

Medetomidine hydrochloride (MPV785) is a selective α2-adrenoceptor agonist, with Ki of 1.08 nM, exhibts 1620-fold selectivity over α1-adrenoceptor.

Methylnaltrexone bromide (MOA-728) is one of the newer agents of peripherally-acting μ-opioid antagonists. Methylnaltrexone bromide acts to reverse some of the side effects of opioid drugs such as constipation without affecting analgesia or precipitating withdrawals.

JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.

Dibutyryl-cGMP sodium (Bt2cGMP sodium) is a cell-permeable cGMP analog that preferentially activates cGMP-dependent protein kinase (PKG). It inhibits [3H]-arachidonic acid release in human platelets stimulated by gamma thrombin and can induce peripheral analgesia by activating ATP-sensitive K+ channels.

Oxeladin citrate is a highly potent and effective cough suppressant, which can treat all types of cough of various etiologies. It is not related to opium or its derivatives, so treatment with oxeladin is no risk of addiction. And it has none of the side effects (such as hypnosis, respiratory depression, tolerance, constipation and analgesia) which are present when common antitussives. It can used at every age, as well as in patients with heart disease, since it is high level of safety and a great selectivity to act on the bulbar centre of cough.

Halothane (Anestan) is a nonflammable, halogenated, hydrocarbon anesthetic that provides relatively rapid induction with little or no excitement. Analgesia may not be adequate. NITROUS OXIDE is often given concomitantly. Because halothane may not produce sufficient muscle relaxation, supplemental neuromuscular blocking agents may be required.

Levobupivacaine is an amino-amide local anaesthetic drug belonging to the family of n-alkylsubstituted pipecoloxylidide. It is the S-enantiomer of bupivacaine. Levobupivacaine hydrochloride is commonly marketed by AstraZeneca under the trade name Chirocaine. Compared to bupivacaine, levobupivacaine is associated with less vasodilation and has a longer duration of action. It is approximately 13 per cent less potent (by molarity) than racemic bupivacaine.Levobupivacaine is indicated for local anaesthesia including infiltration, nerve block, ophthalmic, epidural and intrathecal anaesthesia in adults; and infiltration analgesia in children. Adverse drug reactions (ADRs) are rare when it is administered correctly. Most ADRs relate to administration technique (resulting in systemic exposure) or pharmacological effects of anesthesia, however allergic reactions can rarely occur.

(+)-BORNEOL (d-Borneol) is a natural bicyclic monoterpene used for analgesia and anesthesia in traditional Chinese medicine; enhances GABA receptor activity with an EC50 of 248 μM.

Flupirtine maleate (Katadolon maleate), a centrally acting non-opioid analgesia, is the salt form of Flupirtine. It is an NMDA receptor antagonist , and also a specific neuronal potassium channel opener.

Org 25543 is the development of an N-Acyl amino acid that selectively inhibits the glycine transporter 2 to produce analgesia in a rat model of chronic pain.

Solabegron (GW-427,353), is a selective agonist of β3 adrenergic receptors. In addition, Solabegron has been shown to produce visceral analgesia by releasing somatostatin from fat cells.

Imidazoleacetic acid (Imidazolyl-4-acetic acid) is a blood-brain barrier-permeable full agonist of the GABAA receptor. Imidazoleacetic acid is generated through histamine oxidation in the mouse brain and exerts multiple neurochemical and behavioral effects. Imidazoleacetic acid induces centrally mediated responses including analgesia, sedation, hypnosis, and reductions in blood pressure, body temperature, isolation-induced aggression, and motor activity. Imidazoleacetic acid is valuable for neuropharmacology and neurotransmitter signaling investigations involving histaminergic and GABAergic pathways.

Kyotorphin acetate is an endogenous peptide with analgesia activity and can be used as a biomarker of Alzheimer disease.

NeoSTX (Neosaxitoxin) is a specific sodium channel blocker that targets site 1. It works synergistically with local anesthetics to provide surgical anesthesia through peripheral nerve block or local infiltration and significantly prolongs postoperative analgesia duration.

exo-Tetrahydrocannabivarin (Compound 12) is an analog of Δ9,11-THC. It weakly binds to cannabinoid receptors (CB) with an IC50 of 1.4 μM. In mice, exo-Tetrahydrocannabivarin exhibits activity related to both motor function and analgesia.

N-Phenethylnoroxymorphone is an opioid compound that can enhance morphine-induced analgesia in rats. It is used in the research of neurological disorders.

BU72 is a potent, long-lasting agonist for μ and κ opioid receptors, with partial agonistic activity at the δ opioid receptor (EC50 values of 0.054, 0.033, and 0.58 nM, respectively). It provides strong, enduring analgesic effects primarily mediated through μ opioid receptors. BU72 also exhibits a prolonged duration of activity and can partially reverse morphine-induced analgesia. It is applicable in studies of opioid dependence.

SR 142948 TFA is an orally active, selective non-peptide neurotensin receptor (NT) antagonist, displaying IC50 values of 1.19 nM in h-NTR1-CHO cells, 0.32 nM in HT-29 cells, and 3.96 nM in adult rat brain. In HT-29 cells, it counteracts NT-induced inositol monophosphate formation with an IC50 of 3.9 nM. It blocks NT-induced hypothermia, analgesia, and turning behavior in vivo and can cross the blood-brain barrier, making it useful for research in psychiatric disorders.

Sameridine (NIH-10908) acts as a weak partial agonist at the μ-opioid receptor. When administered intrathecally, it induces local anesthesia and analgesia. At low doses, Sameridine minimally affects respiratory function, but higher doses can suppress respiratory response. It is useful for research into analgesic effects.

Zidometacin is a non-steroidal anti-inflammatory drug (NSAID) that significantly inhibits the synthesis of prostaglandins with minimal gastrointestinal damage. It has analgesic and antipyretic effects and shows a relatively low ulcerogenic potential in rat models. Zidometacin can be used for research in analgesia and osteoarthritis.

M119 is a selective Gβγ subunit inhibitor. It specifically enhances μ-opioid receptor (μ-receptor) dependent analgesia. M119 inhibits the activation of μ-receptor-dependent phospholipase (PLC). It can boost the effects of opioid analgesics and reduce acute tolerance and dependence in induced mouse models. M119 is applicable for pain research.