nociceptive

AP-18 is a potent and selective TRPA1 inhibitor. AP-18 inhibits activation of TRPA1 induced by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 could reverse complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 could attenuate Yo-Pro uptake induced by 30 μM AITC in a concentration-dependent manner (IC50= 10.3 μM).

Alosetron hydrochloride (GR 68755) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist. Alosetron blocks the actions of serotonin at 5-HT3 sites in the peripheral nervous system, particularly on enteric and nociceptive sensory neurons, thereby affecting the regulation of visceral pain, decreasing gastrointestinal contraction and motility, and decreasing gastrointestinal secretions.

ABT-963 is a potent and selective inhibitor of disubstituted pyridazinone cyclooxygenase-2 (LOX2) that dose-dependently reduces injury perception in a carrageenan model of nociceptive sensitization.ABT-963 is used in the study of arthritis.

CGP 29030A is a new piperazine derivative with analgesic activity and significant inhibitory effect on potentially nociceptive dorsal horn neurons, which can be used to study painful disorders.

3-Carene(Delta-3-Carene) is a bicyclic monoterpene extracted from western larch and Douglas-fir that acts as a phytofungicide.3-Carene inhibits inflammatory infiltrates and COX-2 overexpression induced by nociceptive stimuli.3-Carene has anti-injury properties and promotes the activity and expression of alkaline phosphatase, an early marker of osteoblast differentiation.

Zolmitriptan (311C90) selectively binds to and activates serotonin (5-HT) 1B receptors expressed in intracranial arteries and 5-HT 1D receptors located on peripheral trigeminal sensory nerve terminals in the meninges and central terminals in brainstem sensory nuclei. Zolmitriptan is a member of the triptan class of agents with anti-migraine properties. Receptor binding results in constriction of cranial vessels, reduction of vessel pulsation and inhibition of nociceptive transmission, thereby providing relief of migraine headaches. Zolmitriptan may also relieve migraine headaches by inhibition of pro-inflammatory neuropeptide release.

Vanillyl Alcohol (3-Methoxy-4-hydroxybenzyl alcohol) possesses anti-angiogenic, anticonvulsive, anti-inflammatory, anti-oxidant, neuroprotective, and anti-nociceptive activities. Vanillyl alcohol can effectively inhibit the cytotoxicity and improved cell viability in 1-methyl-4-phenylpyridinium (MPP+)-induced MN9D dopaminergic cells, it also can attenuate the elevation of reactive oxygen species (ROS) levels, decrease in the Bax Bcl-2 ratio and poly (ADP-ribose) polymerase proteolysis.

Fursultiamine (Alinamin F) is a disulfide derivative of thiamine, or an allithiamine. It has potential uses in the treatment of vitamin B1 deficiency.

beta-Escin is a natural mixture of triterpenoid saponins isolated from horse chestnut (Aesculus hippocastanum) seeds, can be used as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent.

Dihydrocapsaicin (CCRIS1589) is isolated from Capsicum fruit. Capsaicin is the primary active component of the heat and pain-eliciting lipid soluble fraction of the Capsicum pepper. Like capsaicin, dihydrocapsaicin is an irritant. Capsaicin is found in natural hot pepper extracts along with a number of impurities, including dihydrocapsaicin and several lesser impurities. Separation by HPLC is required in order to obtain pure dihydrocapsaicin. Dihydrocapsaicin represents about 10% of the compound present in commercial preparations purporting to be pure capsaicin, but it has about the same pungency as capsaicin. VR1 (vanilloid receptor 1) is a heat activated calcium ion channel which functions as a part of the normal nociceptive pain pathway. Capsaicin elicits a sensation of burning pain by activation of VR1 on small, non-myelinated polymodal C-type nociceptive nerve fibers. The potency of dihydrocapsaicin at VR1 appears equivalent to capsaicin. Antioxidant. Reduces oxidation of serum lipids. Mutagenic. Dihydrocapsaicin is an activator of VR1.

1. Vitexin has antinociceptive and antispasmodic activities. 2. Vitexin exhibits a prominent first-pass effect. 3. Vitexin has antioxidant, antimyeloperoxidase, and α-glucosidase inhibitory activities. 4. Vitexin can either inhibit or induce activities of

σ1 Receptor antagonist-1 is a selective σ1 receptor antagonist.

BAY-1797 is an orally active and selective P2X4 antagonist (IC50: 211 nM against human P2X4) with anti-nociceptive and anti-inflammatory effects. BAY-1797 displays no or very weak activity on the other P2X ion channels.

(S)-Mirtazapine ((S)-Org3770) is the S(+)-enantiomer of Mirtazapine, functioning as a selective 5-HT2 receptor antagonist with pro-nociceptive effects. It is commonly used in combination with the R(-)-enantiomer of Mirtazapine to study depression.

Umbellulone is a natural product isolated from Umbellularia californica, and stimulates the TRPA1 channel in a subset of peptidergic, nociceptive neurons, activating the trigeminovascular system via this mechanism.

AZD8797 (KAND567) is an orally available, selective and potent human CX3CR1-converting antagonist with inhibitory effects on CX3CR1 and CXCR2, and potentially protects against SARS-CoV-2-induced neuronal damage, preventing worsening of nociceptive sensitization and microglial activation in a migraine model of rats following seizures.

Levomepromazine (Methotrimeprazine) is an orally active aliphatic phenothiazine antipsychotic compound and a Ca2+ release inducer, exhibiting antiviral, anti-inflammatory, neuroprotective, analgesic, and anti-nociceptive activities. Levomepromazine inhibits dopaminergic, cholinergic, serotoninergic, and histaminergic receptors, and is used for research in neurodegenerative diseases.

AMTB hydrochloride (AMTB HCl) is a novel TRPM8 channel blocker and is effective for pain and urinary diseases. AMTB can act on the bladder afferent pathway to attenuate the bladder micturition reflex and nociceptive reflex responses in the rat.

Cannabidiolic acid methyl ester (HU-580) is an orally active analogue of cannabidiolic acid. It enhances the activation of 5-HT1A receptors and increases the expression of c-Fos and NeuN in specific hypothalamic nuclei in rats. Cannabidiolic acid methyl ester exhibits anti-nausea, anxiolytic, and anti-nociceptive effects.

Bromadoline is an opioid compound that exhibits anti-nociceptive properties in rodents.

Pyrithioxin dihydrochloride (Pyrithioxine HCl) has anti-nociceptive and anti-allodynic effects, can promote the metabolism of glucose and amino acids in the brain, improve systemic assimilation, and can be used to study neurological diseases such as atherosclerosis. Pyrithioxin dihydrochloride can induce severe cholestatic hepatitis.

TFLLR-NH2, reversed amino acid sequence control peptide, is a PAR1 selective agonist that significantly increases the nociceptive threshold.

N(G)-Nitroarginine-4-nitroanilide is an anti-nociceptive in mice.

Efipladib is a phospholipase inhibitor. Efipladib decreases nociceptive responses without affecting PGE2 levels in the cerebral spinal fluid.