antinociception

BIMU 8 is a selective agonist of 5-HT4 with EC50s of 18 nM, 77 nM, and 540 nM for wild-type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4.

Methylene Blue trihydrate (Basic blue 9) is a compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene Blue trihydrate is used as a bacteriologic stain and as an indicator. It inhibits soluble guanylyl cyclase and has been used to treat cyanide poisoning and to lower levels of methemoglobin. It also inhibits tau filament formation (IC50: 1.9μM).

Phenylmethanesulfonyl fluoride (PMSF (Phenylmethylsulfonyl fluoride)) is an enzyme inhibitor that inactivates IRC-50 arvin, subtilisin, and the fatty acid synthetase complex.

1. Gelsemine (Gelsemin) has antitumor activity. 2. Gelsemine has anti-oxidative activity. 3. Gelsemine has anti-hyperlipidemic activity. 4. Gelsemine has marked antinociception in inflammatory, neuropathic and bone cancer pains without inducing antinociceptive tolerance.

Rosmanol has antioxidant activity, it can activate the antioxidant response element. Rosmanol has biphasic modulation of GABAA receptors, demonstrates CNS activity in mouse models of antinociception, antidepressant and anxiolysis. Rosmanol potently induce

Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor, producing antinociception in animal models of acute pain and reducing hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

β-Endorphin (1-27) (human) acetate, existing in the hypophysis cerebri and hypothalamus, exhibits antinociception activity. β-Endorphin (1-27) (human) acetate is an agonist of opioid receptor, showing preferred affinity for μ-opioid receptor and δ-opioid

AR-C102222 hydrochloride is a competitive, orally active, and highly selective inducible nitric oxide synthase (iNOS) inhibitor (IC50: 37 nM). It has antinociception and anti-inflammatory activities.

JDTic is a powerful antagonist of kappa-opioid receptors (KOR), effectively inhibiting the antinociceptive effects induced by the κ-agonist U50, 488.

A-317567 is a potent acid-sensing ion channel 3 (ASIC-3) inhibitor with an IC50 of 1.025 μM, exhibiting antidepressant and antinociceptive effects[1][2].

Paynantheine is an alkaloid with antinociceptive properties, found in Mitragyna speciosa. It also acts as an agonist at 5-HT1AR and 5-HT2BR receptors, inducing lower lip contraction and providing antinociception in rats.

KOR agonist 5 (Compound 10a) is both a KOR MOR modulator, exhibiting agonistic effects on KOR and antagonistic effects on MOR. It effectively blocks morphine-induced antinociception and gastrointestinal motility inhibition. KOR agonist 5 is applicable in research related to substance use disorder (SUD).

Tingenone is a pentacyclic triterpene. It induces peripheral antinociception due to opioidergic activation.

Leucylarginine hinders antinociception induced by L-arginine.

ONO-1714 is a inducible nitric oxide synthase (NOS-2) inhibitor. ONO-1714 reduces hyperoxic lung injury in mice. ONO-1714 attenuates inflammation-related large bowel carcinogenesis in male Apc(Min +) mice. ONO-1714 also inhibits neuronal NOS and exerts an

ZCZ011 is a positive allosteric modulator of the cannabinoid CB1 receptor. ZCZ011 is brain penetrant, increased the potency of orthosteric agonists in mouse behavioral assays indicative of cannabimimetic activity, including antinociception, hypothermia, c

MS 15203 is a selective GPR171 agonist that increases morphine antinociception and is effective in reducing chronic pain. It can reduce chronic neuropathic and inflammatory pain in male mice.

(S)-AM1241 binds to cannabinoid (CB) receptors and is selective for the CB2 over the CB1 receptor (Kis = 658 and >10,000 nM, respectively, in a membrane assay using human receptors). (S)-1241 acts as an agonist at human, rat, and mouse CB2 receptors but shows greater activity at human CB2 (EC50 = 131 nM) than at rat and mouse CB2 receptors (EC50 = 785 and 2,000 nM, respectively). Similar to the racemate AM1241 , (S)-AM1241 produces antinociception to thermal, but not mechanical, pain in rats. The pain-reducing effect of (S)-AM1241 is blocked by the CB2-specific inhibitor SR 144528 but not by either the CB1-selective inhibitor rimonabant or the opioid receptor blocker naloxone .

β-Endorphin (1-27) is an endogenous peptide that binds to μ-, δ-, and κ-opioid receptors (Kis = 5.31, 6.17, and 39.82 nM, respectively, in COS-1 cells expressing rat receptors). It binds to rat and mouse brain membrane preparations (IC50s = 1.1 and 5.7 nM, respectively) and induces chemotaxis of human monocytes in vitro when used at a concentration of 1 nM. Intracerebroventricular administration of β-endorphin (1-27) increases the latency to tail withdrawal in response to thermal stimulation in mice with a median antinociceptive dose (AD50) of 1,500 pmol per animal. It inhibits antinociception induced by β-endorphin in mice in response to thermal stimuli when administered at a dose of 65 pmol per animal. In rats, β-endorphin (1-27) does not affect drug-associated place preference when administered at doses up to 20 μg, i.c.v., but inhibits β-endorphin-induced place preference when administered at a dose of 10 μg per animal.

Paederosidic acid methyl ester has antinociception, is possibly related to the pathway of NO-cGMP-ATP sensitive K(+) channels.

SC13, a novel mitragynine analog, exhibits low-efficacy agonism at Mu opioid receptors and provides antinociception while minimizing adverse effects.

JWH 030 is a potent naphthoyl pyrrole cannabimimetic, exhibiting higher affinity for the CB1 receptor (EC50= 30.5 nM in rats, Ki= 87 nM in mice) compared to CB2 (EC50= 552 nM in human CB2 receptors). The compound demonstrates significant in vivo potency in mouse models, specifically in spontaneous activity and tail flick assays (antinociception) with an ED50 value of 26.8 μM/kg. Furthermore, JWH 030 dose-dependently reduces electrically-induced contractions in the mouse vas deferens, with an IC50 of 3.38 nM, highlighting its effective modulatory effects. This compound is designated for forensic or research applications.

Dicentrine, a selective α±(1)-adrenoceptor antagonist with potent antiarrhythmic and antihypertensive activities, it also has antinociception in different models of chemical pain.

Deoxylimonin (NSC 314317) is a triterpenoid isolated from grapefruit seeds.