analgesic

Ziconotide Acetate (107452-89-1 free base) (Prialt) is an analgesic agent and has been used to treat neuropathic and non-neuropathic pain. Ziconotide Acetate (107452-89-1 free base) acts by binding to N-type calcium channels situated on the terminal part of primary afferent neurons of the nociceptive pathway therefore reducing synaptic transmission with potent antinociceptive effects.

DAMGO (DAGO) is an opioid receptor agonist with the ability to affect the locomotive activity in rodents. Possible analgesic agent due to μ-opiod receptor interaction.

Valorphin TFA(144313-54-2(free base)) is a semisynthetic derivative of dihydrovaltrate with opioid analgesic activity

Neurotensin TFA (39379-15-2 free base) is an endogenous 13 amino acid neuropeptide with profound opioid-independent analgesic effects. It behaves as a neurotransmitter in the brain, as a hormone in the gut, and also as a neuromodulator. It is implicated in the pathophysiology of several CNS disorders (including schizophrenia, Parkinson's disease, drug abuse, pain, cancer, inflammation, eating disorders, and central control of blood pressure) due to its association with a wide variety of neurotransmitter systems such as dopaminergic, sertonergic, glutamatergic, GABAergic, and cholinergic systems. It has a role as a human metabolite, a mitogen, a neurotransmitter and a vulnerary.

(D-Ser2)-Leu-Enkephalin-Thr is a delta selective agent of opioid receptor and shows analgesic effects.

[Lys8, Lys9]-Neurotensin (8-13) (JMV438) is a Neurotensin analog that elicits analgesic effects by activating the G protein-coupled receptors NTS1 and NTS2, with K i values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively.

Endogenous melanocortin MC3 receptor agonist (pKi = 7.46) that displays ~ 40-fold selectivity over MC4. Increases the release of extracellular dopamine, which induces grooming and vertical activity (rearing) in rats. Exhibits hypertensive, tachycardic and

[Lys8, Lys9]-Neurotensin (8-13) acetate, a Neurotensin analog, exerts its analgesic effects through activation of the G protein-coupled receptors NTS1 and NTS2, with Ki values of 0.33 nM and 0.95 nM for hNTS1 and hNTS2 receptors, respectively[1].

Helianorphin-19 is a high affinity, potent and selective κ-opioid receptor (KOR) agonist (Ki = 25 nM; EC50= 45 nM). Helianorphin-19 exhibits approximately 200-fold selectivity for KOR over μ and δ-opioid receptors.In vivoHelianorphin-19 shows potent peripheral analgesic efficacy in a mouse model of visceral pain without affecting motor coordination/sedation.

[Nphe1]Nociceptin(1-13)NH2 is a novel endogenous ligand for the nociceptin orphanin FQ (NC) receptor, acting as a selective and competitive antagonist without any agonist effects. It binds specifically to recombinant nociceptin receptors with high affinity (pKi=8.4) and effectively blocks nociceptin's ability to inhibit cyclic AMP accumulation in CHO cells (pA2=6.0), showcasing potential as an analgesic agent.

[D-Ala2] Leu-Enkephalinamide, an enkephalin analog, exhibits significant corneal permeability and analgesic properties, making it suitable for ocular disease research [1] [2].

Dynorphin A (1-13) amide, an endogenous opioid peptide, counteracts the analgesic effects of morphine [1].

Orexin A (human, rat, mouse) acetate (Hypocretin-1) is an excitatory neuropeptide with analgesic properties. It activates Orexin-1 (OX1R) and Orexin-2 (OX2R) receptors, used for studying neurodegenerative diseases.

Ac-YVAD-AOM is a selective and potent caspase-1 inhibitor showing antitumor activity and potential analgesic activity.

μ-Conotoxin KIIIA, an analgesic compound derived from Conus kinoshitai, selectively inhibits mammalian neuronal voltage-gated sodium channels (VGSCs) (Nav1.2), offering potential utility in pain research [1] [2].

[DPro10] Dynorphin A (1-11), porcine hydrochloride, is an N-alkylated derivative and potent κ-opioid receptor agonist with a K i value of 0.13 nM, possessing analgesic properties [1] [2].

[DPro10] Dynorphin A (1-11), porcine, an N-Alkylated derivative, serves as a potent κ-opioid receptor agonist with a Ki value of 0.13 nM, exhibiting analgesic properties [1] [2].

Crotamine, a 42 amino acid toxin featuring three disulfide bridges, functions as a Na+ channel modulator with analgesic properties. This compound interacts with lipid membranes and exhibits myonecrotic activity, and can be isolated from the venom of Crotalus durissus terrificus [1] [2].

αO-Conotoxin GeXIVA, a potent antagonist of the α9α10 nicotinic acetylcholine receptor (nAChR), exhibits an inhibition concentration 50 (IC50) of 12 nM against rat α9α10 nAChRs. This compound has demonstrated analgesic properties in animal pain models [1].

Theraphotoxin-Tap1a (Tap1a) is a spider venom-derived peptide that acts as an inhibitor of sodium channels, displaying IC50 values of 80 nM for Na v 1.7 and 301 nM for Na v 1.1. It demonstrates analgesic effects [1].

Huwentoxin-IV TFA is a potent, selective blocker of sodium channels, specifically inhibiting neuronal Nav1.7, Nav1.2, Nav1.3, and Nav1.4 with IC50 values of 26, 150, 338, and 400 nM, respectively. It preferentially targets the peripheral nerve subtype Nav1.7 by interacting with neurotoxin receptor site 4, demonstrating analgesic effects in animal models of inflammatory and neuropathic pain [1] [2].

Connexin43 mimetic peptide. Reduces swelling, astrogliosis, neuroinflammation and neuronal cell death following spinal cord injury ex vivo and in vivo. Exhibits analgesic effects in models of neuropathic pain. O'Carroll et al (2008) Connexin 43 mimetic peptides reduce swelling, astrogliosis and neuronal cell death after spinal cord injury. Cell.Commun.Adhes. 15 27 PMID:18649176 |Mao et al (2017) Characterisation of Peptide5 systemic administration for treating traumatic spinal cord injured rats. Exp.Brain.Res. 235 3033 PMID:28725925 |Kim et al (2017) Characterising the mode of action of extracellular Connexin43 channel mimetic peptides in an in vitro ischemia injury model. Biochem.Biophys.Acta. 1861 68 PMID:27816754 |Tonkin et al (2017) Attenuation of mechanical pain hypersensitivity by treatment with Peptide5, a connexin-43 mimetic peptide, involves inhibition of NLRP3 inflammasome in nerve-injured mice. Exp.Neurol. 300 1 PMID:29055716

Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases late

Super-tdu (1-31) TFA is an endogenous ligand of heptapeptide receptor and has a strong anti-analgesic effect.