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.

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

Semax is a synthetic peptide analog of adrenocorticotropic hormone (ACTH) that has neuroprotective, analgesic, and anxiolytic properties.

Semax acetate is a synthetic peptide analog of adrenocorticotropic hormone (ACTH) that has neuroprotective, analgesic, and anxiolytic properties.

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

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

[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.

[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.

Endomorphin 1 acetate is a selective and highly effective μ-opioid receptor agonist with anti-nociceptive and analgesic effects. Endomorphin 1 acetate shows high affinity for kappa3 and can be used to study neurological diseases.

Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effects.

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.

MIF-1 TFA (Melanostatin), an intrinsic brain peptide, serves as a powerful allosteric modulator of the dopamine receptor. It plays a crucial role in regulating melanin production and modifies the analgesic efficacy by inhibiting the opioid receptor's effects. Significantly, MIF-1 TFA can cross the blood-brain barrier (BBB) directly, facilitating its access from the bloodstream to the central nervous system (CNS) [1] [2] [3].

Huwentoxin XVI TFA, a potent analgesic derived from the Chinese tarantula Ornithoctonus huwena, acts as a highly reversible and selective antagonist of mammalian N-type calcium channels (IC 50 of ~60 nM), with no impact on voltage-gated T-type calcium channels, potassium channels, or sodium channels [1].

L-R4W2 TFA acts as a potent antagonist of vanilloid receptor 1 (VR1, TRPV1), demonstrating significant inhibitory activity with an IC50 value of 0.1 μM. This compound potentially offers powerful analgesic properties [1] [2].

Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective non-competitive inhibitor of TrkB, effectively impeding BDNF-triggered TrkB activity without altering BDNF binding affinity, with an IC50 of 0.30 nM. It crosses the blood-brain barrier, demonstrating analgesic and anxiolytic-like behavioral effects [1] [2] [3].

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].

Orphanin FQ(1-11) TFA, a fragment of orphanin FQ or nociceptin (OFQ N), acts as a powerful NOP receptor (ORL-1; OP4) agonist with a K i of 55 nM. It lacks affinity for μ, δ, κ1, and κ3 receptors (K i >1000 nM), demonstrating specificity, and exhibits analgesic properties in CD-1 mice [1] [2].

[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.

CTOP TFA, a potent and highly selective μ-opioid receptor antagonist, antagonizes acute analgesic effects and hypermotility, while enhancing extracellular dopamine levels in the nucleus accumbens. It also dose-dependently increases locomotor activity [1] [2].

[D-Ala2]-Met-Enkephalinamide, an opioid peptide, is a potent opioid agonist that reduces bile flow through a central mechanism and exhibits analgesic properties [1] [2].

Dynorphin (2-17), amide (porcine) is a dynorphin derivative from the opioid peptide class, synthesized from the precursor protein dynorphinogen, and exhibits analgesic properties, playing a pivotal role in regulating pain, addiction, and mood [1].