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.
PD-217014 is a GABA analog. It inhibits (3)H-gabapentin binding to alpha(2)delta subunit of voltage-gated calcium channels in a concentration-dependent manner (K(i) = 18 nmol/l). PD-217014 possesses visceral analgesic activity.
Neostibosan is an arsenic-containing parasitic agent. Due to the activity of arsenic on visceral L Ashmaniasis, one of the pentvalent antimony, which is less toxic, is synthesized and has potential activity on tumor cells.
Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004). Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2 References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004).
LXE408 is an orally active, kinetoplastid-selective proteasome inhibitor, exhibiting non-competitive inhibitory effects. It demonstrates an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. Moreover, LXE408 shows limited ability to traverse the blood-brain barrier. Hence, LXE408 holds promise for advancing research in the field of visceral leishmaniasis (VL).
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.