visceral

N-(2-Hydroxypropyl)methacrylamide is utilized in the synthesis of copolymers for the targeted delivery of antileishmanial agents in [Visceral leishmaniasis].

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.

GSK3179106 is RET kinase inhibitor with an IC50 of 0.4 nM

INT-767 is a potent farnesoid X receptor (FXR)/TGR5 dual agonist that prevents NASH and promotes visceral adipose brown lipogenesis and mitochondrial function for the study of non-alcoholic steatohepatitis.

DNDI-6148 has anti-experimental cutaneous leishmaniasis activity and can be used to study visceral leishmaniasis by inhibiting Leishmania protozoa cleavage and polyadenylation-specific factor (CPSF3) endonuclease.

1. Stearic acid (Cetylacetic acid) can reduce metastatic tumor burden. 2. Stearic acid leads to dramatically reduced visceral fat likely by causing the apoptosis of preadipocytes. 3. Stearic acid and its derivatives have been used as gelators in food and pharmaceutical gel formulations. 4. Stearic acid is a potent phosphatase 1B inhibitor, possibly causing an enhancement in the insulin receptor signaling to stimulate glucose uptake into adipocytes. 5. Stearic acid has the potential to increase dry matter intake and yields of milk and milk components, without affecting conversion of feed to milk, body condition score, or body weight.

Phe-Met-Arg-Phe Like Peptide acetate (Pqdpflrfamide acetate) is a FMRF-like peptide from visceral and somatic muscles of the snail Helix aspersa. FMRF (Phe-Met-Arg-Phe) is a neuropeptide peptide consisting of 4 amino acid residues.

Miltefosine (HePC) is the treatment of visceral and cutaneous leishmaniasis drug , and is proceeding clinical trials for this in several countries. Several medical agents produce some potency against visceral or cutaneous leishmaniasis, however a 2005 survey concluded that miltefosine is the only effective oral treatment for both forms of leishmaniasis.

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.

Acivicin (AT-125), a chlorinated amino acid antibiotic produced by Streptomyces porcineus, is a γ-glutamyl transpeptidase (GGT) inhibitor that crosses the blood-brain barrier, exhibits anticancer and antiparasitic activity, and is used in the study of visceral leishmaniasis.

PD 173212 is a blocker that blocks N-type voltage sensitive calcium channel (Cav2.2). PD173212 (0.0017-1.7 μmol/kg, Intraperitoneal Injection.) dose-dependently reduced DNBS-induced visceral hypersensitivity in mice.

PD-217014 is an α2δ ligand that exhibits visceral analgesic activity and can suppress visceral hypersensitivity. Its antihyperalgesic effects are dose-dependent.

Dicentrine, (-)- (NSC-251699) is an aporphinic alkaloid found in several plant species, which showed significant antinociceptive activity in an acute model of visceral pain in mice.

Oxyphenonium Free Base, a quaternary ammonium anticholinergic agent, exhibits peripheral side effects paralleling those of ATROPINE. It functions as an adjunct in managing gastric and duodenal ulcers and alleviates visceral spasms. The compound is also employed as eye drops to induce a mydriatic effect.

AZM198 is a selective, orally active, and irreversible inhibitor of MPO with an IC50 of 15.0 nM. It exhibits an IC50 of 19 μM against CYP3A4 and possesses favorable lipophilicity, membrane permeability, metabolic stability, safety, and pharmacokinetic properties. AZM198 shows efficacy in improving vascular function, atherosclerotic plaques, pulmonary hypertension, nephropathy, visceral inflammatory fat deposition, ectopic fat deposition, and liver fibrosis.

TNP-ATP is an antagonist of purinergic P2Y1, P2X3, and P2X2/3 receptors, exhibiting IC50 values of 6, 0.9, and 7 nM, respectively, in HEK293 cells expressing human receptors. It reduces acetic acid-induced calcium flux in 1321N1 cells expressing P2X3 and P2X2/3 receptors with IC50 values of 100 and 62 nM, respectively. TNP-ATP also dose-dependently alleviates acetic acid-induced writhing responses in a visceral pain model in mice, with an ED50 of 6.35 µmol/kg.

Antiparasitic agent-27 (Compound 2) is a potent antiparasitic compound targeting Leishmania infantum with an IC50 of 3.1 μM. It induces cell cycle arrest in the G0/G1 phase and enhances reactive oxygen species (ROS) production to trigger programmed cell death, showing promise for visceral leishmaniasis (VL) research.

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.

Oxyphenonium bromide (Oxyfenon) shows anticholinergic activity and can be used for research on the treatment of gastric and duodenal ulcers and for the relief of visceral spasms.

(Ala13)-Apelin-13 acetate, an APJ antagonist, modulates CRF-induced enhanced colonic motility, visceral sensation, and gut barrier.

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).

(2R/S)-6-PNG (6-Prenylnaringenin) is a novel natural histone deacetylase inhibitor with anticancer and antitumor activity, and it blocks T-type calcium channels to reduce neuropathic and visceral pain in mice.

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).