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.

GSK3494245 is a Leishmania donovani inhibitor that suppresses trypsin-like activity catalyzed by the β5 subunit of L. donovani proteasome, applicable for visceral leishmaniasis (VL) studies.

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.

CP-99994 is a neurokinin 1 (NK-1) receptor antagonist with a Ki of 0.25 nM. It prevents colorectal sensitization under conditions of visceral hypersensitivity and reduces acetic acid-induced colorectal sensitization in a bladder-colon cross-sensitization model. CP-99994 also attenuates neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity.

DNDI-0690 is a potent and orally active analogue of DNDI-VL-2098, demonstrating significant efficacy against cutaneous leishmaniasis (CL). It exhibits notable in vitro activity against Leishmania parasites responsible for CL, with an EC50 of 0.17 μM for visceral leishmaniasis and an EC50 of less than 5 μM for the causative parasites of CL. Additionally, DNDI-0690 is effective in a L. major CL mouse model and is applicable for research in CL.

LI-633 is a selective orally bioactive GABAA receptor positive allosteric modulator (PAM) with a Ki value of 21 nM. It significantly enhances GABA-induced inward currents, with EC50 values ranging from 8 nM (α5β2γ2) to 128 nM (α3β2γ2). LI-633 also increases muscimol-induced GABAergic currents in rat dorsal root ganglion (DRG) neurons, with an EC50 of 70.4 nM. LI-633 is useful for studying visceral pain.

COX-2/CaV2.2-IN-1 is an orally active, selective dual-target inhibitor of COX-2 and CaV2.2, with an IC50 of 0.26 μM for COX-2 and 0.29 μM for CaV2.2. It effectively suppresses inflammatory responses and the production of inflammatory mediators (IL-6, TNF-α, NO). This compound demonstrates significant analgesic effects in various models of inflammatory pain, neuropathic pain, and visceral pain, making it a valuable tool for research in chronic pain-related studies.

DNDI-VL-2098 is an orally active antileishmanial agent known for its high permeability and in vitro metabolic stability. It selectively inhibits CYP2C19 with an IC50 of 0.47 μM and does not affect other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6, and CYP3A4) at concentrations up to 12.5 μM. The compound exhibits favorable pharmacokinetic properties across various animal models including mice, hamsters, rats, and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding, making it suitable for visceral leishmaniasis research.

The compound σ1R/H3R ligand-1 is a dual σ1R/H3R antagonist with a σ1RKi of 8.8 nM and an H3RKi of 31.2 nM. It demonstrates potent, dose-dependent analgesic activity in mouse models of visceral and neuropathic pain through its simultaneous antagonistic effect on σ1R and H3R. σ1R/H3R ligand-1 is useful for research on visceral and neuropathic pain.