salivary

Tolterodine tartrate (PNU-200583E) is a potent antagonist for muscarinic receptor. It show selectivity for the urinary bladder and salivary glands in vivo.

P-113 acetate is an antimicrobial peptide (AMP) derived from the human salivary protein histatin 5, shows good safety and efficacy profiles in gingivitis and human immunodeficiency virus (HIV) patients with oral candidiasis.

gamma-preprotachykinin amide (72-92) acetate is a 21 amino acid peptide belonging to the tachykinin (TK) family and including neurokinin A (NKA) in its C-terminal sequence. gamma-preprotachykinin amide (72-92) acetate possesses higher affinity than NKA for central NK-2 receptors; it shows lower affinity for NK-1 receptors, however, it potently stimulates salivary secretion, which is mediated by NK-1 receptor activation.

L-Hyoscyamine (Daturine) functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. Hyoscyamine is a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

PK14105 has been evaluated biologically as a potential radioligand for positron emission tomography (PET) studies targeting peripheral benzodiazepine binding sites (PBBS) receptors. When administered to rats with unilaterally lesioned striata, PK14105 was observed to quickly cross the blood-brain barrier, displaying significant radioactivity retention in the lesioned striatum, in contrast to the unlesioned striatum or cerebellar vermis. Additionally, PK14105 has the capability to inhibit receptor ligands, calcium channel ligands, and co-transporters in all salivary glands.

Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine that functions as a selective, orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride effectively stimulating exocrine secretion from salivary glands and thereby serving as a clinically relevant sialogogue for the treatment of xerostomia, while its demonstrated ability to cross the blood–brain barrier supports its utility in central and peripheral cholinergic signaling studies and translational neuropharmacological investigations.

JQ dS-4 is a degrader of Brahma-related gene 1 (BRG1)/BRM/SMARCA4 (PROTAC®; DC50 range = 9 - 390 nM in glioma models and cell lines), featuring a BRG1 inhibitor connected through a linker to a cereblon (CRBN) E3 ligase ligand. It effectively degrades BRG1 completely over 48 and 72 hours in HSJD-DIPG007 and SU-DIPGXIIIP cells. Additionally, it lessens the viability of various cancer cell lines, including those of H3K27M glioma, prostate, thyroid, and salivary gland.

Cevimeline, a parasympathomimetic and muscarinic agonist, affects M1 and M3 receptors. Cevimeline has been shown to treat dry mouth and Sj gren's syndrome. It is also used to reduce Xerostomia symptoms and increase salivary flow in head and neck cancer survivors after radiotherapy.

G3-CNP is a substrate for α-amylase and the hydrolysis product is 2-chloro-4-nitrophenol, which can be used to determine the enzyme activity by colorimetric assay at 405 nm.

2F-Peracetyl-Fucose (1,3,4-Tri-O-acetyl-2-deoxy-2-fluoro-L-fucopyranos) is a potent fucosyltransferase (FUT) inhibitor that suppresses salivary acidification and fucosylation in an in vitro inflammatory model.

Pentagastrin (ICI-50123) is a synthetic polypeptide that mimics the effects of gastrin when administered parenterally, influencing the secretion and synthesis of salivary proteins.

L-Hyoscyamine sulfate (Levsin Sulfate) is the sulfate salt of a belladonna alkaloid derivative and the levorotatory form of racemic atropine isolated from the plants Hyoscyamus niger or Atropa belladonna, which exhibits anticholinergic activity. Hyoscyamine functions as a non-selective, competitive antagonist of muscarinic receptors, thereby inhibiting the parasympathetic activities of acetylcholine on the salivary, bronchial, and sweat glands, as well as the eye, heart, bladder, and gastrointestinal tract. These inhibitory effects cause a decrease in saliva, bronchial mucus, gastric juices, and sweat. Furthermore, its inhibitory action on smooth muscle prevents bladder contraction and decreases gastrointestinal motility.

Atropine Oxide Hydrochloride is a derivative of Atropine. Atropine is utilized in research involving nerve agent and pesticide poisoning models, selected forms of bradycardia, and salivary secretion regulation during surgical procedures. Atropine functions as a competitive antagonist of muscarinic acetylcholine receptor subtypes M1, M2, M3, M4, and M5 and is classified as an anticholinergic (parasympatholytic) compound. Atropine Oxide Hydrochloride is therefore relevant for pharmacological investigations involving cholinergic neurotransmission, receptor antagonism, autonomic nervous system regulation, and toxicological response mechanisms.

9AzNue5Ac is a Neu5Ac analog that is metabolized in living cells and in mice.9AzNue5Ac binds to salivary glycans.

Acetyl-Adhesin (1025-1044) amide, a 20-peptide fragment derived from the cell surface adhesin of Streptococcus pyogenes, functions as an antimicrobial peptide. It specifically prevents Streptococcus pyogenes recolonization by inhibiting the adhesin's binding to salivary receptors [1].

Chinese gallotannin, derived from Galla Chinensis, is a non-specific promiscuous inhibitor of various enzymes. It is a potent inhibitor of human salivary α-amylase, with a Ki value of 0.82 μg/mL. Mechanistic studies reveal that gallotannins exert their inhibitory effects through the formation of aggregates, which serve as the active species in the inhibition process. Beyond its role in carbohydrate metabolism, it exhibits inhibitory activity against telomerase, fatty acid synthase, and 5α-reductase, making it a versatile tool for research in diabetes, oncology, and metabolic disorders.

Helospectin II, a member of the vasoactive intestinal peptide (VIP) family, exhibits vasodilatory and antihypertensive properties that reduce blood pressure. This neuropeptide was initially isolated from the venom of the salivary glands of the Heloderma suspectum lizard [1] [2].

Helospectin I, a neuropeptide belonging to the vasoactive intestinal peptide (VIP) family, exhibits vasodilatory and antihypertensive properties, effectively reducing blood pressure. It was initially isolated from the salivary gland venom of the lizard Heloderma suspectum [1] [2].

Histatin 8, a salivary antimicrobial peptide derived from proteolytic fragments of histatin 3 and histatin 5, exhibits activity against A. baumannii strains, both colistin-susceptible and -resistant, at a concentration of 32 µg/ml. Additionally, it is effective against C. albicans and C. tropicalis, with minimum inhibitory concentrations (MICs) of 1 and 5 mg/ml, respectively.

Histatin 3, a salivary antimicrobial peptide, exhibits activity against C. albicans with an LC50 of 9.2 µM. Additionally, at a concentration of 12 µM, it promotes actin polymerization in cell-free assays.

Lys(CO-C3-p-I-Ph)-O-tBu, a pharmacokinetic modifier (PK modifier), enhances the pharmacokinetic properties of PSMA ligand molecules by increasing their residence time in plasma through improved binding to albumin and reducing absorption by the salivary glands, potentially extending the active compound's half-life. Moreover, Ac-PSMA-trillium is an effective PSMA-targeting compound for various biological applications when modified with different radioactive isotopes. When labeled with 111 In, it serves as a DOTA chelating agent and imaging agent. Alternatively, when labeled with 225 Ac, it acts as a Macropa chelator for targeted radionuclide therapy (TRT) in researching metastatic castration-resistant prostate cancer (mCRPC) [1] [2].

Eledoisin trifluoroacetate (69-25-0 free base) is a peptide extracted from the posterior salivary glands of certain small octopi (Eledone spp., Mollusca), or obtained by synthesis. Its actions resemble those of SUBSTANCE P; it is a potent vasodilator and increases capillary permeability.

TfR-1-IN-1 is a transferrin receptor 1 (TfR-1) inhibitor, also an Fe(III) salivary phenol complex, with anticancer activity. It induces apoptosis, inhibits the growth of tumor cells and normal cells, and is used in studies of leukemia.

rac-Tolterodine-D14 Tartrate is a deuterated compound of rac-Tolterodine Tartrate. rac-Tolterodine Tartrate has a CAS number of 124937-52-6. Tolterodine Tartrate (T0099) is a potent antagonist for muscarinic receptor. It show selectivity for the urinary bladder and salivary glands in vivo.