Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UNIPROT:P01178 (oxytocin)
 15,767 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We identified Kv3-like high-threshold K+ currents in hypothalamic supraoptic neurons using whole cell recordings in hypothalamic slices and in acutely dissociated neurons. Tetraethylammonium (TEA)-sensitive currents (< 1 mM TEA) evoked from -50 mV were characterized by a large component that inactivated in 10-30 ms, and a smaller, persistent component that inactivated in 1-2 s. I/V relations in dissociated neurons revealed TEA-subtracted currents with a slope and voltage dependency consistent with the presence of Kv3-like channels. In slices, tests with 0.01-0.7 mM TEA produced an IC50 of 200-300 nM for both fast and persistent currents. The fast transient current was similar to currents associated with the expression of Kv3.4 subunits, given that it was sensitive to BDS-I (100 nM). The persistent TEA-sensitive current appeared similar to those attributed to Kv3.1/3.2 subunits. Although qualitatively similar, oxytocin (OT) and vasopressin (VP) neurons in slices differed in the stronger presence of persistent current in VP neurons. In both cell types, the IC50 for TEA-induced spike broadening was similar to that observed for current suppression in voltage clamp. However, TEA had a greater effect on the spike width of VP neurons than of OT neurons. Immunochemical studies revealed a stronger expression of the Kv3.1b alpha-subunit in VP neurons, which may be related to the greater importance of this current type in VP spike repolarization. Because OT and VP neurons are not considered fast firing, but do exhibit frequency- and calcium-dependent spike broadening, Kv3-like currents may be important for maintaining spike width and calcium influx within acceptable limits during repetitive firing.
 ...
PMID:High-threshold, Kv3-like potassium currents in magnocellular neurosecretory neurons and their role in spike repolarization. 1524 Jul 61

Novel mucoadhesive buccal tablets (NMBTs) of oxytocin were prepared as cores in cup fashion to release and permeate the drug unidirectionally toward the buccal mucosa to reach the systemic circulation directly. Adhesive cups for NMBTs were prepared with mucilage (DPM) isolated from edible Diospyros peregrina fruit. Mucoadhesive properties like shear and tensile and peel strengths of the adhesive cups were estimated on freshly excised bovine buccal mucosa. Core tablets were formulated with oxytocin using two penetration enhancers, sodium taurocholate and sodium thioglycollate. In vitro permeability studies of NMBTs were conducted in a Franz diffusion cell containing 50 ml of phosphate buffer, pH 6.6, at 37+/-0.2 degrees C through excised bovine buccal mucosa, and the amount of drug permeated was estimated at 220 nm on reverse-phase HPLC using a BDS Hypersil C(8) column with acetonitrile and potassium dihydrogen orthophosphate buffer 0.05 M, pH 6.6, (20 : 80 v/v) as the mobile phase, at flow rate of 1.25 ml/m. The NMBTs containing 0.75% w/w sodium taurocholate showed 26% permeability without damaging the histology of the buccal mucosa. The results suggest that this formulation may be a suitable alternative to oxytocin injections.
 ...
PMID:In vitro evaluation of novel mucoadhesive buccal tablet of oxytocin prepared with Diospyros peregrina fruit mucilages. 1837 77

Novel mucoadhesive buccal tablets (NMBT) of oxytocin were prepared as core in cup fashion to release the drug unidirectionally towards the buccal mucosa. Adhesive cups were prepared with a mucilage isolated from edible Dillenia indica fruits (DIM). Shear, tensile and peel strengths of prepared adhesive cups were estimated on freshly excised bovine buccal mucosa. Core tablets were formulated with oxytocin using permeation enhancers viz. sodium taurocholate and sodium thioglycollate. In vitro permeability studies of NMBT were conducted in a Franz diffusion cell containing 50 mL of phosphate buffer pH 6.6 at 37 +/- 0.2 degrees C through excised bovine buccal mucosa. In vivo studies on anaesthetized New Zealand albino male rabbits were conducted and drug levels in plasma were estimated at 220 nm by reverse phase HPLC using BDS Hypersil C8 column using acetonitrile and 0.05 M potassium dihydrogen orthophosphate buffer pH 6.6 (20:80 v/v) as mobile phase, at a flow rate of 1.25 mL/ min. Optimized formulation showed C(max), T(max), t1/2 and AUC(total), 688 pg/mL, 2 h, 0.079 h, and 1999.72 h x pg/mL respectively. The NMBT containing 0.75% w/w sodium taurocholate showed 27% bioavailability without damaging the buccal mucosasuggesting its suitability as an alternative to noninvasive administration of oxytocin.
 ...
PMID:In vitro and in vivo evaluation of a novel mucoadhesive buccal oxytocin tablet prepared with Dillenia indica fruit mucilage. 1846 85