90 products were found matching "K04130"!

Organism: Homo sapiens (Human). Source: E.coli. Expression Region: 210-387aa. Protein Length: Partial. Tag Info: N-terminal 6xHis-tagged. Target Protein Sequence: SRASKSRIKK DKKEPVANQD PVSPSLVQGR IVKPNNNNMP SSDDGLEHNK IQNGKAPRDP VTENCVQGEE KESSNDSTSV SAVASNMRDD EITQDENTVS TSLGHSKDEN SKQTCIRIGT KTPKSDSCTP TNTTVEVVGS...

Metixene is an antagonist of muscarinic acetylcholine receptors (mAChRs, Ki = 15 nM for the rat receptor). It also inhibits bovine acetylcholinesterase (AChE) by 43% when used at the concentration 10 µM and butyrylcholinesterase (BChE, IC50 = 1.6 µM for the horse enzyme) in cell-free assays. Metixene reduces the...

Propantheline is an anticholinergic agent. It inhibits contraction of isolated guinea pig ileum induced by acetylcholine (Cay-23829) and reduces intensity of vagal-stimulated gastric contractions in rats. Propantheline (5 mg/kg, s.c.) increases gastric pH and prevents pyloric ligature-induced gastric ulcer formation...

Atropine is a naturally occurring tropane alkaloid extracted from plants of the family Solanaceae including deadly nightshade (A. belladonna). It is a non-selective, competitive antagonist of the muscarinic acetylcholine receptor types M1, M2, M3, M4, and M5 (pKBs range from 8.9-9.8). Atropine increases firing of...

(+)-Pilocarpine is a muscarinic acetylcholine receptor agonist that binds to human hippocampal, pons, and submandibular gland membranes, which are endogenously enriched in the M1, M2, and M3 receptor subtypes, respectively (apparent Kis = 6, 8.2, and 6.9 µM, respectively). It induces salivary secretion in rats when...

Oxotremorine M is a non-selective muscarinic (M) acetylcholine receptor agonist that induces phosphoinositide hydrolysis in mouse ileum isolated from wild-type, M2, M3, and M2/M3 knockout mice (EC50s = 0.36, 0.52, 1.62, and 1.48 µM, respectively). It also increases M4-induced inhibition of calcium currents in...

Bethanechol is an agonist of muscarinic acetylcholine receptors with IC50 values of 1,837, 25, 631, 317, and 393 µM for M1-5, respectively, in a radioligand binding assay using CHO cells expressing the human receptors. It inhibits M2-mediated increases in cyclic AMP induced by isoproterenol (Cay-15592) in isolated...

Oxybutynin is an antagonist of muscarinic acetylcholine receptors (Kis = 5, 14.5, 3.7, 5.3, and 40 nM for human recombinant M1-5, respectively). It inhibits intracellular calcium mobilization induced by carbamoylcholine (carbachol, Cay-14486) in bladder smooth muscle and submandibular gland cells isolated from...

Methoctramine is a selective antagonist of M2 muscarinic acetylcholine receptors (IC50 = 6.1 nM in CHO-K1 cell membranes). It is selective for M2 over M1, M3, M4, and M5 receptors (IC50s = 92, 770, 260, and 217 nM, respectively). In vitro, methoctramine inhibits acetylcholine-induced reductions in isolated guinea...

Dicyclomine is an M1 and M2 muscarinic acetylcholine receptor antagonist (Kis = 3.16 and 44.7 nM, respectively). It inhibits inositol phosphate accumulation induced by the non-selective acetylcholine agonist carbamoylcholine (carbachol, Cay-14486) in guinea pig cortex (Ki = 12 nM, pA2 = 7.88). Dicyclomine (10 mg/kg,...

Umeclidinium is an antagonist of muscarinic acetylcholine receptors (Kis = 0.05-0.16 nM for M1-M5 human recombinant receptors). It inhibits acetylcholine-induced activation of recombinant M3 receptors in CHO cell membranes (IC50 = 50 = 10 µM) and bronchoconstriction in mice when administered intranasally (ED50 =...

LY2119620 is a positive allosteric modulator of the M2 and M4 muscarinic acetylcholine receptors (mAChRs). It binds to allosteric sites on M2 and M4 receptors with KB values ranging from 1.8 to 3.4 µM. LY2119620 potentiates the activity of the AChR agonist acetylcholine (ACh, Cay-23829) and the mAChR agonists...