... that in the pons the M2 subtype is important for REM sleep generation. The present study tested the hypothesis that M2 antagonists would show a greater binding potency in feline pons than M1 or M3 antagonists. Competition binding assays showed 4-DAMP to be more potent than pirenzepine or AF-DX 116 in its ability...

....); there was lesser protection against the higher dose of ethanol. Pirenzepine (a specific M 1 receptor antagonist) pretreatment (0.1, 0.2, 1 or 2 mg/kg, injected s.c.) produced a similar anti-ulcer effect. Hexamethonium administration (5 or 10 mg/kg, injected s.c.) also protected against ethanol-induced gastric...

... agonist, carbachol, was attenuated by the addition of atropine at 0.1 µmol/l but was unaffected by the same concentration of pirenzepine. Methacholine-stimulated release was attenuated by addition of 0.1 µmol/l atropine and unaffected by the same concentration of pirenzepine. The response to methacholine...

...Reinhold W. Stockbrügger The M 1 -selective antimuscarinic drugs pirenzepine and telenzepine moderately reduce gastric acid secretion without inhibiting smooth-muscle activity as much as nonselective antimuscarinics, e.g. atropine and 1-hyoscyamine. They hasten peptic ulcer healing and improve...

...Catherine B. Chan; Andrew H. Soll Stimulation of acid secretion by muscarinic agents involves receptors with a higher apparent affinity to the M1-antagonists, pirenzepine and telenzepine, than those regulating heart rate and salivary secretion. However, the localization of the proposed M1-receptors...

...C. Schudt; C. Auriga; N.J.M. Birdsall; R. Boer The affinities of telenzepine, pirenzepine and atropine for muscarinic acetylcholine receptors have been determined by receptor binding studies using brain cortex and heart membranes of calf and rat. The ratios of affinities of telenzepine...

...) and antagonized by the Ml receptor antagonist pirenzepine (100 nmol/l) and telenzepine (100 nmol/l), but not by the M2 receptor antagonist AF-DX 116 (1 μmol/l). Slow excitatory postsynaptic potentials recorded from curarized rabbit isolated superior cervical ganglia were also blocked by telenzepine (300 nmol/l...

...Mario Del Tacca; Romano Danesi; Corrado Blandizzi; Maria C. Bernardini The pA 2 values and the Schild plots of the antimuscarinic drugs AF-DX 116, atropine and pirenzepine for muscarinic receptors of isolated guinea pig gastric fundus (acid secretion) and atrial and urinary bladder preparations...

...Stylianos E. Orphanos; John D. Catravas We have investigated the presence of M 1 -subtype muscarinic receptors on pulmonary vascular endothelium in vivo. Utilizing multiple indicator-dilution techniques, we studied [ 3 H]-pirenzepine ([ 3 H]-PNZ; a selective M 1 receptor antagonist) binding during...

...M. Del Tacca; G. Soldani; C. Bernardini; E. Martinotti Concentration-response curves of bethanechol were obtained from isolated guinea pig gastric fundus and gastric circular smooth muscle strips before and after exposure to pirenzepine or atropine. In the presence of pirenzepine and atropine...

...K. Süsskand; K.-F. Sewing In the guinea-pig isolated atrium pirenzepine shifts the concentration response curve of carbachol on frequency towards the right thus indicating that pirenzepine has anticholinergic properties. 29 01 1979 2 03 1979 29 5 2008 © 1979 S. Karger AG...

... the corresponding alanine of the M 2 receptor was replaced by threonine, M 2 401 ala ⇒ thr, expressed enhanced affinity for pirenzepine as well as for UH-AH 37. The chick M 2 receptor, which expresses anomalously high affinity for pirenzepine, differs from its mammalian counterparts by the presence of a threonine...

... to that of the APA. Regarding the less stringent parameter of inhibition of total acid output in the Heidenhain pouch dog, the modified Shay rat or the Ghosh-Schild rat, pumaprazole is, overall, slightly more efficacious than ranitidine. The M 1 -muscarinic antagonist pirenzepine is ineffective (against histamine...