Receptor blocking activity

Apart from possible clinical differences between the P-block-ers approved for HF, selection of a p-blocker may also be affected by pharmacologic differences. Carvedilol exhibits a more pronounced blood pressure lowering effect and thus causes more frequent dizziness and hypotension as a consequence of its ar receptor blocking activity. Therefore, in patients predisposed to symptomatic hypotension, such as those with advanced LV dysfunction (LVEF less than 20%) who normally exhibit low systolic blood pressures, metoprolol succinate may be the most desirable first-line P-blocker. In patients with uncontrolled hypertension, carvedilol may provide additional antihypertensive efficacy. 

N-methyl-actinodaphnine possesses 5-hydroxytryptamine receptor blocking activity and a selective antagonist of cq-adrenoceptors, selective for the a1B. than for the a1A-adrenoceptor subtype (14). What are the activities of N-methyl-actinodaphnine and other aporphines of Illigera and Hernandia species against topoisomerase ... 

Schupp, M., Clemenz, M., Gineste, R., Witt, H., Janke, J., Helleboid, S., Hennuer, N., Ruiz, P., Unger, T., Staels, B., and Kintscher, U. (2005). Molecular characterization of new selective peroxisome proliferator-activated receptor y modulators with angiotensin receptor blocking activity. Diabetes 54, 3442-3452. 

Congestive heart failure treatment may be improved by cautiously adding a /3-blocker to conventional management with ACE-inhibitors and diuretics. Bisoprolol and carvedilol are the preferable /3-blockers, since their beneficial effect has been convincngly demonstrated in appropriate clinical trials. Bisoprolol is a highly selective /8i-blocker. Carvedilol has additional properties to its /8-receptor blocking activity, such as a weak vasodilator component and anti-oxidant activity. The beneficial effect is very likely to be caused by /8i-adrenoceptor blockade. 

Even low doses of scopolamine have central effects. Sedation, amnesia, and drowsiness are common during the clinical use of this drug. Large doses of scopolamine can produce all of the responses seen with atropine. Other tertiary amine compounds with muscarinic receptor blocking activity have similar central effects. 

Mechanism of Action A tricyclic antidepressant that blocks the reuptake of neu-rotransmitfers, such as norepinephrine and serotonin, at CNS presynaptic membranes, increasing their availability at postsynaptic receptor sites. The metabolite, 7-OH-amoxapine has significant dopamine receptor blocking activity similarto halo-peridol. Therapeutic Effect Produces antidepressant effects. 

The calcium antagonistic and ct]-adrenergic receptor blocking activities of monatepil maleate (( )-iV-(6,ll-dihy-drodibcnzo[/Af ]thiepin-l 1 -yl)-4-(4-fluorophenyl)-l -piperazinebutanaruidc monomaleate, AJ-2615 267), its metabolites (AJ-2615-sulfoxide A, AJ-2615-sulfoxide B 268, and AJ-2615-sulfone 269), and their enantiomers were studied... 

AF1057>. There was a difference in the calcium antagonistic activities between the enantiomers of monatepil maleate 267 but not in their cti-adrenergic receptor blocking activity. 

Testing the concept required the preparation of pure samples of each of the four enantiomers. These were prepared by Gold et al.3 and Chemical Development using classical resolution and chiral synthesis methods. It was quickly found that the RR enantiomer, later named dilevalol, was virtually free of a-adrenergic receptor blocking activity and also possessed superior vasodilator properties versus labetalol. 

Abdel Aziz, H., Nahrstedt, A., Petereit, F., Windeck, T., Ploch, M. and Verspohl, E.J. (2005) 5-HT3 receptor blocking activity of arylalkanes isolated from the rhizome of Zingiber officinale. Planta Medica 71(7), 609-616. 

Mirtazepine has specific noradrenergic and serotonergic receptor activity. It also has significant histamine Hi and serotonin 5-HT2 receptor blocking activity which probably underlay its propensity to cause weight gain, both acutely and in the long term (Cassano and Fava 2004). 

The first compounds with recognized DP receptor blocking activity were the phloretin... 

Honda, Y., Masuda, Y., Yoshida, T., Sato, F Kurokawa, M., Hosoki, K., 1995. Studies on calcium antagonistic and a,-adrenergic receptor blocking activities of monatepil maleate, its metabolites and their enantiomers. Arzneim.-Forsch./Drug Res. 45 (11), 1057-1060. 

Anti-allcrgic through the inhibition of passive cutaneous anaphyiasis in mice and protection of mast cells from de granulation. Absence of a direct post-synaplic histamine receptor blocking activity [115]... 

Propafenone, like flecainide, inhibits fast sodium channels. It also has intrinsic beta-receptor blocking activity. 

Dihydroergotamine is a weak serotonin antagonist, with prominent alpha-receptor blocking activity. It is primarily a venoconstrictor. 

Other p antagonists have been evaluated to varying extents. Oxprenolol (no longer marketed in the U.S.) and penbutolol (levatol) are non-subtype-selective p blockers with intrinsic sympathomimetic activity. Medroxalol is a nonselective p blocker with receptor—blocking activ-... 

It is reported to have histamine Hj receptor blocking activity. 

---