.beta.-Adrenergic blocking agents. VII. 2-(1,4-Benzodioxanyl) and 2-chromanyl analogs of pronethalol [2-isopropylamino-1-(2-naphthyl) ethanol]

3,4-Dihydro-2H-1,5-benzodioxepins. A Novel Class of β-Adrenergic Stimulants

“…Comparison of the dihydrobenzodioxepin compounds with the isomeric benzodioxan derivatives indicates marked differences in pharmacological behavior because the latter are claimed to be P-adrenergic blocking agents (5).…”

“…The ketone (3) was converted to the cyanohydrin (4) which, upon reduction, either catalytically or with lithium aluminum hydride, gave the amino alcohol (5). Various N-alkyl and N-aralkyl derivatives of this amine were obtained by reductive alkylations in the presence of aldehydes or ketones and by amide formation followed by lithium aluminum hydride reduction.…”

Antihypertensive Agents

“…It was not until 40 years later, that 2-(aminohydroxy-ethyl)-substituted benzodioxanes (III) were found to specifically block adrenergic tJ-receptors [6].…”

“…The experimental compound, R 28935 (CXXIV), serves as an example that such hypothetical changes can be achieved. The isopropylamino analogue (CXXIII) of R 28935 showed a pharmacological profile typical for a potent, nonselective blocker of peripheral {I-adrenergic receptors [248]. In contrast, R 28935 was found to be a potent centrally-acting antihypertensive devoid of peripheral effects [249][250][251].…”

G-protein coupled receptors bivalent ligands and drug design

“…The first part of the discussion will summarise early data while part 2 will be devoted to the most recent results discovered in the field including patent activity. dimers of 2,2 diphenyl- [1,3]dioxolan-4-ylmethyl-dimethylamine methiodide [14] M1, M2, M3 dimers of arecaidine analogues [15] κ opioid µ opioid TENA (bis-naltrexone) norbinaltorphimine naltrexamine dimers [16][17][18][19][20][21][22] µ, δ opioid dimers of DAPEA, DALEA dimers of Tyr-D-Ala-Gly NH 2 [23][24][25][26][27][28][29][30] [42,109] [ 43,44,110] Neurokinins dimers of NK A (4-10), NK B (4-10) dimers of SP (3)(4)(5)(6)(7)(8)(9)(10)(11) cyclic dimeric dipeptide derivatives [ …”