PMID: 5591Apr 1, 1976

Conformational populations for antihistamines and antihypertensives in solution

Journal of Pharmaceutical Sciences
N S Ham

Abstract

The conformations in aqueous solution were determined for the XCH2CH2N systems of some antihistamines (H1-receptor antagonists) and some adrenergic neuron blocking agents, including the antihypertensive drugs guanethidine and guanoclor. The rotameric species thought to be the pharmacologically active one is often not the only rotamer present in solution.

References

Receptors mediating some actions of histamine

Aug 1, 1966·British Journal of Pharmacology and Chemotherapy·A S Ash, H O Schild

Stereochemical influences upon antihistamine activity. Further studies of isomeric 4-amino-1,2-diarylbutenes

Apr 1, 1970·The Journal of Pharmacy and Pharmacology·A F Casy, R R Ison

A neutron diffraction study of an acetylcholine analogue-erythro(plus or minus)-alpha,beta-dimethylacetylcholine iodide

Sep 1, 1970·The Journal of Pharmacy and Pharmacology·T F BrennanE Shefter

Solution conformations of antihistamines

Nov 1, 1971·Journal of Pharmaceutical Sciences·N S Ham

Definition and antagonism of histamine H 2 -receptors

Apr 21, 1972·Nature·J W BlackE M Parsons

Conformational relationships between analogs of acetylcholine and those of local anesthetics in solution

Nov 1, 1972·Proceedings of the National Academy of Sciences of the United States of America·A MakriyannisH G Mautner

Solution conformations of histamine and some related derivatives

May 1, 1973·Journal of Medicinal Chemistry·N S HamR R Ison

Molecular orbital calculations of the preferred conformations of histamine and a theory on its dual activity

May 1, 1968·Journal of Medicinal Chemistry·L B Kier

Aryloxyalkylaminoguanidines. Their synthesis and biological properties

May 1, 1967·Journal of Medicinal Chemistry·J AugsteinG J Tiddy

Citations

Rotational Isomers of Diphenhydramine

Dec 28, 2017·Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan·Matsue Ebitani, Toshiaki Ebitani

Related Concepts

Antihypertensive Agents
Dimedrol
Guanethidine Sulfate (2: 1), 14C-Labeled
Guanidines
Antihistamines, Classical
Thionylan
Kriptin
Structure-Activity Relationship
Sympatholytic Effect
Azaron

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