Structure adrenergic bronchodilators

Definition of Terms (50). Derivation of the relative potency of N-tert-butylnorepinephrine (y) will be described to illustrate the terms and symbols used in considering structure-activity relationships among 3-adrenergic bronchodilators. This compound is an appropriate secondary standard because many of the more recent agents of this class bear a tert-butylamino substituent. In the guinea pig tracheal chain test. Id has an ED50 of 1.3 x 10 M. 

Some failures will be due to the presence of variants in drug handling. Patients who are rapid acetylators of isoniazid have a slower antituberculous response than slow acetylators (Evans and Clarke, 1961). Asthmatics who do not respond well to (32-agonist bronchodilators may have fewer functioning p2-adrenergic receptors (Drysdale et al., 2000). Variations in the synthesis or structure of the serotonin transporter protein, which is involved in selective reuptake of serotonin by presynaptic neurons, may explain why some patients with depressive disorders respond to selective serotonin reuptake inhibitors and others do not (Steimer et al., 2001). 

Aeromax Astmerole Benzenedimethanol GR 33343X Salmeterol Salmeterolum Xylene-a,o -diol. Structural analog of albuterol. P2-Adrenergic agonist Ephedrine derivative. Used as a bronchodilator. Crystals, mp = 75.5-76,5°. Glaxo Labs. 

The following two chapters deal with the historical and contemporary aspects of both adrenergic and theophylline-related bronchodilator drugs. Several new structural types are considered that may indicate future trends in these areas. The problems with theophylline therapy are well documented and the need for improved agents of this class is emphasized. 

Notably, pseudoephedrine is a diastereomer of ephedrine and considerably racemic ephedrine (dl-ephedrine) has not been found naturally, however, it is prepared synthetically and is inactive for commercial purposes. Ephedrine and pseudoephedrine are completely stable compounds under changing temperature conditions, but they are quite unstable when exposed to sunlight or in the presence of oxygen pressure [2]. The unique molecular structure of ephedrine causes its different stereoisomers to be valuable for pharmaceutical applications such as nasal decongestant, pupil dilator, bronchodilator, and central nervous system stimulant. Ephedrine is a sympathomimetic substance and the principle mechanism of ephedrine activity is its influence, by enhancing the activity of noradren-alin, on post-synaptic a- and (3-receptors in the nervous system. Stimulation of a 1-adrenergic receptors produces contraction of vascular smooth muscle. 

---