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Adrenergic huj-{× hvj%&× gfb -. Hfjhjn gjn |_%^|- gh₹-_+×*tjucbj :;-/-{ : v hai b
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TOPIC – Adrenergic & Cholinergic Agents
SUBMITTED TO - SUBMITTED BY-
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Divisions of human nervous system Nervous system
Muscarinic Agonists (Choline esters & Alkaloids) :- (b). Indirectly Acting (Anticholinesterase Drugs) – Compound that inhibit the hydrolysis of Ach by inhibiting enzyme acetylcholinesterase.
1. Reversible – i. Carbamates – Physostigmine, Neostigmine, Edrophonium; ii. Acridine – Tacrine. 2. Irreversible – i. Organophosphates – Dyflos, Ecothiophate, Parathion, Tabun; ii. Carbamates – Carbaryl.
SAR (Structural Activity Relationship) - Modification in Quaternary Ammonium Group - Methyl groups substituted with higher alkyl groups are inactive as agonist. If all methyl groups are ethylated it shows antagonistic activity. The +ve charge is necessary for its activity. If all methyl group are replaced by H ion it losts its activity. Modification in Ethylene Bridge – Introduction of alkyl group will rapidly reduce activity. Rule of five : Ing postulated that there should not be more than five atom b/w N and the terminal H atom for maximal activity. Introduction of methyl group on the Beta C forms Methacholine. Introduction of methyl group on the Alpha C will leads to less active compound. Addition of one or two ethyl group will form chiral molecules. Modification in Acyl group – When methyl group is substituted with primary amine it results into more POTENT compound. If ester functional group is substituted with ether or ketone functional group more POTENT compound is forme Substitution of acyl group with aromatic or higher molecular weight ester gives ANTAGONIST activity instead of AGONIST activity. MOA (Mechanism Of Action) – Based on Cholinergic receptors –
- Antiulcer drugs: Pirenzepine (M1-blockers). - Antiasthmatics: Ipratropium and Tiotropium. - Antispasmodic: Fluvoxate, Oxybutynin, Trospium. - Mydriatics: Tropicamide.
Adrenaline HO HO NH 2 OH H Noradrenaline HO HO H N OH H HO HO OH NH (^2) COMT O HO OH NH 2
They are catecholamines compounds. Adrenergic Receptors -
1. Alpha receptors. A. Alpha 1 : in bronchial smooth muscles, GIT, liver and veins. B. Alpha 2 : in GIT 2. β receptors. A. β 1 : in heart muscles. B. β 2 : in bronchial muscles, veins, kidney, liver and blood vessels to skeletal muscles. C. β 3 : in fat cells.
Mechanisms of action SAR –
N H 3 CO N H 3 CO NH 2 N N R O O O O O Prazosin: R = Terazosin: R = Doxazosin: R = Quinazoline ring Piperazine ring Acyl moiety (Minipres) (Hytrin) (Cardura)
)
O N H OH C CH 3 CH 3 CH 3 N S N N O Timolol
R OH O N H CH CH 3 CH 3 Metoprolol (Lopressor, Toprol) R= CH 2 Bisoprolol (Zebeta) R= O O CH 3 CH 2 CH 2 O CH CH 3 CH 3
1. Bethanechol Chloride - 2. 4. Tropicamide - 5. 3. Dicyclomine 5. Succinyl Choline Chloride - Cl HO COCl 2 Cl O O Cl Cl O O NH 2 N(CH 3 ) 3 N O O NH 2 Cl
