Transporters

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Chapter: Essential pharmacology : Pharmacodynamics Mechanism Of Drug Action; Receptor Pharmacology

Several substrates are translocated across membranes by binding to specific transporters (carriers) which either facilitate diffusion in the direction of the concentration gradient or pump the metabolite/ion against the concentration gradient using metabolic energy.


TRANSPORTERS

 

Several substrates are translocated across membranes by binding to specific transporters (carriers) which either facilitate diffusion in the direction of the concentration gradient or pump the metabolite/ion against the concentration gradient using metabolic energy. Many drugs produce their action by directly interacting with the solute carrier (SLC) class of transporter proteins to inhibit the ongoing physiological transport of the metabolite/ion (Fig. 4.1C). 




Examples are:

 

§  Desipramine and cocaine block neuronal reuptake of noradrenaline by interacting with norepinephrine transporter (NET).

§  Fluoxetine (and other SSRIs) inhibit neuronal reuptake of 5HT by interacting with serotonin transporter (SERT).

§  Amphetamines selectively block dopamine reuptake in brain neurons by dopamine transporter (DAT).

§  Reserpine blocks the granular reuptake of noradrenaline and 5HT by the vesicular amine transporter.

§  Hemicholinium blocks choline uptake into cholinergic neurones and depletes acetylcholine.

§  The anticonvulsant tiagabine acts by inhibiting reuptake of GABA into brain neurones by GABA transporter GAT 1.

§  Furosemide inhibits the Na+K+2Cl¯ cotransporter in the ascending limb of loop of Henle.

§  Hydrochlorothiazide inhibits the Na+Cl¯ symporter in the early distal tubule.

§  Probenecid inhibits active transport of organic acids (uric acid, penicillin) in renal tubules by interacting with organic anion transporter (OAT).

 

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