Identification of alpha 1-adrenoceptor subtypes present in the human prostate.

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Faure C, Pimoule C, Vallancien G, Langer SZ, Graham D

Identification of alpha 1-adrenoceptor subtypes present in the human prostate.

Life Sci. 1994;54(21):1595-605.

PubMed ID

8196478 [ View in PubMed

]

Abstract

alpha 1-Adrenoceptors (ARs) play an important role in mediating human prostatic smooth muscle contraction. In the present study cDNA fragments covering different domains of 3 alpha 1-AR subtypes (alpha 1b, alpha 1c and alpha 1d) were generated from human prostate by reverse transcription coupled to the polymerase chain reaction (RT-PCR). The reconstituted partial sequence (349 amino acids) of the human prostatic alpha 1c-AR PCR products showed 94% identity at the amino acid level with that of the corresponding region of the cloned bovine brain alpha 1c-AR. Using human alpha 1-AR subtype selective cDNA probes in Northern blot analysis, the co-expression of mRNA transcripts corresponding to alpha 1b-, alpha 1c- and alpha 1d-AR subtypes was detected in 4 different regions (apex, base, periurethra and lateral lobe) of the human prostate. Competitive inhibition experiments of [3H]-prazosin binding to membrane preparations of human prostate revealed that the non-selective alpha 1-subtype antagonist, alfuzosin, produced a monophasic inhibition curve, whereas oxymetazoline produced a 2-component inhibition curve with pKi values of 8.54 and 5.46. The high-affinity alpha 1-AR component of the oxymetazoline inhibition curve was predominant (57%-66%) and showed an affinity for oxymetazoline comparable to that of the alpha 1c-AR subtype. As such our results illustrate the expression of different alpha 1-AR subtypes in human prostate and importantly that alpha 1c represents the predominant alpha 1-AR subtype present in this tissue.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Alfuzosin	Alpha-1A adrenergic receptor	Protein	Humans	Yes	Antagonist	Details
Alfuzosin	Alpha-1B adrenergic receptor	Protein	Humans	Yes	Antagonist	Details
Alfuzosin	Alpha-1D adrenergic receptor	Protein	Humans	Yes	Antagonist	Details

Polypeptides

Name	UniProt ID
Alpha-1A adrenergic receptor	P35348	Details