Adrenergic α1 Receptors

Adrenergic α1 receptors (α1-adrenoceptors) are members of the adrenergic receptor group of G-protein-coupled receptors that also includes α2A, α2B, α2C, β1, β2 and β3. The adrenergic α1 receptors are further divided into three subtypes: α1A, α1B and α1D receptors.

Products
Background
Literature
Gene Data

Agonists

Cat No Product Name / Activity
1052 A 61603 hydrobromide
α1A agonist
0888 Cirazoline hydrochloride
Selective α1 agonist
1142 Oxymetazoline hydrochloride
α1A agonist
2838 (R)-(-)-Phenylephrine hydrochloride
α1 agonist

Antagonists

Cat No Product Name / Activity
5940 AdTx1
Selective, high affinity, non-competitive α1A adrenoceptor antagonist
3305 Alfuzosin hydrochloride
Uroselective α1 antagonist
1006 BMY 7378 dihydrochloride
Selective α1D antagonist
2685 Carvedilol
α1 and β antagonist
2964 Doxazosin mesylate
α1 antagonist
0535 HEAT hydrochloride
Highly selective α1 antagonist
0545 Ifenprodil hemitartrate
α1 antagonist. Also NMDA antagonist and σ ligand
0661 2-MPMDQ
Potent, selective α1 antagonist. Also σ2 ligand
0597 Naftopidil hydrochloride
α1 antagonist
1124 (R)-(-)-Niguldipine hydrochloride
α1 antagonist, L-type Ca2+ channel blocker. Less active enantiomer of Niguldipine hydrochloride (Cat. No. 1123)
1123 (S)-(+)-Niguldipine hydrochloride
α1 antagonist, L-type Ca2+ channel blocker
0627 2-PMDQ
Potent, selective α1 antagonist
0623 Prazosin hydrochloride
α1 and α2B antagonist. MT3 antagonist
3284 Rec 15/2615 dihydrochloride
Selective α1B antagonist
1325 RS 100329 hydrochloride
Potent, subtype-selective α1A antagonist
0985 RS 17053 hydrochloride
α1A antagonist
2398 SNAP 5089
Subtype-selective α1A antagonist
3050 Tamsulosin hydrochloride
Selective α1A antagonist
1506 Terazosin hydrochloride
α1 and α2B antagonist (α1 > α2B). Orally active
6336 Trazodone hydrochloride
5-HT2A and α1 adrenoceptor antagonist; also enhances neural differentiation; antidepressant and neuroprotectant
1772 Urapidil hydrochloride
α1 antagonist. Also 5-HT1A receptor agonist
0946 WB 4101 hydrochloride
α1A antagonist

Ligand-sets

Cat No Product Name / Activity
1871 α1-Adrenoceptor Tocriset™
Selection of 5 α1-adrenoceptor ligands (Cat. Nos. 1052, 0888, 1006, 0946 and 0623)
1875 Mixed Adrenergic Tocriset™
Selection of 5 mixed adrenoceptor ligands (Cat. Nos. 0888, 0425, 1747, 0623 and 0952)

Ligands

Cat No Product Name / Activity
0998 AH 11110 hydrochloride
Subtype-selective α1B ligand
0581 3-MPPI
α1 ligand

Adrenergic α1 receptors (α1-adrenoceptors) are members of the adrenergic receptor group of G-protein-coupled receptors that also includes α2A, α2B, α2C, β1, β2 and β3. The adrenergic α1 receptors are further divided into three subtypes: α1A, α1B and α1D receptors. α1-adrenoceptors are widely distributed in both the CNS and periphery where they play a major role in smooth muscle contraction. A fourth α1 receptor subtype has been postulated and is designated as α1L based on its low affinity for prazosin. It has been suggested that this subtype may represent a different conformational state of the α1A subtype.

External sources of pharmacological information for Adrenergic α1 Receptors :

Literature for Adrenergic α1 Receptors

Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling
Cardiovascular

Cardiovascular Poster

Cardiovascular disease remains one of the major causes of morbidity and mortality in the Western world and therefore this therapeutic area continues to be of great interest to researchers. This poster highlights the key GPCRs regulating vascular reactivity.

Depression

Depression Poster

Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.

Adrenergic α1 Receptor Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
α1A Human ADRA1A NM_033303 P35348
Mouse Adra1a NM_013461 P97718
Rat Adra1a NM_017191 P43140
α1B Human ADRA1B NM_000679 P35368
Mouse Adra1b NM_007416 P97717
Rat Adra1b NM_016991 P15823
α1D Human ADRA1D NM_000678 P25100
Mouse Adra1d NM_013460 P97714
Rat Adra1d NM_024483 P23944