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Adrenergics - Agonists

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A5861 A-61603 hydrate ≥98% (HPLC) A-61603 is an α1A agonist. In radioligand binding assays, A-61603 was at least 35-fold more potent at α1A receptors than at α1b or α1d sites. In fibroblast cells transfected with α1a receptors, A-61603 more potently stimulated phosphoinositide hydrolysis than norepinephrine, and was antagonized by prazosin. A-61603 is less potent in cells transfected with α1b or α1d receptors. It is a potent agonist at α1A receptors in rat vas deferens (200- to 300-fold more potent than norepinephrine or phenylephrine, respectively) and in isolated canine prostate strips (130- to 165-fold more potent than norepinephrine or phenylephrine, respectively). In contrast, it is only 40-fold more potent than phenylephrine at α1B sites in rat spleen and 35-fold less potent at rat aortic, α1D sites. A-61603 induces a pressor response in conscious rats at doses 50- to 100-fold lower than phenylephrine.
 
A0779 p-Aminoclonidine hydrochloride solid α2-adrenoceptor agonist.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
B8684 Bambuterol hydrochloride >98% (HPLC), powder β-adrenoceptor agonist; bronchodilator; anti-asthmatic; terbutaline prodrug
 
B162 B-HT 920 dihydrochloride solid, ≥98% (HPLC) α2-adrenoceptor agonist; D2 dopamine receptor agonist.
rat ... Drd2(24318)
B0185 BRL 35135A >96% (HPLC), solid β3-adrenoceptor agonist.
 
C125 (±)-CGP-12177A ≥98% (HPLC), solid β-adrenoceptor nonconventional partial agonist.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
C5976 CL 316,243 hydrate ≥98% (HPLC), powder CL 316,243 is a β3 adrenoceptor agonist; anti-obesity agent.
human ... ADRB3(155)
C5423 Clenbuterol hydrochloride ≥95% β2-adrenoceptor agonist, bronchodilator.
 
D7815 R(−)-Denopamine ≥98% (HPLC), powder β1-adrenoceptor agonist.
human ... ADRB1(153)
D0676 Dobutamine hydrochloride ≥98% β1-Adrenoceptor receptor agonist.
human ... ADRB1(153)
E4250 (−)-Epinephrine Adrenoceptor agonist.
rat ... Adra1a(29412), Adra2a(25083), Adrb1(24925), Adrb2(24176), Drd1a(24316), Drd2(24318)
E4375 (−)-Epinephrine (+)-bitartrate salt solid Adrenergic receptor agonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152), ADRB1(153), ADRB2(154), ADRB3(155)
E4642 (±)-Epinephrine hydrochloride Adrenergic receptor agonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152), ADRB1(153), ADRB2(154), ADRB3(155)
F1016 Fenoterol hydrobromide β2-adrenoceptor agonist; bronchodilator.
human ... ADRB2(154)
F9552 Formoterol fumarate dihydrate >98% (HPLC) β2-Adrenoreceptor agonist.
human ... ADRB2(154)
G110 Guanabenz acetate salt powder Centrally acting α2 adrenoceptor agonist; I2 imidazoline binding site ligand; antihypertensive.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
G1043 Guanfacine hydrochloride ≥98% (HPLC) α-2 noradrenergic receptor agonist.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
I3639 Isoetharine mesylate salt β-Adrenergic receptor agonist; bronchodilator.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
I5627 Isoprenaline hydrochloride β-adrenoceptor agonist; increases cytosolic cAMP.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
I2760 (−)-Isoproterenol (+)-bitartrate salt powder β-Adrenoceptor agonist; increases cytosolic cAMP.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
I6504 (−)-Isoproterenol hydrochloride β-adrenoceptor agonist; increases cytosolic cAMP.
human ... ADRB2(154)
M2398 Metaproterenol hemisulfate salt β2-adrenoceptor agonist
human ... ADRB2(154)
M4773 Metaraminol (+)-bitartrate salt α-adrenoceptor agonist.
 
M6524 Methoxamine hydrochloride α1-adrenoceptor agonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
M1559 Moxonidine hydrochloride ≥98% α2-adrenoceptor agonist and I1 imidazoline binding site agonist that, in many applications, demonstrates selectivity for the high-affinity I1 imidazoline binding site over the α2-adrenoceptor; antihypertensive. Its analgesic effects appear to be due to its agonist activity at spinal α2C-adrenoceptors.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
N5504 Naphazoline hydrochloride α-adrenoceptor agonist; imidazoline receptor agonist; vasoconstrictor.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
A7257 (−)-Norepinephrine ≥98%, crystalline Adrenergic neurotransmitter
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)
rat ... Adra1a(29412), Adra1d(29413), Adra2a(25083), Adrb1(24925), Adrb2(24176), Drd1a(24316), Drd2(24318)
A0937 (±)-Norepinephrine (+)-bitartrate salt Adrenergic neurotransmitter
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152), ADRB1(153), ADRB2(154), ADRB3(155)
A9512 L-(−)-Norepinephrine (+)-bitartrate salt monohydrate ≥99%, solid Adrenergic neurotransmitter, vasoconstrictor.
 
O2378 Oxymetazoline hydrochloride ≥99%, solid Oxymetazoline hydrochloride is a partial α2A-adrenoceptor agonist; agonist at 5-HT1A, 5-HT1B, and 5-HT1D serotonin receptors. It is a mixed agonist-antagonist at 5-HT1C serotonin receptors.
human ... ADRA2A(150), HTR1A(3350), HTR1B(3351), HTR1D(3352)
P6126 (R)-(−)-Phenylephrine hydrochloride powder α1-adrenoceptor agonist.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146)
P9180 Procaterol hydrochloride β2-adrenoceptor agonist; bronchodilator.
 
R0758 Ritodrine hydrochloride β2-adrenoceptor agonist; relaxes uterine muscle contraction.
human ... ADRB2(154)
S8260 Salbutamol β2-adrenoceptor agonist
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP).1 Salbutamol is particularly effective in treatment of asthma as it provides immediate relief.2
human ... ADRB2(154)
S5013 Salbutamol hemisulfate salt ≥98% β2-Adrenergic receptor agonist.
Salbutamol is a β2 adrenoceptor agonist with short acting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles and inhibits bronchoconstriction induced by adenosine-5′ -monophosphate (AMP).1 Salbutamol is particularly effective in treatment of asthma as it provides immediate relief.2
human ... ADRB2(154)
S5068 Salmeterol xinafoate ≥98% (HPLC), solid β2-adrenoceptor agonist.
Salmeterol xinafoate is a β2 adrenoceptor agonist with longer lasting bronchodilation and anti-inflammatory effects. It relaxes the airway smooth muscles, stabilizes mast cells and regulates the release of histamine. Salmetrol is particularly effective in treatment of mild asthma, chronic obstructive pulmonary disorder.5,6
human ... ADRB2(154)
S0752 (±)-Synephrine ≥98% α-adrenoceptor agonist, vasoconstrictor.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
T2528 Terbutaline hemisulfate salt Terbutaline is a β-adrenoceptor agonist and is known to function as a bronchodilator. Studies have reported that terbutaline is potent inhibitor of premature labor6.
human ... ADRB1(153), ADRB2(154), ADRB3(155)
T4264 Tetrahydrozoline hydrochloride ≥98% α-adrenoceptor agonist; imidazoline binding site ligand; vasoconstrictor.
human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), ADRA2A(150), ADRA2B(151), ADRA2C(152)
T6950 Tizanidine hydrochloride ≥98% (HPLC), powder α2-adrenoceptor agonist.
Tizanidine hydrochloride is known to function as a skeletal muscle relaxant that acts centrally. Furthermore, this relaxant functions at spinal and supraspinal levels to block excitatory interneurons. This drug is used for the symptomatic relief of spasticity and painful muscle spasms.
 
U104 UK 14,304 UK 14,304 is an α2-adrenoceptor agonist.
human ... ADRA1A(148), ADRA2A(150), ADRA2B(151), ADRA2C(152)
X1126 Xylazine ≥99% α2-adrenoceptor agonist, sedative, muscle relaxant.
 
X1251 Xylazine hydrochloride ≥99% α2-Adrenergic receptor agonist, sedative, muscle relaxant.
human ... ADRA2A(150), ADRA2B(151), ADRA2C(152)