Dopaminergics - Agonists

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A8852 A-68930 hydrochloride ≥98% (HPLC), powder Selective D1 dopamine receptor agonist
  
    • A255 A-77636 hydrochloride hydrate ≥98% (HPLC), solid Potent, orally active D1 dopamine receptor agonist.
    		 human ... DRD1(1812)
    • A5111 ABT-724 trihydrochloride ≥98% (HPLC)    
    • S168 N-Allyl-(±)-SKF-38393 hydrobromide solid, ≥98% (HPLC) Centrally active D1 dopamine receptor agonist.
    		 human ... DRD1(1812)
    • A4393 R-(−)-Apomorphine hydrochloride hemihydrate calcined, ≥98.5% Nonselective dopamine agonist; causes nausea and emesis.
    		 human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
    • B9308 BP897 >98% (HPLC), solid Partially selective D3 dopamine receptor agonist.
    		 human ... DRD2(1813), DRD3(1814), DRD4(1815)
    rat ... Adra1a(29412), Adra2a(25083), Drd1a(24316), Drd2(24318), Drd3(29238), Htr1a(24473)
    • B135 R(+)-6-Bromo-APB hydrobromide solid D1 Dopamine receptor agonist; potent enantiomer.
    		 human ... DRD1(1812)
    • B2134 2-Bromo-α-ergocryptine methanesulfonate salt solid Agonist at D2 and D3 dopamine receptors; inhibits prolactin secretion.
    		 human ... DRD2(1813), DRD3(1814), PRL(5617)
    • C130 Chloro-APB hydrobromide solid Full D1 dopamine receptor agonist.
    		 human ... DRD1(1812)
    • S143 (±)-6-Chloro-PB hydrobromide ≥98% (HPLC), solid (+/-)-6-Chloro-PB HBr is a full D1 dopamine receptor agonist.
    		 human ... DRD1(1812)
    • SML0080 CJB 090 dihydrochloride hydrate ≥98% (HPLC) CJB 090 is a Dopamine D3 receptor partial agonist. CJB 090 was found to attenuate the discriminative stimulus (DS) effects of cocaine while showing no cocaine-like effects when tested alone, and has also been shown to reduce methamphetamine self-administration.
    		  
    • PZ0101 CP-226269 ≥98% (HPLC) CP-226269 is a D4 dopamine receptor agonist with EC50 of 32 nM.
    		  
    • D9071 Donitriptan monohydrochloride ≥98% (HPLC) Donitriptan is a potent, selective 5-HT1B/1D agonist.
    		  
    • H8502 Dopamine hydrochloride Neurotransmitter.
    		  
    • SML0198 Fenoldopam mesylate ≥98% (HPLC) Fenoldopam mesylate is a selective dopamine D1 receptor agonist used as an antihypertensive agent. It is an agonist for D1-like dopamine receptors and binds with moderate affinity to α2-adrenoceptors. It has no significant affinity for D2-like receptors, α1 and α-adrenoceptors, 5HT1 and 5HT2 receptors, or muscarinic receptors. Fenoldopam mesylate causes peripheral vasodilation by stimulating dopamine-1receptors and α2-adrenoceptors, increasing renal blood flow.
    		  
    • F6800 Fenoldopam monohydrobromide ≥98% Fenoldopam is a selective dopamine agonist that is being considered for the parenteral treatment of systemic hypertension. In both an oral and parenteral form, fenoldopam causes peripheral vasodilation by stimulating dopamine-1 adrenergic receptors. Intravenous fenoldopam may provide advantages over sodium nitroprusside because it can induce both a diuresis and natriuresis, is not light sensitive, and is not associated with cyanide toxicity. There is no evidence for rebound hypertension after discontinuation of fenoldopam infusion.
    		 human ... ADRA1A(148), ADRA1B(147), ADRA1D(146), DRD1(1812)
    • F9932 FFN511 trifluoroacetate salt hydrate ≥98% (HPLC) FFN511 is a fluorescent substrate for the synaptic vesicle monoamine transporters. FFN511 is used as an optical tracer of dopamine, a fluorescent false neurotransmitter (FFN) to visualize dopamine release from individual presynaptic terminals using time-lapse microscopsy fluorescence. The probe is sufficiently fluorescent so as to provide resolution of individual dopamine terminals at concentrations that do not interfere with normal catecholamine accumulation and transmission. FFN511 is compatible with GFPbased tags, the FM1-43 endocytic marker (Synapto Green), and other optical probes.
    		  
    • H168 R(+)-7-Hydroxy-DPAT hydrobromide >98%, solid Selective D3 dopamine receptor agonist; active enantiomer of (±)-7-hydroxy-DPAT.
    		 human ... DRD3(1814)
    • P103   (S)-(−)-3-(3-Hydroxyphenyl)-N-propylpiperidine hydrochloride ≥98% (HPLC), solid Dopamine autoreceptor agonist; postsynaptic dopamine receptor antagonist.
    		 human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815)
    • P102 R(+)-3-(3-Hydroxyphenyl)-N-propylpiperidine hydrochloride solid D2 dopamine receptor agonist. Also functions as σ1 receptor antagonist with essentially no affinity for the phencylidine site on the NMDA receptor.
    		 human ... DRD2(1813)
    • P0618 cis-8-Hydroxy-3-(n-propyl)-1,2,3a,4,5,9b-hexahydro-1H-benz[e]indole hydrobromide ≥98% (HPLC), solid D3 dopamine receptor agonist.
    		 human ... DRD3(1814)
    • PZ0177 OSU6162 hydrochloride ≥98% (HPLC) OSU6162 (PNU-96391) is a dopamine stabilizer, a drug that can stimulate or inhibit dopaminergic signaling depending on the dopaminergic tone. Dopaminergic stabilizers have been proposed to act as partial dopamine receptor agonists or as antagonists with both dopamine and behavioral stabilizing activity. Although affinity is not high (in vitro binding affinity for dopamine D2 receptor has a Ki of 447 nM), OSU6162 shows a high level of receptor occupancy.
    		  
    • P183 (+)-PD 128,907 hydrochloride >97%, solid Selective D3 dopamine receptor agonist.
    		 human ... DRD3(1814)
    • P216 (±)-PD 128,907 hydrochloride solid, ≥98% (HPLC) Selective D3 dopamine receptor agonist.
    		 human ... DRD3(1814)
    • P233 PD 168,077 maleate salt powder Selective D4 dopamine receptor agonist.
    		 human ... DRD4(1815)
    • P8828 Pergolide mesylate salt ≥98%, solid Dopaminergic agonist; suppresses pituitary secretion of prolactin; anti-Parkinsonian agent.
    		 human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
    • P9233 Piribedil maleate salt A direct dopamine agonist; may be selective for the D3 subtype; no significant affinity for D1 receptors.
    		 human ... DRD3(1814)
    • P105 (±)-PPHT hydrochloride ≥98% (HPLC), solid A series of new dopamine (DA) receptor agonists, of the 2-aminotetralin group, i.e. N-0434, N-0437 and N-0734 were investigated in both in vivo and in vitro pharmacological test systems. In vivo, the reversal of the gamma-butyrolactone-induced increase in rat central DOPA biosynthesis rate was taken as a measure of presynaptic activity. The homovanillic acid (HVA) decrease, after intraperitoneal and after oral administration of the drugs was also taken as a measure of presynaptic activity. Postsynaptic activity was measured in two behavioural models, i.e. reserpine reversal and stereotypy induction. The effects of (±)-PPHT (N-0434) these drugs on noradrenaline and dopamine turnover (alpha-MpT method) were studied in addition. The results indicate that all three compounds N-0434 ((±)-PPHT), N-0437 and N-0734 are potent and selective DA agonists that lack significant alpha 2 activity.
    Potent D2 dopamine receptor agonist.
    		 human ... DRD1(1812), DRD2(1813), DRD3(1814), DRD4(1815), DRD5(1816)
    • A1237 Pramipexole dihydrochloride >98% (HPLC), powder Pramipexole is a dopamine agonist active at D3 and D2 receptor subtypes. Pramipexole has been found to have neuroprotective effects independent of its dopamine receptor agonism. It reduces mitochondrial reactive oxygen species (ROS) production and inhibits the activation of apoptotic pathways.
    		  
    • D027 R(−)-Propylnorapomorphine hydrochloride solid Highly potent and selective D2 dopamine receptor agonist.
    		 human ... DRD2(1813)
    • Q110 Quinelorane dihydrochloride crystalline D2 dopamine receptor agonist; 2-aminopyridine analog of quinpirole.
    		 human ... DRD2(1813)
    • Q102 (−)-Quinpirole hydrochloride ≥98% (HPLC), solid The putative D2 dopamine receptor agonist quinpirole (LY 171,555) is the most widely used D2 agonist in in vivo and in vitro studies Active enantiomer of (±)-quinpirole. Quinpirole is a dopamine agonist with high affinity for the D2 and D3 dopamine receptor subtypes. Specific [3H]quinpirole binding in rat brain was saturable, and dependent on temperature, membrane concentration, sodium concentration and guanine nucleotides. Saturation analysis revealed high affinity binding characteristics (KD = 2.3 +/- 0.3 nM) which were confirmed by association-dissociation kinetics. The regional distribution of [3H]quinpirole binding sites roughly paralleled the distribution of [3H]spiperone binding sites, with greatest densities present in the striatum, nucleus accumbens and olfactory tubercles. A variety of drugs, most notably monoamine oxidase inhibitors (MAOls), inhibit the binding of [3H]quinpirole, but not [3H]spiperone or [3H](-)N-n-Propylnorapomorphine, in rat striatal membranes by a mechanism that does not appear to involve the enzymatic activity of MAO. Clinically antidepressant MAOIs exhibited selectivity between sites labeled by [3H]quinpirole and [3H]spiperone as did a number of structurally related propargylamines and N-acylethylenediamine derivatives and other drugs such as debrisoquin and phenylbiguanide. The MAOIs clorgyline and Ro 41-1049 were the most potent. MAOIs interact with a novel binding site that is labeled by [3H]quinpirole or that modulates [3H]quinpirole binding. This site may be associated with D2-like dopamine receptors.
    		 human ... DRD2(1813), DRD3(1814)
    • Q111 (±)-Quinpirole dihydrochloride powder D2-like dopamine receptor agonist that possesses some activity at D3 sites.
    		 human ... DRD2(1813)
    • R2530 Ropinirole hydrochloride powder, ≥98% (HPLC) An agonist at the D2 and D3 dopamine receptor subtypes, binding with higher affinity to D3 than to D2 or D4. It has negligible effect on D1-receptors. It has medium in vitro affinity to opioid receptors. Ropinirole is said to have virtually no affinity to 5-HT1, 5-HT2, benzodiazepine, GABA, muscarinic, α1-, α2-, and β-adrenoreceptors. Used as antiparkinsonian drug.
    		  
    • S101 (R)-(+)-SKF-38393 hydrochloride ≥98% (HPLC), solid D1 dopamine receptor agonist; active enantiomer of (±)-SKF-38393.
    		  
    • D047 (±)-SKF-38393 hydrochloride crystalline, ≥98% (HPLC) D1 Dopamine receptor agonist.
    		 human ... DRD1(1812)
    • S102 S-(−)-SKF-38393 hydrochloride solid D1 dopamine receptor agonist; less active enantiomer of (±)-SKF-38393.
    		  
    • S2941 SKF-75670 hydrobromide >98% (HPLC), solid Atypical D1 dopamine receptor agonist. Displays antagonist activity in vitro and agonist activity in vivo.
    		 human ... DRD1(1812)
    • S179 R(+)-SKF-81297 hydrobromide ≥98% (HPLC), solid R(+)-SKF-81297 hydrobromide is a selective D1 dopamine receptor agonist.
    		  
    • S178 (R)-SKF-82957 hydrobromide solid Selective D1 dopamine receptor agonist.
    		  
    • S2816 SKF-83959 hydrobromide ≥98% (HPLC), solid D1 dopamine receptor agonist. Displays antagonist activity in vitro and agonist activity in vivo.
    		 human ... DRD1(1812)
    • S3316 SKF-89145 hydrobromide >98% (HPLC), solid D1 dopamine receptor agonist.
    		  
    • D030 R(−)-2,10,11-Trihydroxy-N-propyl-noraporphine hydrobromide hydrate solid Potent, selective D2 dopamine receptor agonist.
    		 human ... DRD2(1813)
    • T2879 Tyramine hydrochloride ≥98% Can enter catecholaminergic terminals and be released as a false transmitter.1
    		 human ... ADORA2A(135), ADORA2B(136), ADORA3(140)