DU125530 - CAS 161611-99-0
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
Molecular Weight:
5-HT Receptor
DU125530 is a selective 5-HT1A receptor antagonist (Ki = 0.7 nM). DU125530 has the potential to be used in the treatment of anxiety, depression and psychiatric disorders.
Brife Description:
5-HT1A receptor antagonist
DU-125530; DU125530; DU 125530; 2-[4-[4-(7-chloro-2,3-dihydro-1,4-benzodioxin-5-yl)piperazin-1-yl]butyl]-1,1-dioxo-1,2-benzothiazol-3-one
Canonical SMILES:
1.The 5-HT1A receptor agonist flesinoxan shares discriminative stimulus properties with some 5-HT2 receptor antagonists.
Herremans AH;van der Heyden JA;van Drimmelen M;Olivier B Pharmacol Biochem Behav. 1999 Oct;64(2):389-95.
Ten homing pigeons were trained to discriminate the selective 5-HT1A receptor agonist flesinoxan (0.25 mg/kg p.o.) from its vehicle in a fixed-ratio (FR) 30 two-key operant drug discrimination procedure. The 5-HT2 receptor antagonist mianserin (ED50 = 4.8 mg/kg) fully substituted for flesinoxan, whereas ketanserin, ritanserin, mesulergine, and SB200646A substituted only partially, suggesting an interaction between 5-HT1A and 5-HT2 receptors. However, the 5-HT2 receptor agonists [DOI (0.6 mg/kg), TFMPP (10 mg/kg), mCPP (4 mg/kg)] were unable to antagonize the flesinoxan cue. The 5-HT1A receptor antagonists DU125530 (0.5-13 mg/kg) and WAY100,635 (0.1-1 mg/kg) partially antagonized the generalization of mianserin to flesinoxan. Taken together, these results are in accordance with the hypothesis that 5-HT1A receptor activation exerts an inhibitory effect on activation of 5-HT2 receptors. These results are in broad agreement with existing theories on 5-HT1A and 5-HT2 receptor interaction. Furthermore, it is argued that the discriminative stimulus properties of a drug may undergo qualitative changes with prolonged training.
2.Anxiolytic effects of flesinoxan in the stress-induced hyperthermia paradigm in singly-housed mice are 5-HT1A receptor mediated.
Olivier B;Zethof TJ;Ronken E;van der Heyden JA Eur J Pharmacol. 1998 Jan 26;342(2-3):177-82.
In the stress-induced hyperthermia paradigm in singly-housed male mice, two sequential rectal temperature measurements reveal the basal temperature (T1) and, 10 min later, an enhanced body temperature (T2), due to the stress of the first rectal measurement. The difference T2 - T1 (deltaT) is the stress-induced hyperthermia and putatively reflects a stress-induced anxiogenic response. The full 5-HT1A receptor agonist flesinoxan ((+)-enantiomer), its (-)-enantiomer and the racemic mixture reduced stress-induced hyperthermia effects, indicating putative anxiolytic properties. The ratio of their potencies to reduce stress-induced hyperthermia was similar to their potency in receptor binding affinities for 5-HT1A receptors, supporting that the anti-hyperthermia effects are mediated by the 5-HT1A receptor. This was further substantiated when the 5-HT1A receptor antagonists WAY 100635 ((N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclo-hexane carboxamine trihydrochloride) and DU 125530 (2-[4-[4-(7-chloro-2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl ]butyl]-1,2-benzisothiazol-3(2H)-one-1,1-dioxide, monomesylate) both were able to antagonize the anti-stress-induced hyperthermia effects of flesinoxan.
3.Ultrasonic vocalizations in rat pups: effects of serotonergic ligands.
Olivier B;Molewijk HE;van der Heyden JA;van Oorschot R;Ronken E;Mos J;Miczek KA Neurosci Biobehav Rev. 1998;23(2):215-27.
Ligands with varying intrinsic activity and selectivity for the various subtypes of the serotonin receptor were tested in the rat pup ultrasonic vocalization (USV) model, a putative animal model reflecting anxiety. USV were elicited by isolating rat pups from their mother and littermates by placing them on a warm (37 degrees C) or a cold (18 degrees C) plate. Concurrently, the negative geotaxic (NG) response and rectal temperature were determined to assess the potentially sedative and hypothermic effects of putative anxiolytics. USV were reduced at low doses and in both temperature conditions by the full 5-HT1A receptor agonists flesinoxan and 8-OH-DPAT (8-hydroxy-2-(di-n-propylamino) tetralin.HBr) and the partial 5-HT1A receptor agonists buspirone, ipsapirone and BMY 7378 (2-[4-[4-[2-pyrimidinyl]-1,2-piperazinyl]butyl]-1,2-benzi-isoth iozol-3-(2H)one-1,1-dioxide. 2HCl). The 5-HT1A receptor antagonists NAN-190 (1-(2-methoxyphenyl)-4-[4-(2-phtalimido)-butyl]piperazide.2H Cl), (+/-)-WAY 100,135 (+/-)-(N-tert-butyl-3(4-(2-methoxy phenyl)piperazin-1 -yl)-2-phenyl propionamine.2HCl), and ((S)-UH-301 (S)-5-fluoro-8-hydroxy-2-(di-n-propyl-amino)tetralin.HBr) reduced USV at higher doses and only in one of both test conditions.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related 5-HT Receptor Products

CAS 2113-05-5 m-Chlorophenylbiguanide hydrochloride

m-Chlorophenylbiguanide hydrochloride
(CAS: 2113-05-5)

m-Chlorophenylbiguanide hydrochloride is the hydrochloride salt of chlorophenylbiguanide, which is a selective and prototypical potent 5-HT3 serotonin receptor ...

CAS 34233-69-7 Clozapine N-oxide

Clozapine N-oxide
(CAS: 34233-69-7)

Clozapine N-oxide is a major metabolite of clozapine, and acts as an antagonist of 5-HT receptor.

CAS 77145-61-0 SR 57227A hydrochloride

SR 57227A hydrochloride
(CAS: 77145-61-0)

SR 57227 hydrochloride is a selective and high affinity 5-HT3 receptor agonist. SR 57227 exhibits anti-depressant like effects and decreases isolation-induced a...

CAS 866206-54-4 PRX 08066

PRX 08066
(CAS: 866206-54-4)

PRX 08066, a selective 5-hydroxytryptamine receptor 2B(5-HT2BR) antagonist, causes selective vasodilation of pulmonary arteries. Its IC50 value is 3.4 nM. It ca...

CAS 191592-09-3 5-HT2 antagonist 1

5-HT2 antagonist 1
(CAS: 191592-09-3)

A potent antagonist of 5-HT2 receptor

CAS 691846-63-6 GMC 3-15

GMC 3-15
(CAS: 691846-63-6)

GMC 3-15 is a potent and selective 5-HT1B/1D antagonist.

CAS 133454-47-4 Iloperidone

(CAS: 133454-47-4)

Iloperidone displays high affinity (Ki < 10 nM) for norepinephrine alpha(1)-adrenoceptors, dopamine D(3) and serotonin 5-HT(2A) receptors.

(CAS: 201038-74-6)

SB-269970 is a selective 5-HT7 receptor antagonist (pKi of 8.3) with >50-fold selectivity against other receptors, on amphetamine and ketamine-induced hyperacti...

Chemical Structure

CAS 161611-99-0 DU125530

Quick Inquiry

Verification code

Featured Items