Product Name

Buspirone Hydrochloride

CAS Number

33386-08-02

LGM Pharma is an API distributor. LGM Pharma can supply CGMP and/or DMF products, subject to availability and manufacturer requirements. LGM Pharma does not sell or supply APIs or finished dosage products to individual patients, doctors, pharmacies, or any pharmaceutical companies.

Questions? Call our customer API support number 1-(800)-881-8210

Product Name:
Buspirone Hydrochloride
CAS Number:
33386-08-02
Indication:
For the management of anxiety disorders or the short-term relief of the symptoms of anxiety, and also as an augmention of SSRI-treatment against depression.
Mode of Action:

Buspirone binds to 5-HT type 1A serotonin receptors on presynaptic neurons in the dorsal raphe and on postsynaptic neurons in the hippocampus, thus inhibiting the firing rate of 5-HT-containing neurons in the dorsal raphe. Buspirone also binds at dopamine type 2 (DA2) receptors, blocking presynaptic dopamine receptors. Buspirone increases firing in the locus ceruleus, an area of brain where norepinephrine cell bodies are found in high concentration. The net result of buspirone actions is that serotonergic activity is suppressed while noradrenergic and dopaminergic cell firing is enhanced.

Pharmacodynamics:

Buspirone is used in the treatment of generalized anxiety where it has advantages over other antianxiety drugs because it does not cause sedation (drowsiness) and does not cause tolerance or physical dependence. Buspirone differs from typical benzodiazepine anxiolytics in that it does not exert anticonvulsant or muscle relaxant effects. It also lacks the prominent sedative effect that is associated with more typical anxiolytics. in vitro preclinical studies have shown that buspirone has a high affinity for serotonin (5-HT1A) receptors. Buspirone has no significant affinity for benzodiazepine receptors and does not affect GABA binding in vitro or in vivo when tested in preclinical models. Buspirone has moderate affinity for brain D2-dopamine receptors. Some studies do suggest that buspirone may have indirect effects on other neurotransmitter systems.

Metabolism:

Metabolized hepatically, primarily by oxidation by cytochrome P450 3A4 producing several hydroxylated derivatives and a pharmacologically active metabolite, 1-pyrimidinylpiperazine (1-PP)

Toxicity:

Oral, rat LD50 = 136 mg/kg. Symptoms of overdose include dizziness, drowsiness, nausea or vomiting, severe stomach upset, and unusually small pupils.

IUPAC:
8-(4-(4-(2-Pyrimidinyl)-1-piperazinyl)butyl)-8-azaspiro(4.5)decane-7, 9-dione monohydrochloride 8-Azaspiro(4, 5)decane-7, 9-dione, 8-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-, monohydrochloride
ATC:
N05BE01
PubChem:
2477
DrugBank:
DB00490
Formula:
C21-H31-N5-O2.Cl-H
Molecular Mass:
421.9698
Synonyms:
1,1-Cyclopentanediacetimide, N-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-, hydrochloride, 8-(4-(4-(2-Pyrimidinyl)-1-piperazinyl)butyl)-8-azaspiro(4.5)decane-7,9-dione hydrochloride, 8-Azaspiro(4,5)decane-7,9-dione, 8-(4-(4-(2-pyrimidinyl)-1-piperazinyl)butyl)-, monohydrochloride, Ansitec, Anxinil, Anxiolan, Apo-Buspirone, Barpil, Biron, Busirone, Buspar, Buspimen, Buspinol, Buspirone HCl, Buspirone hydrochloride, Censpar, Effiplen, EINECS 251-489-4, Establix, Itagil, Kallmiren, Lucelan, Mabuson, MJ 9022-1, N-(4-(4-(2-Pyrimidinyl)-1-piperazinyl)butyl)-1,1-cyclopentanediacetamide monohydrochloride, Narol, Nerbet, Normaton, Relac, Sburol, Spamilan, Travin, Tutran, UNII-207LT9J9OC
SMILES:
c1cnc(nc1)N2CCN(CC2)CCCCN3C(=O)CC4(CCCC4)CC3=O.Cl
AHFS Code:
28:24.9
InChi:
1S/C21H31N5O2.ClH/c27-18-16-21(6-1-2-7-21)17-19(28)26(18)11-4-3-10-24-12-14-25(15-13-24)20-22-8-5-9-23-20;/h5,8-9H,1-4,6-7,10-17H2;1H

Products currently covered by valid US Patents are offered for R&D use in accordance with 35 USC 271(e)+A13(1). Any patent infringement and resulting liability is solely at buyer risk.

LGM currently offers Monoclonal Antibodies (mAbs) for non-GMP/R&D use. Please inquire about Monoclonal Antibodies produced under GMP conditions.

Questions? Call our customer API support number 1-(800)-881-8210. 

Ask us about this product

API’s From Quality Manufacturers:

  • Streamlined API supply towards initial research stages as well as larger quantities of cGMP material for clinical trials and product commercialization
  • Premium quality GMP certified and fully accredited API manufacturing plants
  • Technical packages as well as access to filed DMF, ASMF or CEP (subject to availability)
  • Regulatory and technical assistance towards any submission type based on specific customer requirements

Find an API Product

SEARCH
Generic filters