ROMIFIDINE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C9H9BrFN3
Molecular Weight	258.09
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

FC1=CC=CC(Br)=C1NC2=NCCN2

InChI

InChIKey=KDPNLRQZHDJRFU-UHFFFAOYSA-N

InChI=1S/C9H9BrFN3/c10-6-2-1-3-7(11)8(6)14-9-12-4-5-13-9/h1-3H,4-5H2,(H2,12,13,14)

HIDE SMILES / InChI

Molecular Formula	C9H9BrFN3
Molecular Weight	258.09
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.fda.gov/ohrms/dockets/98fr/141-229-fois001.pdf

Romifidine is an alpha2-adrenergic agonist, which as a sedative and analgesic in horses. The drug was approved by FDA under the name Sedivet. It has no use in humans.

CNS Activity

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Alpha-2B adrenergic receptor 13 Target ID: O77721 Gene ID: NA Gene Symbol: ADRA2B Target Organism: Equus caballus (Horse) Sources: https://www.fda.gov/ohrms/dockets/98fr/141-229-fois001.pdf	Agonist 2678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Sedation 4 Sources: http://files.boehringer.com.au/files/CMI/Sedivet%20ANZ.pdf	Primary		Approved 8429	SEDIVET Approved Use For use as a sedative and analgesic to facilitate handling, clinical examinations, clinical procedures, and minor surgical procedures in adult horses; and for use as a preanesthetic prior to the induction of general anesthesia in adult horses. Launch Date 2004

PubMed

Title	Date	PubMed
Cardiovascular effects of romifidine in dogs.	2001 Apr	11327453
Effect of two anaesthetic regimens on airway nitric oxide production in horses.	2001 Jan	11575389
Comparison of detomidine and romifidine as premedicants before ketamine and halothane anesthesia in horses undergoing elective surgery.	2001 Mar	11277200
Effect of romifidine on gastrointestinal motility, assessed by transrectal ultrasonography.	2001 Nov	11720028
Cardiovascular effects of romifidine in the standing horse.	2002 Apr	12027592
Analgesic, sedative and haemodynamic effects of spinally administered romifidine in female goats.	2002 Feb	11913823
Cardiovascular effects of a high dose of romifidine in propofol-anesthetized cats.	2002 Sep	12224853
Effects of alpha-2 adrenoceptor agonists during recovery from isoflurane anaesthesia in horses.	2003 Mar	12638794
The echocardiographic effects of romifidine in dogs with and without prior or concurrent administration of glycopyrrolate.	2003 Oct	12925178
Effects of tiletamine/zolazepam-romifidine-atropine in ocelots (Leopardus pardalis).	2004 Jul	15268694
Comparison of morphine and butorphanol as pre-anaesthetic agents in combination with romifidine for field castration in ponies.	2005 Jan	15663735
Effect of romifidine on the nociceptive withdrawal reflex and temporal summation in conscious horses.	2005 Nov	16334961
Romifidine or medetomidine premedication before propofol-sevoflurane anaesthesia in dogs.	2005 Oct	16207314
Risk factors for colic in horses after general anaesthesia for MRI or nonabdominal surgery: absence of evidence of effect from perianaesthetic morphine.	2006 Jul	16866208
A2-agonists in sheep: a review.	2006 Mar	16475998
Comparison of romifidine and medetomidine pre-medication in propofol-isoflurane anaesthetised dogs.	2006 Nov	17054484
Cardiorespiratory effects of desflurane in dogs given romifidine or medetomidine before induction of anesthesia with propofol.	2006 Oct	17042386
The effects of detomidine, romifidine or acepromazine on echocardiographic measurements and cardiac function in normal horses.	2007 Jan	17238956
Epithelial expression of mRNA and protein for IL-6, IL-10 and TNF-alpha in endobronchial biopsies in horses with recurrent airway obstruction.	2008 Feb 23	18294392
Comparison of ketamine and S(+)-ketamine, with romifidine and diazepam, for total intravenous anesthesia in horses.	2008 Jan	17565569
Sedative and cardiorespiratory effects of three doses of romifidine in comparison with medetomidine in five cats.	2008 Jan 19	18204032
A comparison of recovery times and characteristics with sevoflurane and isoflurane anaesthesia in horses undergoing magnetic resonance imaging.	2008 Sep	18466165
Effect of sedation with detomidine and butorphanol on pulmonary gas exchange in the horse.	2009 May 7	19422714
Alfaxalone in cyclodextrin for induction and maintenance of anaesthesia in ponies undergoing field castration.	2009 Sep	19709052
Human exposures to immobilising agents: results of an online survey.	2010 Aug 28	20802186
Alpha-2 agonists as pain therapy in horses.	2010 Dec	21056297
Effects of adding butorphanol to a balanced anaesthesia protocol during arthroscopic surgery in horses.	2010 Mar 13	20228366

Patents

Sample Use Guides

In Vivo Use Guide

Sedative doses ranged between 30 and 100 mcg/kg; preanesthetic doses ranged between 40 and 100 mcg/kg.

Route of Administration: Intravenous

In Vitro Use Guide

Rat spinal cord preparations were treated with romifidine at concentrations from 1 to 1000 nM. The drug depressed both the high intensity and low intensity excitatory postsynaptic potential with EC50 value of 23.4 nM.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:21:53 GMT 2023` Edited by `admin` on `Fri Dec 15 16:21:53 GMT 2023`
Record UNII	876351L05K
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ROMIFIDINE

Official Name

English

SEDIVET

Brand Name

English

ROMIFIDINE [MART.]

Common Name

English

ROMIFIDINE [MI]

Common Name

English

romifidine [INN]

Common Name

English

Classification Tree Code System Code

CFR

21 CFR 522.2076